Jason Gestwicki, PhD
Professor
Pharmaceutical Chemistry
School of Pharmacy

Many of our chemical probes target allosteric and protein-protein interaction sites on the molecular chaperones and we have a significant interest in discovering inhibitors of "difficult" targets. We hope to better understand the logic of protein folding and misfolding and use this information to design more effective therapies.

• Proteostasis perturbation of N-Myc leveraging HSP70 mediated protein turnover improves treatment of neuroendocrine prostate cancer.
  Nature communications 2024 Xu P, Yang JC, Chen B, Ning S, Zhang X, Wang L, Nip C, Shen Y, Johnson OT, Grigorean G, Phinney B, Liu L, Wei Q, Corey E, Tepper CG, Chen HW, Evans CP, Dall'Era MA, Gao AC, Gestwicki JE, Liu C
• iPSC-induced neurons with the V337M MAPT mutation are selectively vulnerable to caspase-mediated cleavage of tau and apoptotic cell death.
  Molecular and cellular neurosciences 2024 Theofilas P, Wang C, Butler D, Morales DO, Petersen C, Ambrose A, Chin B, Yang T, Khan S, Ng R, Kayed R, Karch CM, Miller BL, Gestwicki JE, Gan L, Temple S, Arkin MR, Grinberg LT
• Asymmetric apical domain states of mitochondrial Hsp60 coordinate substrate engagement and chaperonin assembly.
  Nature structural & molecular biology 2024 Braxton JR, Shao H, Tse E, Gestwicki JE, Southworth DR
• Plexin D1 emerges as a novel target in the development of neural lineage plasticity in treatment-resistant prostate cancer.
  Oncogene 2024 Chen B, Xu P, Yang JC, Nip C, Wang L, Shen Y, Ning S, Shang Y, Corey E, Gao AC, Gestwicki JE, Wei Q, Liu L, Liu C
• DSFworld: A flexible and precise tool to analyze differential scanning fluorimetry data.
  Protein science : a publication of the Protein Society 2024 Wu T, Gale-Day ZJ, Gestwicki JE
• Exploration of the binding determinants of protein phosphatase 5 (PP5) reveals a chaperone-independent activation mechanism.
  The Journal of biological chemistry 2024 Devi S, Charvat A, Millbern Z, Vinueza N, Gestwicki JE
• Illuminating the function of the orphan transporter, SLC22A10, in humans and other primates.
  Nature communications 2024 Yee SW, Ferrández-Peral L, Alentorn-Moron P, Fontsere C, Ceylan M, Koleske ML, Handin N, Artegoitia VM, Lara G, Chien HC, Zhou X, Dainat J, Zalevsky A, Sali A, Brand CM, Wolfreys FD, Yang J, Gestwicki…
• Protein-adaptive differential scanning fluorimetry using conformationally responsive dyes.
  Nature biotechnology 2024 Wu T, Yu JC, Suresh A, Gale-Day ZJ, Alteen MG, Woo AS, Millbern Z, Johnson OT, Carroll EC, Partch CL, Fourches D, Vinueza NR, Vocadlo DJ, Gestwicki JE
• Heat shock protein 72 supports extracellular matrix production in metastatic mammary tumors.
  Cell stress & chaperones 2024 Lang BJ, Holton KM, Guerrero-Gimenez ME, Okusha Y, Magahis PT, Shi A, Neguse M, Venkatesh S, Nhu AM, Gestwicki JE, Calderwood SK
• Plexin D1 emerges as a novel target in the development of neural lineage plasticity in treatment-resistant prostate cancer.
  Research square 2024 Liu C, Chen B, Xu P, Yang J, Nip C, Wang L, Shen Y, Ning S, Shang Y, Corey E, Gao AC, Gestwicki J, Wei Q, Liu L
• Plasmodium falciparum heat shock proteins as antimalarial drug targets: An update.
  Cell stress & chaperones 2024 Ahmad T, Alhammadi BA, Almaazmi SY, Arafa S, Blatch GL, Dutta T, Gestwicki JE, Keyzers RA, Shonhai A, Singh H
• A missense mutation in the Hspa8 gene encoding heat shock cognate protein 70 causes neuroaxonal dystrophy in rats.
  Frontiers in neuroscience 2024 Tanaka M, Fujikawa R, Sekiguchi T, Hernandez J, Johnson OT, Tanaka D, Kumafuji K, Serikawa T, Hoang Trung H, Hattori K, Mashimo T, Kuwamura M, Gestwicki JE, Kuramoto T
• Stress biology: Complexity and multifariousness in health and disease.
  Cell stress & chaperones 2024 Mayer MP, Blair L, Blatch GL, Borges TJ, Chadli A, Chiosis G, de Thonel A, Dinkova-Kostova A, Ecroyd H, Edkins AL, Eguchi T, Fleshner M, Foley KP, Fragkostefanakis S, Gestwicki J, Goloubinoff P, …
• J-domain proteins: From molecular mechanisms to diseases.
  Cell stress & chaperones 2023 Marszalek J, De Los Rios P, Cyr D, Mayer MP, Adupa V, Andréasson C, Blatch GL, Braun JEA, Brodsky JL, Bukau B, Chapple JP, Conz C, Dementin S, Genevaux P, Genest O, Goloubinoff P, Gestwicki J, Hammond…
• Cholesterol Dysregulation Drives Seed-Dependent Tau Aggregation in Patient Stem Cell-Derived Models of Tauopathy.
  bioRxiv : the preprint server for biology 2023 Lam M, Kuo SY, Reis S, Gestwicki JE, Silva MC, Haggarty SJ
• Protocol for performing and optimizing differential scanning fluorimetry experiments.
  STAR protocols 2023 Wu T, Hornsby M, Zhu L, Yu JC, Shokat KM, Gestwicki JE
• De novo designed Hsp70 activator dissolves intracellular condensates.
  bioRxiv : the preprint server for biology 2023 Zhang JZ, Greenwood N, Hernandez J, Cuperus JT, Huang B, Ryder BD, Queitsch C, Gestwicki JE, Baker D
• Phosphorylation of a Cleaved Tau Proteoform at a Single Residue Inhibits Binding to the E3 Ubiquitin Ligase, CHIP.
  bioRxiv : the preprint server for biology 2023 Nadel CM, Wucherer K, Oehler A, Thwin AC, Basu K, Callahan MD, Southworth DR, Mordes DA, Craik CS, Gestwicki JE
• An Unbiased Screen Identified the Hsp70-BAG3 Complex as a Regulator of Myosin-Binding Protein C3.
  JACC. Basic to translational science 2023 Thompson AD, Wagner MJ, Rodriguez J, Malhotra A, Vander Roest S, Lilienthal U, Shao H, Vignesh M, Weber K, Yob JM, Prosser BL, Helms AS, Gestwicki JE, Ginsburg D, Day SM
• The E3 Ubiquitin Ligase, CHIP/STUB1, Inhibits Aggregation of Phosphorylated Proteoforms of Microtubule-associated Protein Tau (MAPT).
  Journal of molecular biology 2023 Nadel CM, Thwin AC, Callahan M, Lee K, Connelly E, Craik CS, Southworth DR, Gestwicki JE
• Asymmetric apical domain states of mitochondrial Hsp60 coordinate substrate engagement and chaperonin assembly.
  bioRxiv : the preprint server for biology 2023 Braxton JR, Shao H, Tse E, Gestwicki JE, Southworth DR
• Mitoribosome sensitivity to HSP70 inhibition uncovers metabolic liabilities of castration-resistant prostate cancer.
  PNAS nexus 2023 Echtenkamp FJ, Ishida R, Rivera-Marquez GM, Maisiak M, Johnson OT, Shrimp JH, Sinha A, Ralph SJ, Nisbet I, Cherukuri MK, Gestwicki JE, Neckers LM
• A Comprehensive Enumeration of the Human Proteostasis Network. 2. Components of the Autophagy-Lysosome Pathway.
  bioRxiv : the preprint server for biology 2023 Elsasser S, Elia LP, Morimoto RI, Powers ET, Finley D, Costa B, Budron M, Tokuno Z, Wang S, Iyer RG, Barth B, Mockler E, Finkbeiner S, Gestwicki JE, Richardson RAK, Stoeger T, Tan EP, Xiao Q, Cole CM,…
• Allosteric inhibition of HSP70 in collaboration with STUB1 augments enzalutamide efficacy in antiandrogen resistant prostate tumor and patient-derived models.
  Pharmacological research 2023 Xu P, Yang JC, Ning S, Chen B, Nip C, Wei Q, Liu L, Johnson OT, Gao AC, Gestwicki JE, Evans CP, Liu C
• Chemical Features of Polyanions Modulate Tau Aggregation and Conformational States.
