Adam Renslo, PhD
Professor
Pharmaceutical Chemistry
School of Pharmacy

Our group also developed a parallel synthetic methodology to produce a library of disulfide 'fragments', thereby enabling cysteine-disulfide (Tethering) screening at UCSF. Finally, we design, synthesize and validate novel small molecule probes for the study of labile ferrous iron in biology and disease. Most recently, we described the first of a new class of activity-based probes for proximity labelling of proteins in an iron-dependent fashion, thus enabling the first chemoproteomic studies of the labile iron 'interactome'.

• Development of covalent chemogenetic K2P channel activators.
  bioRxiv : the preprint server for biology 2023 Deal PE, Lee H, Mondal A, Lolicato M, de Mendonca PRF, Black H, El-Hilali X, Bryant C, Isacoff EY, Renslo AR, Minor DL
• In vivo bioluminescence imaging of labile iron in xenograft models and liver using FeAL-1, an iron-activatable form of D-luciferin.
  Cell chemical biology 2023 Gonciarz RL, Jiang H, Tram L, Hugelshofer CL, Ekpenyong O, Knemeyer I, Aron AT, Chang CJ, Flygare JA, Collisson EA, Renslo AR
• Imaging-Selected Host Responses in the Context of Infections.
  The Journal of infectious diseases 2023 Foss CA, Renslo AR
• Structure-Based Optimization of Covalent, Small-Molecule Stabilizers of the 14-3-3σ/ERα Protein-Protein Interaction from Nonselective Fragments.
  Journal of the American Chemical Society 2023 Konstantinidou M, Visser EJ, Vandenboorn E, Chen S, Jaishankar P, Overmans M, Dutta S, Neitz RJ, Renslo AR, Ottmann C, Brunsveld L, Arkin MR
• From Tethered to Freestanding Stabilizers of 14-3-3 Protein-Protein Interactions through Fragment Linking.
  Angewandte Chemie (International ed. in English) 2023 Visser EJ, Jaishankar P, Sijbesma E, Pennings MAM, Vandenboorn EMF, Guillory X, Neitz RJ, Morrow J, Dutta S, Renslo AR, Brunsveld L, Arkin MR, Ottmann C
• Large library docking for novel SARS-CoV-2 main protease non-covalent and covalent inhibitors.
  Protein science : a publication of the Protein Society 2023 Fink EA, Bardine C, Gahbauer S, Singh I, Detomasi TC, White K, Gu S, Wan X, Chen J, Ary B, Glenn I, O'Connell J, O'Donnell H, Fajtová P, Lyu J, Vigneron S, Young NJ, Kondratov IS, Alisoltani A, Simons…
• Systematic Study of Heteroarene Stacking Using a Congeneric Set of Molecular Glues for Procaspase-6.
  Journal of medicinal chemistry 2023 Togo T, Tram L, Denton LG, ElHilali-Pollard X, Gu J, Jiang J, Liu C, Zhao Y, Zhao Y, Zheng Y, Zheng Y, Yang J, Fan P, Arkin MR, Härmä H, Sun D, Canan SS, Wheeler SE, Renslo AR
• Engaging a Non-catalytic Cysteine Residue Drives Potent and Selective Inhibition of Caspase-6.
  Journal of the American Chemical Society 2023 Van Horn KS, Wang D, Medina-Cleghorn D, Lee PS, Bryant C, Altobelli C, Jaishankar P, Leung KK, Ng RA, Ambrose AJ, Tang Y, Arkin MR, Renslo AR
• Artefenomel Regioisomer RLA-3107 Is a Promising Lead for the Discovery of Next-Generation Endoperoxide Antimalarials.
  ACS medicinal chemistry letters 2023 Blank BR, Gut J, Rosenthal PJ, Renslo AR
• Selective ablation of primary and paracrine senescent cells by targeting iron dyshomeostasis.