  Journal of the American Chemical Society 2023 Montgomery KM, Carroll EC, Thwin AC, Quddus AY, Hodges P, Southworth DR, Gestwicki JE
• Conformationally responsive dyes enable protein-adaptive differential scanning fluorimetry.
  bioRxiv : the preprint server for biology 2023 Wu T, Yu JC, Suresh A, Gale-Day ZJ, Alteen MG, Woo AS, Millbern Z, Johnson OT, Carroll EC, Partch CL, Fourches D, Vinueza NR, Vocadlo DJ, Gestwicki JE
• Iterative computational design and crystallographic screening identifies potent inhibitors targeting the Nsp3 macrodomain of SARS-CoV-2.
  Proceedings of the National Academy of Sciences of the United States of America 2023 Gahbauer S, Correy GJ, Schuller M, Ferla MP, Doruk YU, Rachman M, Wu T, Diolaiti M, Wang S, Neitz RJ, Fearon D, Radchenko DS, Moroz YS, Irwin JJ, Renslo AR, Taylor JC, Gestwicki JE, von Delft F, …
• N-myc-Mediated Translation Control Is a Therapeutic Vulnerability in Medulloblastoma.
  Cancer research 2023 Kuzuoglu-Ozturk D, Aksoy O, Schmidt C, Lea R, Larson JD, Phelps RRL, Nasholm N, Holt M, Contreras A, Huang M, Wong-Michalak S, Shao H, Wechsler-Reya R, Phillips JJ, Gestwicki JE, Ruggero D, Weiss WA
• Iterative computational design and crystallographic screening identifies potent inhibitors targeting the Nsp3 Macrodomain of SARS-CoV-2.
  bioRxiv : the preprint server for biology 2022 Gahbauer S, Correy GJ, Schuller M, Ferla MP, Doruk YU, Rachman M, Wu T, Diolaiti M, Wang S, Neitz RJ, Fearon D, Radchenko D, Moroz Y, Irwin JJ, Renslo AR, Taylor JC, Gestwicki JE, von Delft F, …
• Allosteric HSP70 inhibitors perturb mitochondrial proteostasis and overcome proteasome inhibitor resistance in multiple myeloma.
  Cell chemical biology 2022 Ferguson ID, Lin YT, Lam C, Shao H, Tharp KM, Hale M, Kasap C, Mariano MC, Kishishita A, Patiño Escobar B, Mandal K, Steri V, Wang D, Phojanakong P, Tuomivaara ST, Hann B, Driessen C, Van Ness B, …
• A campaign targeting a conserved Hsp70 binding site uncovers how subcellular localization is linked to distinct biological activities.
  Cell chemical biology 2022 Shao H, Taguwa S, Gilbert L, Shkedi A, Sannino S, Guerriero CJ, Gale-Day ZJ, Young ZT, Brodsky JL, Weissman J, Gestwicki JE, Frydman J
• Multivalent protein-protein interactions are pivotal regulators of eukaryotic Hsp70 complexes.
  Cell stress & chaperones 2022 Johnson OT, Gestwicki JE
• Stress routes clients to the proteasome via a BAG2 ubiquitin-independent degradation condensate.
  Nature communications 2022 Carrettiero DC, Almeida MC, Longhini AP, Rauch JN, Han D, Zhang X, Najafi S, Gestwicki JE, Kosik KS
• Multi-protein complexes as drug targets.
  Cell chemical biology 2022 Gestwicki JE
• Microglial NF-κB drives tau spreading and toxicity in a mouse model of tauopathy.
  Nature communications 2022 Wang C, Fan L, Khawaja RR, Liu B, Zhan L, Kodama L, Chin M, Li Y, Le D, Zhou Y, Condello C, Grinberg LT, Seeley WW, Miller BL, Mok SA, Gestwicki JE, Cuervo AM, Luo W, Gan L
• The YΦ motif defines the structure-activity relationships of human 20S proteasome activators.
  Nature communications 2022 Opoku-Nsiah KA, de la Pena AH, Williams SK, Chopra N, Sali A, Lander GC, Gestwicki JE
• Two distinct classes of cochaperones compete for the EEVD motif in heat shock protein 70 to tune its chaperone activities.
  The Journal of biological chemistry 2022 Johnson OT, Nadel CM, Carroll EC, Arhar T, Gestwicki JE
• Selective vulnerabilities in the proteostasis network of castration-resistant prostate cancer.
  Cell chemical biology 2022 Shkedi A, Taylor IR, Echtenkamp F, Ramkumar P, Alshalalfa M, Rivera-Márquez GM, Moses MA, Shao H, Karnes RJ, Neckers L, Feng F, Kampmann M, Gestwicki JE
• Analogs of the Heat Shock Protein 70 Inhibitor MKT-077 Suppress Medullary Thyroid Carcinoma Cells.
  International journal of molecular sciences 2022 Hong SK, Starenki D, Johnson OT, Gestwicki JE, Park JI
• The interactions of molecular chaperones with client proteins: why are they so weak?
  The Journal of biological chemistry 2021 Arhar T, Shkedi A, Nadel CM, Gestwicki JE
• Inhibitor Combinations Reveal Wiring of the Proteostasis Network in Prostate Cancer Cells.
  Journal of medicinal chemistry 2021 Shkedi A, Adkisson M, Schroeder A, Eckalbar WL, Kuo SY, Neckers L, Gestwicki JE
• The structure of an Hsp90-immunophilin complex reveals cochaperone recognition of the client maturation state.
  Molecular cell 2021 Lee K, Thwin AC, Nadel CM, Tse E, Gates SN, Gestwicki JE, Southworth DR
• Adhesion-mediated mechanosignaling forces mitohormesis.
  Cell metabolism 2021 Tharp KM, Higuchi-Sanabria R, Timblin GA, Ford B, Garzon-Coral C, Schneider C, Muncie JM, Stashko C, Daniele JR, Moore AS, Frankino PA, Homentcovschi S, Manoli SS, Shao H, Richards AL, Chen KH, Hoeve …
• Retraction of "Enantioselective Organocatalytic Hantzsch Synthesis of Polyhydroquinolines".
  Organic letters 2021 Evans CG, Gestwicki JE
• Acetylated tau inhibits chaperone-mediated autophagy and promotes tau pathology propagation in mice.
  Nature communications 2021 Caballero B, Bourdenx M, Luengo E, Diaz A, Sohn PD, Chen X, Wang C, Juste YR, Wegmann S, Patel B, Young ZT, Kuo SY, Rodriguez-Navarro JA, Shao H, Lopez MG, Karch CM, Goate AM, Gestwicki JE, Hyman BT, …
• Fragment binding to the Nsp3 macrodomain of SARS-CoV-2 identified through crystallographic screening and computational docking.
  Science advances 2021 Schuller M, Correy GJ, Gahbauer S, Fearon D, Wu T, Díaz RE, Young ID, Carvalho Martins L, Smith DH, Schulze-Gahmen U, Owens TW, Deshpande I, Merz GE, Thwin AC, Biel JT, Peters JK, Moritz M, Herrera N,…
• Inhibitors of heat shock protein 70 (Hsp70) with enhanced metabolic stability reduce tau levels.
  Bioorganic & medicinal chemistry letters 2021 Shao H, Li X, Hayashi S, Bertron JL, Schwarz DMC, Tang BC, Gestwicki JE
• Hsp70 chaperone blocks α-synuclein oligomer formation via a novel engagement mechanism.
  The Journal of biological chemistry 2021 Tao J, Berthet A, Citron YR, Tsiolaki PL, Stanley R, Gestwicki JE, Agard DA, McConlogue L
• Functional genomics screen identifies proteostasis targets that modulate prion protein (PrP) stability.
  Cell stress & chaperones 2021 Abrams J, Arhar T, Mok SA, Taylor IR, Kampmann M, Gestwicki JE
• Chemical validation of a druggable site on Hsp27/HSPB1 using in silico solvent mapping and biophysical methods.
  Bioorganic & medicinal chemistry 2021 Makley LN, Johnson OT, Ghanakota P, Rauch JN, Osborn D, Wu TS, Cierpicki T, Carlson HA, Gestwicki JE
• Exported plasmodial J domain protein, PFE0055c, and PfHsp70-x form a specific co-chaperone-chaperone partnership.
  Cell stress & chaperones 2020 Dutta T, Singh H, Gestwicki JE, Blatch GL
• Fragment Binding to the Nsp3 Macrodomain of SARS-CoV-2 Identified Through Crystallographic Screening and Computational Docking.
  bioRxiv : the preprint server for biology 2020 Schuller M, Correy GJ, Gahbauer S, Fearon D, Wu T, Díaz RE, Young ID, Martins LC, Smith DH, Schulze-Gahmen U, Owens TW, Deshpande I, Merz GE, Thwin AC, Biel JT, Peters JK, Moritz M, Herrera N, …
• Luminescence complementation assay for measurement of binding to protein C-termini in live cells.
  Analytical biochemistry 2020 Nadel CM, Ran X, Gestwicki JE
• A Phosphoramidate Strategy Enables Membrane Permeability of a Non-nucleotide Inhibitor of the Prolyl Isomerase Pin1.
  ACS medicinal chemistry letters 2020 Schwarz DMC, Williams SK, Dillenburg M, Wagner CR, Gestwicki JE
• Inhibition of DNAJ-HSP70 interaction improves strength in muscular dystrophy.
  The Journal of clinical investigation 2020 Bengoechea R, Findlay AR, Bhadra AK, Shao H, Stein KC, Pittman SK, Daw JA, Gestwicki JE, True HL, Weihl CC
• Differential scanning fluorimetry (DSF) screen to identify inhibitors of Hsp60 protein-protein interactions.
  Organic & biomolecular chemistry 2020 Shao H, Oltion K, Wu T, Gestwicki JE
• A Novel Radioligand Reveals Tissue Specific Pharmacological Modulation of Glucocorticoid Receptor Expression with Positron Emission Tomography.
  ACS chemical biology 2020 Huang Y, Zhao N, Wang YH, Truillet C, Wei J, Blecha JE, VanBrocklin HF, Seo Y, Sayeed M, Feldman BJ, Aggarwal R, Behr SC, Shao H, Wilson DM, Villanueva-Meyer JE, Gestwicki JE, Evans MJ
• Mortalin/HSPA9 targeting selectively induces KRAS tumor cell death by perturbing mitochondrial membrane permeability.
  Oncogene 2020 Wu PK, Hong SK, Starenki D, Oshima K, Shao H, Gestwicki JE, Tsai S, Park JI
• Pharmacologic dissection of the overlapping impact of heat shock protein family members on platelet function.
  Journal of thrombosis and haemostasis : JTH 2020 Jackson JW, Rivera-Marquez GM, Beebe K, Tran AD, Trepel JB, Gestwicki JE, Blagg BSJ, Ohkubo S, Neckers LM
• Mortalin (HSPA9) facilitates BRAF-mutant tumor cell survival by suppressing ANT3-mediated mitochondrial membrane permeability.
  Science signaling 2020 Wu PK, Hong SK, Chen W, Becker AE, Gundry RL, Lin CW, Shao H, Gestwicki JE, Park JI
• Management of Hsp90-Dependent Protein Folding by Small Molecules Targeting the Aha1 Co-Chaperone.
  Cell chemical biology 2020 Singh JK, Hutt DM, Tait B, Guy NC, Sivils JC, Ortiz NR, Payan AN, Komaragiri SK, Owens JJ, Culbertson D, Blair LJ, Dickey C, Kuo SY, Finley D, Dyson HJ, Cox MB, Chaudhary J, Gestwicki JE, Balch WE
• Neutral analogs of the heat shock protein 70 (Hsp70) inhibitor, JG-98.
  Bioorganic & medicinal chemistry letters 2020 Shao H, Gestwicki JE
• Tryptophan scanning mutagenesis as a way to mimic the compound-bound state and probe the selectivity of allosteric inhibitors in cells.
  Chemical science 2020 Taylor IR, Assimon VA, Kuo SY, Rinaldi S, Li X, Young ZT, Morra G, Green K, Nguyen D, Shao H, Garneau-Tsodikova S, Colombo G, Gestwicki JE
• Promoting tau secretion and propagation by hyperactive p300/CBP via autophagy-lysosomal pathway in tauopathy.
  Molecular neurodegeneration 2020 Chen X, Li Y, Wang C, Tang Y, Mok SA, Tsai RM, Rojas JC, Karydas A, Miller BL, Boxer AL, Gestwicki JE, Arkin M, Cuervo AM, Gan L
• Individualized management of genetic diversity in Niemann-Pick C1 through modulation of the Hsp70 chaperone system.
  Human molecular genetics 2020 Wang C, Scott SM, Sun S, Zhao P, Hutt DM, Shao H, Gestwicki JE, Balch WE
• End-Binding E3 Ubiquitin Ligases Enable Protease Signaling.
  ACS chemical biology 2019 Ravalin M, Basu K, Gestwicki JE, Craik CS
• Author Correction: Hsp70 and Hsp40 inhibit an inter-domain interaction necessary for transcriptional activity in the androgen receptor.
  Nature communications 2019 Eftekharzadeh B, Banduseela VC, Chiesa G, Martínez-Cristóbal P, Rauch JN, Nath SR, Schwarz DMC, Shao H, Marin-Argany M, Di Sanza C, Giorgetti E, Yu Z, Pierattelli R, Felli IC, Brun-Heath I, García J, …
• Compromised function of the ESCRT pathway promotes endolysosomal escape of tau seeds and propagation of tau aggregation.
  The Journal of biological chemistry 2019 Chen JJ, Nathaniel DL, Raghavan P, Nelson M, Tian R, Tse E, Hong JY, See SK, Mok SA, Hein MY, Southworth DR, Grinberg LT, Gestwicki JE, Leonetti MD, Kampmann M
• Pathogenic Tau Impairs Axon Initial Segment Plasticity and Excitability Homeostasis.
  Neuron 2019 Sohn PD, Huang CT, Yan R, Fan L, Tracy TE, Camargo CM, Montgomery KM, Arhar T, Mok SA, Freilich R, Baik J, He M, Gong S, Roberson ED, Karch CM, Gestwicki JE, Xu K, Kosik KS, Gan L
• Hsp70 and Hsp40 inhibit an inter-domain interaction necessary for transcriptional activity in the androgen receptor.
  Nature communications 2019 Eftekharzadeh B, Banduseela VC, Chiesa G, Martínez-Cristóbal P, Rauch JN, Nath SR, Schwarz DMC, Shao H, Marin-Argany M, Di Sanza C, Giorgetti E, Yu Z, Pierattelli R, Felli IC, Brun-Heath I, García J, …
• Mechanism of Action of VP1-001 in cryAB(R120G)-Associated and Age-Related Cataracts.
  Investigative ophthalmology & visual science 2019 Molnar KS, Dunyak BM, Su B, Izrayelit Y, McGlasson-Naumann B, Hamilton PD, Qian M, Covey DF, Gestwicki JE, Makley LN, Andley UP
• Specificity for latent C termini links the E3 ubiquitin ligase CHIP to caspases.
  Nature chemical biology 2019 Ravalin M, Theofilas P, Basu K, Opoku-Nsiah KA, Assimon VA, Medina-Cleghorn D, Chen YF, Bohn MF, Arkin M, Grinberg LT, Craik CS, Gestwicki JE
• Correction: The pleiotropic effects of TNFα in breast cancer subtypes is regulated by TNFAIP3/A20.
  Oncogene 2019 Lee E, Ouzounova M, Piranlioglu R, Ma MT, Guzel M, Marasco D, Chadli A, Gestwicki JE, Cowell JK, Wicha MS, Hassan KA, Korkaya H
• A Legionella pneumophila Kinase Phosphorylates the Hsp70 Chaperone Family to Inhibit Eukaryotic Protein Synthesis.
  Cell host & microbe 2019 Moss SM, Taylor IR, Ruggero D, Gestwicki JE, Shokat KM, Mukherjee S
• Zika Virus Dependence on Host Hsp70 Provides a Protective Strategy against Infection and Disease.
  Cell reports 2019 Taguwa S, Yeh MT, Rainbolt TK, Nayak A, Shao H, Gestwicki JE, Andino R, Frydman J
• Designing de Novo Small Molecules That Control Heat Shock Protein 70 (Hsp70) and Heat Shock Organizing Protein (HOP) within the Chaperone Protein-Folding Machinery.
  Journal of medicinal chemistry 2018 Zaiter SS, Huo Y, Tiew FY, Gestwicki JE, McAlpine SR
• Myopathy associated BAG3 mutations lead to protein aggregation by stalling Hsp70 networks.
  Nature communications 2018 Meister-Broekema M, Freilich R, Jagadeesan C, Rauch JN, Bengoechea R, Motley WW, Kuiper EFE, Minoia M, Furtado GV, van Waarde MAWH, Bird SJ, Rebelo A, Zuchner S, Pytel P, Scherer SS, Morelli FF, Carra…
• Predicting protein targets for drug-like compounds using transcriptomics.