  Cell reports 2023 Admasu TD, Kim K, Rae M, Avelar R, Gonciarz RL, Rebbaa A, Pedro de Magalhães J, Renslo AR, Stolzing A, Sharma A
• Elevated labile iron in castration-resistant prostate cancer is targetable with ferrous iron-activatable antiandrogen therapy.
  European journal of medicinal chemistry 2023 Gonciarz RL, Sakhamuri S, Hooshdaran N, Kumar G, Kim H, Evans MJ, Renslo AR
• 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, …
• 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, …
• Systematic Exploration of Passive Permeability in Tetrapeptides with Hydrogen-Bond-Accepting Amino Acid Side Chains.
  ChemMedChem 2022 Shimizu H, Renslo AR
• Structure-Based Ligand Design Targeting Pseudomonas aeruginosa LpxA in Lipid A Biosynthesis.
  ACS infectious diseases 2022 Sacco MD, Defrees K, Zhang X, Lawless W, Nwanochie E, Balsizer A, Darch SE, Renslo AR, Chen Y
• Inhibiting a dynamic viral protease by targeting a non-catalytic cysteine.
  Cell chemical biology 2022 Hulce KR, Jaishankar P, Lee GM, Bohn MF, Connelly EJ, Wucherer K, Ongpipattanakul C, Volk RF, Chuo SW, Arkin MR, Renslo AR, Craik CS
• Pyrvinium Pamoate and Structural Analogs Are Early Macrofilaricide Leads.
  Pharmaceuticals (Basel, Switzerland) 2022 Gunderson EL, Bryant C, Bulman CA, Fischer C, Luo M, Vogel I, Lim KC, Jawahar S, Tricoche N, Voronin D, Corbo C, Ayiseh RB, Manfo FPT, Mbah GE, Cho-Ngwa F, Beerntsen B, Renslo AR, Lustigman S, …
• Correction: Expanded scope of Griesbaum co-ozonolysis for the preparation of structurally diverse sensors of ferrous iron.
  RSC advances 2021 Chen J, Gonciarz RL, Renslo AR
• Mutation of the conserved Asp-Asp pair impairs the structure, function, and inhibition of CTX-M Class A β-lactamase.
  FEBS letters 2021 Kemp MT, Nichols DA, Zhang X, Defrees K, Na I, Renslo AR, Chen Y
• Expanded scope of Griesbaum co-ozonolysis for the preparation of structurally diverse sensors of ferrous iron.
  RSC advances 2021 Chen J, Gonciarz RL, Renslo AR
• A zebrafish screen reveals Renin-angiotensin system inhibitors as neuroprotective via mitochondrial restoration in dopamine neurons.
  eLife 2021 Kim GJ, Mo H, Liu H, Wu Z, Chen S, Zheng J, Zhao X, Nucum D, Shortland J, Peng L, Elepano M, Tang B, Olson S, Paras N, Li H, Renslo AR, Arkin MR, Huang B, Lu B, Sirota M, Guo S
• Emerging role of ferrous iron in bacterial growth and host-pathogen interaction: New tools for chemical (micro)biology and antibacterial therapy.
  Current opinion in chemical biology 2021 Gonciarz RL, Renslo AR
• Ferrous Iron-Dependent Pharmacology.
  Trends in pharmacological sciences 2020 Gonciarz RL, Collisson EA, Renslo AR
• Druggable Hot Spots in the Schistosomiasis Cathepsin B1 Target Identified by Functional and Binding Mode Analysis of Potent Vinyl Sulfone Inhibitors.
  ACS infectious diseases 2020 Jílková A, Rubešová P, Fanfrlík J, Fajtová P, Rezácová P, Brynda J, Lepšík M, Mertlíková-Kaiserová H, Emal CD, Renslo AR, Roush WR, Horn M, Caffrey CR, Mareš M
• Antimalarial Trioxolanes with Superior Drug-Like Properties and In Vivo Efficacy.
  ACS infectious diseases 2020 Blank BR, Gonciarz RL, Talukder P, Gut J, Legac J, Rosenthal PJ, Renslo AR
• Oscillatory cAMP signaling rapidly alters H3K4 methylation.