  PLoS computational biology 2018 Pabon NA, Xia Y, Estabrooks SK, Ye Z, Herbrand AK, Süß E, Biondi RM, Assimon VA, Gestwicki JE, Brodsky JL, Camacho CJ, Bar-Joseph Z
• Function, evolution, and structure of J-domain proteins.
  Cell stress & chaperones 2018 Kampinga HH, Andreasson C, Barducci A, Cheetham ME, Cyr D, Emanuelsson C, Genevaux P, Gestwicki JE, Goloubinoff P, Huerta-Cepas J, Kirstein J, Liberek K, Mayer MP, Nagata K, Nillegoda NB, Pulido P, …
• A Local Allosteric Network in Heat Shock Protein 70 (Hsp70) Links Inhibitor Binding to Enzyme Activity and Distal Protein-Protein Interactions.
  ACS chemical biology 2018 Rinaldi S, Assimon VA, Young ZT, Morra G, Shao H, Taylor IR, Gestwicki JE, Colombo G
• Competing protein-protein interactions regulate binding of Hsp27 to its client protein tau.
  Nature communications 2018 Freilich R, Betegon M, Tse E, Mok SA, Julien O, Agard DA, Southworth DR, Takeuchi K, Gestwicki JE
• Inhibitors and chemical probes for molecular chaperone networks.
  The Journal of biological chemistry 2018 Gestwicki JE, Shao H
• The pleiotropic effects of TNFα in breast cancer subtypes is regulated by TNFAIP3/A20.
  Oncogene 2018 Lee E, Ouzounova M, Piranlioglu R, Ma MT, Guzel M, Marasco D, Chadli A, Gestwicki JE, Cowell JK, Wicha MS, Hassan KA, Korkaya H
• KHS101 disrupts energy metabolism in human glioblastoma cells and reduces tumor growth in mice.
  Science translational medicine 2018 Polson ES, Kuchler VB, Abbosh C, Ross EM, Mathew RK, Beard HA, da Silva B, Holding AN, Ballereau S, Chuntharpursat-Bon E, Williams J, Griffiths HBS, Shao H, Patel A, Davies AJ, Droop A, Chumas P, …
• Exploration of Benzothiazole Rhodacyanines as Allosteric Inhibitors of Protein-Protein Interactions with Heat Shock Protein 70 (Hsp70).
  Journal of medicinal chemistry 2018 Shao H, Li X, Moses MA, Gilbert LA, Kalyanaraman C, Young ZT, Chernova M, Journey SN, Weissman JS, Hann B, Jacobson MP, Neckers L, Gestwicki JE
• Aim for the core: suitability of the ubiquitin-independent 20S proteasome as a drug target in neurodegeneration.
  Translational research : the journal of laboratory and clinical medicine 2018 Opoku-Nsiah KA, Gestwicki JE
• Inhibitors of protein-protein interactions (PPIs): an analysis of scaffold choices and buried surface area.
  Current opinion in chemical biology 2018 Ran X, Gestwicki JE
• HSC70 is a chaperone for wild-type and mutant cardiac myosin binding protein C.
  JCI insight 2018 Glazier AA, Hafeez N, Mellacheruvu D, Basrur V, Nesvizhskii AI, Lee LM, Shao H, Tang V, Yob JM, Gestwicki JE, Helms AS, Day SM
• Revisiting the "Art of the Chemical Probe".
  ACS chemical biology 2018 Schwarz DMC, Gestwicki JE
• Targeting the Hsp40/Hsp70 Chaperone Axis as a Novel Strategy to Treat Castration-Resistant Prostate Cancer.
  Cancer research 2018 Moses MA, Kim YS, Rivera-Marquez GM, Oshima N, Watson MJ, Beebe KE, Wells C, Lee S, Zuehlke AD, Shao H, Bingman WE, Kumar V, Malhotra SV, Weigel NL, Gestwicki JE, Trepel JB, Neckers LM
• The disorderly conduct of Hsc70 and its interaction with the Alzheimer's-related Tau protein.
  The Journal of biological chemistry 2018 Taylor IR, Ahmad A, Wu T, Nordhues BA, Bhullar A, Gestwicki JE, Zuiderweg ERP
• Mapping interactions with the chaperone network reveals factors that protect against tau aggregation.
  Nature structural & molecular biology 2018 Mok SA, Condello C, Freilich R, Gillies A, Arhar T, Oroz J, Kadavath H, Julien O, Assimon VA, Rauch JN, Dunyak BM, Lee J, Tsai FTF, Wilson MR, Zweckstetter M, Dickey CA, Gestwicki JE
• Protein cross-linking capillary electrophoresis at increased throughput for a range of protein-protein interactions.
  The Analyst 2018 Ouimet CM, Dawod M, Grinias J, Assimon VA, Lodge J, Mapp AK, Gestwicki JE, Kennedy RT
• Rational design and screening of peptide-based inhibitors of heat shock factor 1 (HSF1).
  Bioorganic & medicinal chemistry 2018 Ran X, Burchfiel ET, Dong B, Rettko NJ, Dunyak BM, Shao H, Thiele DJ, Gestwicki JE
• Protein-Protein Interactions in the Molecular Chaperone Network.
  Accounts of chemical research 2018 Freilich R, Arhar T, Abrams JL, Gestwicki JE
• SIRT1 Deacetylates Tau and Reduces Pathogenic Tau Spread in a Mouse Model of Tauopathy.
  The Journal of neuroscience : the official journal of the Society for Neuroscience 2018 Min SW, Sohn PD, Li Y, Devidze N, Johnson JR, Krogan NJ, Masliah E, Mok SA, Gestwicki JE, Gan L
• High-throughput screen for inhibitors of protein-protein interactions in a reconstituted heat shock protein 70 (Hsp70) complex.
  The Journal of biological chemistry 2018 Taylor IR, Dunyak BM, Komiyama T, Shao H, Ran X, Assimon VA, Kalyanaraman C, Rauch JN, Jacobson MP, Zuiderweg ERP, Gestwicki JE
• Therapeutic Strategies for Restoring Tau Homeostasis.
  Cold Spring Harbor perspectives in medicine 2018 Young ZT, Mok SA, Gestwicki JE
• X-linked inhibitor of apoptosis protein (XIAP) is a client of heat shock protein 70 (Hsp70) and a biomarker of its inhibition.
  The Journal of biological chemistry 2017 Cesa LC, Shao H, Srinivasan SR, Tse E, Jain C, Zuiderweg ERP, Southworth DR, Mapp AK, Gestwicki JE
• Heat Shock Protein 70 (Hsp70) Suppresses RIP1-Dependent Apoptotic and Necroptotic Cascades.
  Molecular cancer research : MCR 2017 Srinivasan SR, Cesa LC, Li X, Julien O, Zhuang M, Shao H, Chung J, Maillard I, Wells JA, Duckett CS, Gestwicki JE
• Interactions between Microtubule-Associated Protein Tau (MAPT) and Small Molecules.
  Cold Spring Harbor perspectives in medicine 2017 Rauch JN, Olson SH, Gestwicki JE
• From Fuzzy to Function: The New Frontier of Protein-Protein Interactions.
  Accounts of chemical research 2017 Pricer R, Gestwicki JE, Mapp AK
• The remarkable multivalency of the Hsp70 chaperones.
  Cell stress & chaperones 2017 Zuiderweg ER, Hightower LE, Gestwicki JE
• BAG3 Is a Modular, Scaffolding Protein that physically Links Heat Shock Protein 70 (Hsp70) to the Small Heat Shock Proteins.
  Journal of molecular biology 2016 Rauch JN, Tse E, Freilich R, Mok SA, Makley LN, Southworth DR, Gestwicki JE
• Unbiased screen identifies aripiprazole as a modulator of abundance of the polyglutamine disease protein, ataxin-3.
  Brain : a journal of neurology 2016 Costa MDC, Ashraf NS, Fischer S, Yang Y, Schapka E, Joshi G, McQuade TJ, Dharia RM, Dulchavsky M, Ouyang M, Cook D, Sun D, Larsen MJ, Gestwicki JE, Todi SV, Ivanova MI, Paulson HL
• Backbone and methyl resonance assignments of the 42 kDa human Hsc70 nucleotide binding domain in the ADP state.
  Biomolecular NMR assignments 2016 Zuiderweg ER, Gestwicki JE
• Anticancer Effects of Targeting Hsp70 in Tumor Stromal Cells.
  Cancer research 2016 Gabai VL, Yaglom JA, Wang Y, Meng L, Shao H, Kim G, Colvin T, Gestwicki J, Sherman MY
• Stabilizing the Hsp70-Tau Complex Promotes Turnover in Models of Tauopathy.
  Cell chemical biology 2016 Young ZT, Rauch JN, Assimon VA, Jinwal UK, Ahn M, Li X, Dunyak BM, Ahmad A, Carlson GA, Srinivasan SR, Zuiderweg ER, Dickey CA, Gestwicki JE
• Non-canonical Interactions between Heat Shock Cognate Protein 70 (Hsc70) and Bcl2-associated Anthanogene (BAG) Co-Chaperones Are Important for Client Release.
  The Journal of biological chemistry 2016 Rauch JN, Zuiderweg ER, Gestwicki JE
• Protein Cross-Linking Capillary Electrophoresis for Protein-Protein Interaction Analysis.
  Analytical chemistry 2016 Ouimet CM, Shao H, Rauch JN, Dawod M, Nordhues B, Dickey CA, Gestwicki JE, Kennedy RT
• Peptidyl-Proline Isomerases (PPIases): Targets for Natural Products and Natural Product-Inspired Compounds.
  Journal of medicinal chemistry 2016 Dunyak BM, Gestwicki JE
• Combined chemical-genetic approach identifies cytosolic HSP70 dependence in rhabdomyosarcoma.
  Proceedings of the National Academy of Sciences of the United States of America 2016 Sabnis AJ, Guerriero CJ, Olivas V, Sayana A, Shue J, Flanagan J, Asthana S, Paton AW, Paton JC, Gestwicki JE, Walter P, Weissman JS, Wipf P, Brodsky JL, Bivona TG
• Structural and Biological Interaction of hsc-70 Protein with Phosphatidylserine in Endosomal Microautophagy.
  The Journal of biological chemistry 2016 Morozova K, Clement CC, Kaushik S, Stiller B, Arias E, Ahmad A, Rauch JN, Chatterjee V, Melis C, Scharf B, Gestwicki JE, Cuervo AM, Zuiderweg ER, Santambrogio L
• Inhibition of Both Hsp70 Activity and Tau Aggregation in Vitro Best Predicts Tau Lowering Activity of Small Molecules.
  ACS chemical biology 2016 Martin MD, Baker JD, Suntharalingam A, Nordhues BA, Shelton LB, Zheng D, Sabbagh JJ, Haystead TA, Gestwicki JE, Dickey CA
• Apratoxin Kills Cells by Direct Blockade of the Sec61 Protein Translocation Channel.
  Cell chemical biology 2016 Paatero AO, Kellosalo J, Dunyak BM, Almaliti J, Gestwicki JE, Gerwick WH, Taunton J, Paavilainen VO
• Allosteric heat shock protein 70 inhibitors block hepatitis C virus assembly.
  International journal of antimicrobial agents 2016 Khachatoorian R, Riahi R, Ganapathy E, Shao H, Wheatley NM, Sundberg C, Jung CL, Ruchala P, Dasgupta A, Arumugaswami V, Gestwicki JE, French SW
• Guidelines for the use and interpretation of assays for monitoring autophagy (3rd edition).
  Autophagy 2016 Klionsky DJ, Abdelmohsen K, Abe A, Abedin MJ, Abeliovich H, Acevedo Arozena A, Adachi H, Adams CM, Adams PD, Adeli K, Adhihetty PJ, Adler SG, Agam G, Agarwal R, Aghi MK, Agnello M, Agostinis P, …
• Targeting Allosteric Control Mechanisms in Heat Shock Protein 70 (Hsp70).
  Current topics in medicinal chemistry 2016 Li X, Shao H, Taylor IR, Gestwicki JE
• Specific Binding of Tetratricopeptide Repeat Proteins to Heat Shock Protein 70 (Hsp70) and Heat Shock Protein 90 (Hsp90) Is Regulated by Affinity and Phosphorylation.
  Biochemistry 2015 Assimon VA, Southworth DR, Gestwicki JE
• Defining Hsp70 Subnetworks in Dengue Virus Replication Reveals Key Vulnerability in Flavivirus Infection.
  Cell 2015 Taguwa S, Maringer K, Li X, Bernal-Rubio D, Rauch JN, Gestwicki JE, Andino R, Fernandez-Sesma A, Frydman J
• Pharmacological chaperone for α-crystallin partially restores transparency in cataract models.
  Science (New York, N.Y.) 2015 Makley LN, McMenimen KA, DeVree BT, Goldman JW, McGlasson BN, Rajagopal P, Dunyak BM, McQuade TJ, Thompson AD, Sunahara R, Klevit RE, Andley UP, Gestwicki JE
• Critical role of acetylation in tau-mediated neurodegeneration and cognitive deficits.
  Nature medicine 2015 Min SW, Chen X, Tracy TE, Li Y, Zhou Y, Wang C, Shirakawa K, Minami SS, Defensor E, Mok SA, Sohn PD, Schilling B, Cong X, Ellerby L, Gibson BW, Johnson J, Krogan N, Shamloo M, Gestwicki J, Masliah E, …
• Selective Targeting of Cells via Bispecific Molecules That Exploit Coexpression of Two Intracellular Proteins.
  ACS chemical biology 2015 Dunyak BM, Nakamura RL, Frankel AD, Gestwicki JE
• Direct and Propagated Effects of Small Molecules on Protein-Protein Interaction Networks.
  Frontiers in bioengineering and biotechnology 2015 Cesa LC, Mapp AK, Gestwicki JE
• Deconvolution method for specific and nonspecific binding of ligand to multiprotein complex by native mass spectrometry.
  Analytical chemistry 2015 Guan S, Trnka MJ, Bushnell DA, Robinson PJ, Gestwicki JE, Burlingame AL
• The active Hsc70/tau complex can be exploited to enhance tau turnover without damaging microtubule dynamics.
  Human molecular genetics 2015 Fontaine SN, Martin MD, Akoury E, Assimon VA, Borysov S, Nordhues BA, Sabbagh JJ, Cockman M, Gestwicki JE, Zweckstetter M, Dickey CA
• Isoform-selective Genetic Inhibition of Constitutive Cytosolic Hsp70 Activity Promotes Client Tau Degradation Using an Altered Co-chaperone Complement.
  The Journal of biological chemistry 2015 Fontaine SN, Rauch JN, Nordhues BA, Assimon VA, Stothert AR, Jinwal UK, Sabbagh JJ, Chang L, Stevens SM, Zuiderweg ER, Gestwicki JE, Dickey CA
• Concise Synthesis of Spergualin-Inspired Molecules With Broad-Spectrum Antibiotic Activity.
  MedChemComm 2015 Assimon VA, Shao H, Garneau-Tsodikova S, Gestwicki JE
• Synthesis, stereochemical analysis, and derivatization of myricanol provide new probes that promote autophagic tau clearance.
  ACS chemical biology 2015 Martin MD, Calcul L, Smith C, Jinwal UK, Fontaine SN, Darling A, Seeley K, Wojtas L, Narayan M, Gestwicki JE, Smith GR, Reitz AB, Baker BJ, Dickey CA
• Validation of the Hsp70-Bag3 protein-protein interaction as a potential therapeutic target in cancer.
  Molecular cancer therapeutics 2015 Li X, Colvin T, Rauch JN, Acosta-Alvear D, Kampmann M, Dunyak B, Hann B, Aftab BT, Murnane M, Cho M, Walter P, Weissman JS, Sherman MY, Gestwicki JE
• Correction to enantioselective organocatalytic hantzsch synthesis of polyhydroquinolines.
  Organic letters 2014 Evans CG, Gestwicki JE
• Targeting Hsp90/Hsp70-based protein quality control for treatment of adult onset neurodegenerative diseases.
  Annual review of pharmacology and toxicology 2014 Pratt WB, Gestwicki JE, Osawa Y, Lieberman AP
• Genomic heat shock element sequences drive cooperative human heat shock factor 1 DNA binding and selectivity.
  The Journal of biological chemistry 2014 Jaeger AM, Makley LN, Gestwicki JE, Thiele DJ
• Epitope analysis following active immunization with tau proteins reveals immunogens implicated in tau pathogenesis.
  Journal of neuroinflammation 2014 Selenica ML, Davtyan H, Housley SB, Blair LJ, Gillies A, Nordhues BA, Zhang B, Liu J, Gestwicki JE, Lee DC, Gordon MN, Morgan D, Dickey CA
• Rehabilitating mutant GCase.
  Chemistry & biology 2014 Rauch JN, Gestwicki JE
• An allosteric modulator of HIV-1 protease shows equipotent inhibition of wild-type and drug-resistant proteases.