  Life science alliance 2019 Huff TC, Camarena V, Sant DW, Wilkes Z, Van Booven D, Aron AT, Muir RK, Renslo AR, Chang CJ, Monje PV, Wang G
• Activation of Caspase-6 Is Promoted by a Mutant Huntingtin Fragment and Blocked by an Allosteric Inhibitor Compound.
  Cell chemical biology 2019 Ehrnhoefer DE, Skotte NH, Reinshagen J, Qiu X, Windshügel B, Jaishankar P, Ladha S, Petina O, Khankischpur M, Nguyen YTN, Caron NS, Razeto A, Meyer Zu Rheda M, Deng Y, Huynh KT, Wittig I, Gribbon P, …
• An Empirical Study of Amide-Heteroarene π-Stacking Interactions Using Reversible Inhibitors of a Bacterial Serine Hydrolase.
  Organic chemistry frontiers : an international journal of organic chemistry 2019 DeFrees K, Kemp MT, ElHilali-Pollard X, Zhang X, Mohamed A, Chen Y, Renslo AR
• Active-Site Druggability of Carbapenemases and Broad-Spectrum Inhibitor Discovery.
  ACS infectious diseases 2019 Torelli NJ, Akhtar A, DeFrees K, Jaishankar P, Pemberton OA, Zhang X, Johnson C, Renslo AR, Chen Y
• Measuring Dynamic Changes in the Labile Iron Pool in Vivo with a Reactivity-Based Probe for Positron Emission Tomography.
  ACS central science 2019 Muir RK, Zhao N, Wei J, Wang YH, Moroz A, Huang Y, Chen YC, Sriram R, Kurhanewicz J, Ruggero D, Renslo AR, Evans MJ
• Cilia-Associated Oxysterols Activate Smoothened.
  Molecular cell 2018 Raleigh DR, Sever N, Choksi PK, Sigg MA, Hines KM, Thompson BM, Elnatan D, Jaishankar P, Bisignano P, Garcia-Gonzalo FR, Krup AL, Eberl M, Byrne EFX, Siebold C, Wong SY, Renslo AR, Grabe M, McDonald …
• Antibacterial Spectrum of a Tetrazole-Based Reversible Inhibitor of Serine β-Lactamases.
  Antimicrobial agents and chemotherapy 2018 Pemberton OA, Zhang X, Nichols DA, DeFrees K, Jaishankar P, Bonnet R, Adams J, Shaw LN, Renslo AR, Chen Y
• Toward a Ferrous Iron-Cleavable Linker for Antibody-Drug Conjugates.
  Molecular pharmaceutics 2018 Spangler B, Kline T, Hanson J, Li X, Zhou S, Wells JA, Sato AK, Renslo AR
• cAMP signaling regulates DNA hydroxymethylation by augmenting the intracellular labile ferrous iron pool.
  eLife 2017 Camarena V, Sant DW, Huff TC, Mustafi S, Muir RK, Aron AT, Chang CJ, Renslo AR, Monje PV, Wang G
• In vivo bioluminescence imaging of labile iron accumulation in a murine model of Acinetobacter baumannii infection.
  Proceedings of the National Academy of Sciences of the United States of America 2017 Aron AT, Heffern MC, Lonergan ZR, Vander Wal MN, Blank BR, Spangler B, Zhang Y, Park HM, Stahl A, Renslo AR, Skaar EP, Chang CJ
• USP7 small-molecule inhibitors interfere with ubiquitin binding.
  Nature 2017 Kategaya L, Di Lello P, Rougé L, Pastor R, Clark KR, Drummond J, Kleinheinz T, Lin E, Upton JP, Prakash S, Heideker J, McCleland M, Ritorto MS, Alessi DR, Trost M, Bainbridge TW, Kwok MCM, Ma TP, …
• Ras Binder Induces a Modified Switch-II Pocket in GTP and GDP States.