  Journal of medicinal chemistry 2014 Ung PM, Dunbar JB, Gestwicki JE, Carlson HA
• Hsp70-Bag3 interactions regulate cancer-related signaling networks.
  Cancer research 2014 Colvin TA, Gabai VL, Gong J, Calderwood SK, Li H, Gummuluru S, Matchuk ON, Smirnova SG, Orlova NV, Zamulaeva IA, Garcia-Marcos M, Li X, Young ZT, Rauch JN, Gestwicki JE, Takayama S, Sherman MY
• A model in which heat shock protein 90 targets protein-folding clefts: rationale for a new approach to neuroprotective treatment of protein folding diseases.
  Experimental biology and medicine (Maywood, N.J.) 2014 Pratt WB, Morishima Y, Gestwicki JE, Lieberman AP, Osawa Y
• High-throughput screen of natural product extracts in a yeast model of polyglutamine proteotoxicity.
  Chemical biology & drug design 2014 Walter GM, Raveh A, Mok SA, McQuade TJ, Arevang CJ, Schultz PJ, Smith MC, Asare S, Cruz PG, Wisen S, Matainaho T, Sherman DH, Gestwicki JE
• The molecular chaperone Hsp70 activates protein phosphatase 5 (PP5) by binding the tetratricopeptide repeat (TPR) domain.
  The Journal of biological chemistry 2013 Connarn JN, Assimon VA, Reed RA, Tse E, Southworth DR, Zuiderweg ER, Gestwicki JE, Sun D
• Binding of human nucleotide exchange factors to heat shock protein 70 (Hsp70) generates functionally distinct complexes in vitro.
  The Journal of biological chemistry 2013 Rauch JN, Gestwicki JE
• Identification of key hinge residues important for nucleotide-dependent allostery in E. coli Hsp70/DnaK.
  PLoS computational biology 2013 Ung PM, Thompson AD, Chang L, Gestwicki JE, Carlson HA
• Analogs of the Allosteric Heat Shock Protein 70 (Hsp70) Inhibitor, MKT-077, as Anti-Cancer Agents.
  ACS medicinal chemistry letters 2013 Li X, Srinivasan SR, Connarn J, Ahmad A, Young ZT, Kabza AM, Zuiderweg ER, Sun D, Gestwicki JE
• Development of a capillary electrophoresis platform for identifying inhibitors of protein-protein interactions.
  Analytical chemistry 2013 Rauch JN, Nie J, Buchholz TJ, Gestwicki JE, Kennedy RT
• The E3 ubiquitin ligase CHIP and the molecular chaperone Hsc70 form a dynamic, tethered complex.
  Biochemistry 2013 Smith MC, Scaglione KM, Assimon VA, Patury S, Thompson AD, Dickey CA, Southworth DR, Paulson HL, Gestwicki JE, Zuiderweg ER
• Inhibitors of difficult protein-protein interactions identified by high-throughput screening of multiprotein complexes.
  ACS chemical biology 2013 Cesa LC, Patury S, Komiyama T, Ahmad A, Zuiderweg ERP, Gestwicki JE
• CSAR data set release 2012: ligands, affinities, complexes, and docking decoys.
  Journal of chemical information and modeling 2013 Dunbar JB, Smith RD, Damm-Ganamet KL, Ahmed A, Esposito EX, Delproposto J, Chinnaswamy K, Kang YN, Kubish G, Gestwicki JE, Stuckey JA, Carlson HA
• Allosteric heat shock protein 70 inhibitors rapidly rescue synaptic plasticity deficits by reducing aberrant tau.
  Biological psychiatry 2013 Abisambra J, Jinwal UK, Miyata Y, Rogers J, Blair L, Li X, Seguin SP, Wang L, Jin Y, Bacon J, Brady S, Cockman M, Guidi C, Zhang J, Koren J, Young ZT, Atkins CA, Zhang B, Lawson LY, Weeber EJ, Brodsky…
• Synthesis and initial evaluation of YM-08, a blood-brain barrier permeable derivative of the heat shock protein 70 (Hsp70) inhibitor MKT-077, which reduces tau levels.
  ACS chemical neuroscience 2013 Miyata Y, Li X, Lee HF, Jinwal UK, Srinivasan SR, Seguin SP, Young ZT, Brodsky JL, Dickey CA, Sun D, Gestwicki JE
• Allostery in the Hsp70 chaperone proteins.
  Topics in current chemistry 2013 Zuiderweg ER, Bertelsen EB, Rousaki A, Mayer MP, Gestwicki JE, Ahmad A
• Expanding the number of 'druggable' targets: non-enzymes and protein-protein interactions.
  Chemical biology & drug design 2013 Makley LN, Gestwicki JE
• Hsp70 protein complexes as drug targets.
  Current pharmaceutical design 2013 Assimon VA, Gillies AT, Rauch JN, Gestwicki JE
• Imbalance of Hsp70 family variants fosters tau accumulation.
  FASEB journal : official publication of the Federation of American Societies for Experimental Biology 2012 Jinwal UK, Akoury E, Abisambra JF, O'Leary JC, Thompson AD, Blair LJ, Jin Y, Bacon J, Nordhues BA, Cockman M, Zhang J, Li P, Zhang B, Borysov S, Uversky VN, Biernat J, Mandelkow E, Gestwicki JE, …
• Activation of Hsp70 reduces neurotoxicity by promoting polyglutamine protein degradation.
  Nature chemical biology 2012 Wang AM, Miyata Y, Klinedinst S, Peng HM, Chua JP, Komiyama T, Li X, Morishima Y, Merry DE, Pratt WB, Osawa Y, Collins CA, Gestwicki JE, Lieberman AP
• Cysteine reactivity distinguishes redox sensing by the heat-inducible and constitutive forms of heat shock protein 70.
  Chemistry & biology 2012 Miyata Y, Rauch JN, Jinwal UK, Thompson AD, Srinivasan S, Dickey CA, Gestwicki JE
• Synthetic lethal interactions in yeast reveal functional roles of J protein co-chaperones.
  Molecular bioSystems 2012 Gillies AT, Taylor R, Gestwicki JE
• Inducible renitence limits Listeria monocytogenes escape from vacuoles in macrophages.
  Journal of immunology (Baltimore, Md. : 1950) 2012 Davis MJ, Gregorka B, Gestwicki JE, Swanson JA
• A screen for modulators of large T antigen's ATPase activity uncovers novel inhibitors of Simian Virus 40 and BK virus replication.
  Antiviral research 2012 Seguin SP, Ireland AW, Gupta T, Wright CM, Miyata Y, Wipf P, Pipas JM, Gestwicki JE, Brodsky JL
• Features of protein-protein interactions that translate into potent inhibitors: topology, surface area and affinity.
  Expert reviews in molecular medicine 2012 Smith MC, Gestwicki JE
• Analysis of the tau-associated proteome reveals that exchange of Hsp70 for Hsp90 is involved in tau degradation.
  ACS chemical biology 2012 Thompson AD, Scaglione KM, Prensner J, Gillies AT, Chinnaiyan A, Paulson HL, Jinwal UK, Dickey CA, Gestwicki JE
• Fine-tuning multiprotein complexes using small molecules.
  ACS chemical biology 2012 Thompson AD, Dugan A, Gestwicki JE, Mapp AK
• Molecular chaperones DnaK and DnaJ share predicted binding sites on most proteins in the E. coli proteome.
  Molecular bioSystems 2012 Srinivasan SR, Gillies AT, Chang L, Thompson AD, Gestwicki JE
• Pharmacological tuning of heat shock protein 70 modulates polyglutamine toxicity and aggregation.
  ACS chemical biology 2012 Chafekar SM, Wisén S, Thompson AD, Echeverria A, Walter GM, Evans CG, Makley LN, Gestwicki JE, Duennwald ML
• The C-terminal repeating units of CsgB direct bacterial functional amyloid nucleation.
  Journal of molecular biology 2012 Hammer ND, McGuffie BA, Zhou Y, Badtke MP, Reinke AA, Brännström K, Gestwicki JE, Olofsson A, Almqvist F, Chapman MR
• Cdc37/Hsp90 protein complex disruption triggers an autophagic clearance cascade for TDP-43 protein.
  The Journal of biological chemistry 2012 Jinwal UK, Abisambra JF, Zhang J, Dharia S, O'Leary JC, Patel T, Braswell K, Jani T, Gestwicki JE, Dickey CA
• The three cornerstones of chemical biology: innovative probes, new discoveries, and enabling tools.
  ACS chemical biology 2012 Thompson AD, Makley LN, McMenimen K, Gestwicki JE
• Rhodacyanine derivative selectively targets cancer cells and overcomes tamoxifen resistance.
  PloS one 2012 Koren J, Miyata Y, Kiray J, O'Leary JC, Nguyen L, Guo J, Blair LJ, Li X, Li X, Jinwal UK, Cheng JQ, Gestwicki JE, Dickey CA
• Guidelines for the use and interpretation of assays for monitoring autophagy.
  Autophagy 2012 Klionsky DJ, Abdalla FC, Abeliovich H, Abraham RT, Acevedo-Arozena A, Adeli K, Agholme L, Agnello M, Agostinis P, Aguirre-Ghiso JA, Ahn HJ, Ait-Mohamed O, Ait-Si-Ali S, Akematsu T, Akira S, Al-Younes …
• Methylthioninium chloride (methylene blue) induces autophagy and attenuates tauopathy in vitro and in vivo.
  Autophagy 2012 Congdon EE, Wu JW, Myeku N, Figueroa YH, Herman M, Marinec PS, Gestwicki JE, Dickey CA, Yu WH, Duff KE
• Protein quality control in neurodegenerative disease.
  Progress in molecular biology and translational science 2012 Gestwicki JE, Garza D
• Visualization and functional analysis of the oligomeric states of Escherichia coli heat shock protein 70 (Hsp70/DnaK).
  Cell stress & chaperones 2011 Thompson AD, Bernard SM, Skiniotis G, Gestwicki JE
• Ordered assembly of heat shock proteins, Hsp26, Hsp70, Hsp90, and Hsp104, on expanded polyglutamine fragments revealed by chemical probes.
  The Journal of biological chemistry 2011 Walter GM, Smith MC, Wisén S, Basrur V, Elenitoba-Johnson KS, Duennwald ML, Kumar A, Gestwicki JE
• Molecular chaperones and regulation of tau quality control: strategies for drug discovery in tauopathies.
  Future medicinal chemistry 2011 Miyata Y, Koren J, Kiray J, Dickey CA, Gestwicki JE
• Ube2w and ataxin-3 coordinately regulate the ubiquitin ligase CHIP.
  Molecular cell 2011 Scaglione KM, Zavodszky E, Todi SV, Patury S, Xu P, Rodríguez-Lebrón E, Fischer S, Konen J, Djarmati A, Peng J, Gestwicki JE, Paulson HL
• Heme-dependent activation of neuronal nitric oxide synthase by cytosol is due to an Hsp70-dependent, thioredoxin-mediated thiol-disulfide interchange in the heme/substrate binding cleft.
  Biochemistry 2011 Morishima Y, Lau M, Peng HM, Miyata Y, Gestwicki JE, Pratt WB, Osawa Y
• Allosteric drugs: the interaction of antitumor compound MKT-077 with human Hsp70 chaperones.
  Journal of molecular biology 2011 Rousaki A, Miyata Y, Jinwal UK, Dickey CA, Gestwicki JE, Zuiderweg ER
• Insight into amyloid structure using chemical probes.
  Chemical biology & drug design 2011 Reinke AA, Gestwicki JE
• Improved synthesis of 15-deoxyspergualin analogs using the Ugi multi-component reaction.
  Bioorganic & medicinal chemistry letters 2011 Evans CG, Smith MC, Carolan JP, Gestwicki JE
• Chemical screens against a reconstituted multiprotein complex: myricetin blocks DnaJ regulation of DnaK through an allosteric mechanism.
  Chemistry & biology 2011 Chang L, Miyata Y, Ung PM, Bertelsen EB, McQuade TJ, Carlson HA, Zuiderweg ER, Gestwicki JE
• Chemical probes that selectively recognize the earliest Aβ oligomers in complex mixtures.
  Journal of the American Chemical Society 2010 Reinke AA, Ung PM, Quintero JJ, Carlson HA, Gestwicki JE
• Identification of dihydropyridines that reduce cellular tau levels.
  Chemical communications (Cambridge, England) 2010 Evans CG, Jinwal UK, Makley LN, Dickey CA, Gestwicki JE
• Bicinchoninic acid (BCA) assay in low volume.
  Analytical biochemistry 2010 Bainor A, Chang L, McQuade TJ, Webb B, Gestwicki JE
• Phenothiazine-mediated rescue of cognition in tau transgenic mice requires neuroprotection and reduced soluble tau burden.
  Molecular neurodegeneration 2010 O'Leary JC, Li Q, Marinec P, Blair LJ, Congdon EE, Johnson AG, Jinwal UK, Koren J, Jones JR, Kraft C, Peters M, Abisambra JF, Duff KE, Weeber EJ, Gestwicki JE, Dickey CA
• Conditionally controlling nuclear trafficking in yeast by chemical-induced protein dimerization.
  Nature protocols 2010 Xu T, Johnson CA, Gestwicki JE, Kumar A
• High-throughput screen for Escherichia coli heat shock protein 70 (Hsp70/DnaK): ATPase assay in low volume by exploiting energy transfer.
  Journal of biomolecular screening 2010 Miyata Y, Chang L, Bainor A, McQuade TJ, Walczak CP, Zhang Y, Larsen MJ, Kirchhoff P, Gestwicki JE
• Quantifying prefibrillar amyloids in vitro by using a "thioflavin-like" spectroscopic method.
  Chembiochem : a European journal of chemical biology 2010 Reinke AA, Abulwerdi GA, Gestwicki JE
• Heat shock protein 70 (hsp70) as an emerging drug target.
  Journal of medicinal chemistry 2010 Evans CG, Chang L, Gestwicki JE
• Binding of a small molecule at a protein-protein interface regulates the chaperone activity of hsp70-hsp40.
  ACS chemical biology 2010 Wisén S, Bertelsen EB, Thompson AD, Patury S, Ung P, Chang L, Evans CG, Walter GM, Wipf P, Carlson HA, Brodsky JL, Zuiderweg ER, Gestwicki JE
• Mutagenesis reveals the complex relationships between ATPase rate and the chaperone activities of Escherichia coli heat shock protein 70 (Hsp70/DnaK).
  The Journal of biological chemistry 2010 Chang L, Thompson AD, Ung P, Carlson HA, Gestwicki JE
• Inhibition of hsp70 by methylene blue affects signaling protein function and ubiquitination and modulates polyglutamine protein degradation.
  The Journal of biological chemistry 2010 Wang AM, Morishima Y, Clapp KM, Peng HM, Pratt WB, Gestwicki JE, Osawa Y, Lieberman AP
• Hsc70 rapidly engages tau after microtubule destabilization.
  The Journal of biological chemistry 2010 Jinwal UK, O'Leary JC, Borysov SI, Jones JR, Li Q, Koren J, Abisambra JF, Vestal GD, Lawson LY, Johnson AG, Blair LJ, Jin Y, Miyata Y, Gestwicki JE, Dickey CA
• Special series: Molecular chaperones in protein folding and disease.
  Biopolymers 2010 Gestwicki JE
• Facilitating Akt clearance via manipulation of Hsp70 activity and levels.
  The Journal of biological chemistry 2009 Koren J, Jinwal UK, Jin Y, O'Leary J, Jones JR, Johnson AG, Blair LJ, Abisambra JF, Chang L, Miyata Y, Cheng AM, Guo J, Cheng JQ, Gestwicki JE, Dickey CA
• Chemical manipulation of hsp70 ATPase activity regulates tau stability.
  The Journal of neuroscience : the official journal of the Society for Neuroscience 2009 Jinwal UK, Miyata Y, Koren J, Jones JR, Trotter JH, Chang L, O'Leary J, Morgan D, Lee DC, Shults CL, Rousaki A, Weeber EJ, Zuiderweg ER, Gestwicki JE, Dickey CA
• A chemical screening approach reveals that indole fluorescence is quenched by pre-fibrillar but not fibrillar amyloid-beta.
  Bioorganic & medicinal chemistry letters 2009 Reinke AA, Seh HY, Gestwicki JE
• Synthesis of orthogonally reactive FK506 derivatives via olefin cross metathesis.
  Bioorganic & medicinal chemistry 2009 Marinec PS, Evans CG, Gibbons GS, Tarnowski MA, Overbeek DL, Gestwicki JE
• Enantioselective organocatalytic Hantzsch synthesis of polyhydroquinolines.
  Organic letters 2009 Evans CG, Gestwicki JE
• Solution conformation of wild-type E. coli Hsp70 (DnaK) chaperone complexed with ADP and substrate.
  Proceedings of the National Academy of Sciences of the United States of America 2009 Bertelsen EB, Chang L, Gestwicki JE, Zuiderweg ER
• Clarifying allosteric control of flap conformations in the 1TW7 crystal structure of HIV-1 protease.
  Proteins 2009 Lexa KW, Damm KL, Quintero JJ, Gestwicki JE, Carlson HA
• FK506-binding protein (FKBP) partitions a modified HIV protease inhibitor into blood cells and prolongs its lifetime in vivo.
  Proceedings of the National Academy of Sciences of the United States of America 2009 Marinec PS, Chen L, Barr KJ, Mutz MW, Crabtree GR, Gestwicki JE
• Conditional nuclear import and export of yeast proteins using a chemical inducer of dimerization.
  Cell biochemistry and biophysics 2009 Patury S, Geda P, Dobry CJ, Kumar A, Gestwicki JE
• Pharmacological targeting of the Hsp70 chaperone.
  Current topics in medicinal chemistry 2009 Patury S, Miyata Y, Gestwicki JE
• A poke in the eye: inhibiting HIV-1 protease through its flap-recognition pocket.
  Biopolymers 2008 Damm KL, Ung PM, Quintero JJ, Gestwicki JE, Carlson HA
• A small molecule-directed approach to control protein localization and function.
  Yeast (Chichester, England) 2008 Geda P, Patury S, Ma J, Bharucha N, Dobry CJ, Lawson SK, Gestwicki JE, Kumar A
• The interface of chemistry and biology is actually a continuum.
  ACS chemical biology 2008 Gestwicki JE
• Bifunctional molecules evade cytochrome P(450) metabolism by forming protective complexes with FK506-binding protein.
  Molecular bioSystems 2008 Marinec PS, Lancia JK, Gestwicki JE
• Identification of small molecules that modify the protein folding activity of heat shock protein 70.
  Analytical biochemistry 2007 Wisén S, Gestwicki JE
• Chemical modulators of heat shock protein 70 (Hsp70) by sequential, microwave-accelerated reactions on solid phase.
  Bioorganic & medicinal chemistry letters 2007 Wisén S, Androsavich J, Evans CG, Chang L, Gestwicki JE
• Derrubone, an inhibitor of the Hsp90 protein folding machinery.
  Journal of natural products 2007 Hadden MK, Galam L, Gestwicki JE, Matts RL, Blagg BS
• Chemical control over protein-protein interactions: beyond inhibitors.
  Combinatorial chemistry & high throughput screening 2007 Gestwicki JE, Marinec PS
• Structure-activity relationships of amyloid beta-aggregation inhibitors based on curcumin: influence of linker length and flexibility.
  Chemical biology & drug design 2007 Reinke AA, Gestwicki JE
• High-throughput screen for small molecules that modulate the ATPase activity of the molecular chaperone DnaK.
  Analytical biochemistry 2007 Chang L, Bertelsen EB, Wisén S, Larsen EM, Zuiderweg ER, Gestwicki JE
• Rescue of degradation-prone mutants of the FK506-rapamycin binding (FRB) protein with chemical ligands.
  Chembiochem : a European journal of chemical biology 2007 Stankunas K, Bayle JH, Havranek JJ, Wandless TJ, Baker D, Crabtree GR, Gestwicki JE
• Potential therapeutic applications of autophagy.
  Nature reviews. Drug discovery 2007 Rubinsztein DC, Gestwicki JE, Murphy LO, Klionsky DJ
• Heat shock proteins 70 and 90 inhibit early stages of amyloid beta-(1-42) aggregation in vitro.
  The Journal of biological chemistry 2006 Evans CG, Wisén S, Gestwicki JE
• Reclamation of proteins from the cellular scrap heap.
  ACS chemical biology 2006 Gestwicki JE
• Synthetic multivalent ligands as probes of signal transduction.
  Angewandte Chemie (International ed. in English) 2006 Kiessling LL, Gestwicki JE, Strong LE
• Rapamycin analogs with differential binding specificity permit orthogonal control of protein activity.
  Chemistry & biology 2006 Bayle JH, Grimley JS, Stankunas K, Gestwicki JE, Wandless TJ, Crabtree GR
• 'Nature-inspired' drug-protein complexes as inhibitors of Abeta aggregation.
  Biochemical Society transactions 2005 Bose M, Gestwicki JE, Devasthali V, Crabtree GR, Graef IA
• Target identification for a promising anti-lupus drug.
  Chemistry & biology 2005 Gestwicki JE
• Harnessing chaperones to generate small-molecule inhibitors of amyloid beta aggregation.
  Science (New York, N.Y.) 2004 Gestwicki JE, Crabtree GR, Graef IA
• A field of myocardial-endocardial NFAT signaling underlies heart valve morphogenesis.
  Cell 2004 Chang CP, Neilson JR, Bayle JH, Gestwicki JE, Kuo A, Stankunas K, Graef IA, Crabtree GR
• Conditional protein alleles using knockin mice and a chemical inducer of dimerization.
  Molecular cell 2003 Stankunas K, Bayle JH, Gestwicki JE, Lin YM, Wandless TJ, Crabtree GR
• Visualization and characterization of receptor clusters by transmission electron microscopy.
  Methods in enzymology 2003 Gestwicki JE, Cairo CW, Borrok MJ, Kiessling LL
• Influencing receptor-ligand binding mechanisms with multivalent ligand architecture.
  Journal of the American Chemical Society 2002 Gestwicki JE, Cairo CW, Strong LE, Oetjen KA, Kiessling LL
• Conserved amplification of chemotactic responses through chemoreceptor interactions.
  Journal of bacteriology 2002 Lamanna AC, Gestwicki JE, Strong LE, Borchardt SL, Owen RM, Kiessling LL
• Synthesis and applications of end-labeled neoglycopolymers.
  Organic letters 2002 Owen RM, Gestwicki JE, Young T, Kiessling LL
• Selective immobilization of multivalent ligands for surface plasmon resonance and fluorescence microscopy.
  Analytical biochemistry 2002 Gestwicki JE, Cairo CW, Mann DA, Owen RM, Kiessling LL
• Control of multivalent interactions by binding epitope density.
  Journal of the American Chemical Society 2002 Cairo CW, Gestwicki JE, Kanai M, Kiessling LL
• Cell aggregation by scaffolded receptor clusters.
  Chemistry & biology 2002 Gestwicki JE, Strong LE, Cairo CW, Boehm FJ, Kiessling LL
• Inter-receptor communication through arrays of bacterial chemoreceptors.
  Nature 2002 Gestwicki JE, Kiessling LL
• Using receptor conformational change to detect low molecular weight analytes by surface plasmon resonance.
  Analytical chemistry 2001 Gestwicki JE, Hsieh HV, Pitner JB
• Designed potent multivalent chemoattractants for Escherichia coli.
  Bioorganic & medicinal chemistry 2001 Gestwicki JE, Strong LE, Borchardt SL, Cairo CW, Schnoes AM, Kiessling LL
• Visualization of Single Multivalent Receptor-Ligand Complexes by Transmission Electron Microscopy The authors thank Colleen Lavin (UW Madison, Microscopy Resource) and Kim Dickson for experimental support. This work was supported in part by the NIH (GM 55984). J.E.G. acknowledges the NIH Biotechnology Training Grant for support (T32GM08349). L.E.S. was supported by an NIH predoctoral fellowship (GM 18750).
  Angewandte Chemie (International ed. in English) 2000 Gestwicki JE, Strong LE, Kiessling LL
• Synthetic multivalent ligands in the exploration of cell-surface interactions.
  Current opinion in chemical biology 2000 Kiessling LL, Gestwicki JE, Strong LE
• Evolutionary conservation of methyl-accepting chemotaxis protein location in Bacteria and Archaea.
  Journal of bacteriology 2000 Gestwicki JE, Lamanna AC, Harshey RM, McCarter LL, Kiessling LL, Adler J
• A quantitative-trait locus controlling peripheral B-cell deficiency maps to mouse Chromosome 15.
  Immunogenetics 2000 Hoag KA, Clise-Dwyer K, Lim YH, Nashold FE, Gestwicki J, Cancro MP, Hayes CE
• Motility and chemotaxis of filamentous cells of Escherichia coli.
  Journal of bacteriology 2000 Maki N, Gestwicki JE, Lake EM, Kiessling LL, Adler J
• Tuning chemotactic responses with synthetic multivalent ligands.
  Chemistry & biology 2000 Gestwicki JE, Strong LE, Kiessling LL
• Microwave-induced esterification using heterogeneous acid catalyst in a low dielectric constant medium
  The Journal of organic chemistry 2000 Kabza KG, Chapados BR, Gestwicki JE, McGrath JL
• Synthesis of end-labeled multivalent ligands for exploring cell-surface-receptor-ligand interactions.
  Chemistry & biology 2000 Gordon EJ, Gestwicki JE, Strong LE, Kiessling LL