  Cell chemical biology 2017 Gentile DR, Rathinaswamy MK, Jenkins ML, Moss SM, Siempelkamp BD, Renslo AR, Burke JE, Shokat KM
• A Liquid Chromatography/Mass Spectrometry Method for Screening Disulfide Tethering Fragments.
  SLAS discovery : advancing life sciences R & D 2017 Hallenbeck KK, Davies JL, Merron C, Ogden P, Sijbesma E, Ottmann C, Renslo AR, Wilson C, Arkin MR
• Allosteric Inhibitors, Crystallography, and Comparative Analysis Reveal Network of Coordinated Movement across Human Herpesvirus Proteases.
  Journal of the American Chemical Society 2017 Acker TM, Gable JE, Bohn MF, Jaishankar P, Thompson MC, Fraser JS, Renslo AR, Craik CS
• Enantioselective Synthesis and in Vivo Evaluation of Regioisomeric Analogues of the Antimalarial Arterolane.
  Journal of medicinal chemistry 2017 Blank BR, Gut J, Rosenthal PJ, Renslo AR
• Identification and Optimization of Thienopyridine Carboxamides as Inhibitors of HIV Regulatory Complexes.
  Antimicrobial agents and chemotherapy 2017 Nakamura RL, Burlingame MA, Yang S, Crosby DC, Talbot DJ, Chui K, Frankel AD, Renslo AR
• Targeting Non-Catalytic Cysteine Residues Through Structure-Guided Drug Discovery.
  Current topics in medicinal chemistry 2017 Hallenbeck KK, Turner DM, Renslo AR, Arkin MR
• A Novel Tumor-Activated Prodrug Strategy Targeting Ferrous Iron Is Effective in Multiple Preclinical Cancer Models.
  Journal of medicinal chemistry 2016 Spangler B, Fontaine SD, Shi Y, Sambucetti L, Mattis AN, Hann B, Wells JA, Renslo AR
• Ceapins are a new class of unfolded protein response inhibitors, selectively targeting the ATF6α branch.
  eLife 2016 Gallagher CM, Garri C, Cain EL, Ang KK, Wilson CG, Chen S, Hearn BR, Jaishankar P, Aranda-Diaz A, Arkin MR, Renslo AR, Walter P
• Structure-Activity Studies of Bis-O-Arylglycolamides: Inhibitors of the Integrated Stress Response.
  ChemMedChem 2016 Hearn BR, Jaishankar P, Sidrauski C, Tsai JC, Vedantham P, Fontaine SD, Walter P, Renslo AR
• Trioxolane-Mediated Delivery of Mefloquine Limits Brain Exposure in a Mouse Model of Malaria.
  ACS medicinal chemistry letters 2015 Lauterwasser EM, Fontaine SD, Li H, Gut J, Katneni K, Charman SA, Rosenthal PJ, Bogyo M, Renslo AR
• High-throughput matrix screening identifies synergistic and antagonistic antimalarial drug combinations.
  Scientific reports 2015 Mott BT, Eastman RT, Guha R, Sherlach KS, Siriwardana A, Shinn P, McKnight C, Michael S, Lacerda-Queiroz N, Patel PR, Khine P, Sun H, Kasbekar M, Aghdam N, Fontaine SD, Liu D, Mierzwa T, Mathews-…
• Antileishmanial Activity of Disulfiram and Thiuram Disulfide Analogs in an Ex Vivo Model System Is Selectively Enhanced by the Addition of Divalent Metal Ions.
  Antimicrobial agents and chemotherapy 2015 Peniche AG, Renslo AR, Melby PC, Travi BL
• Different 2-Aminothiazole Therapeutics Produce Distinct Patterns of Scrapie Prion Neuropathology in Mouse Brains.
  The Journal of pharmacology and experimental therapeutics 2015 Giles K, Berry DB, Condello C, Hawley RC, Gallardo-Godoy A, Bryant C, Oehler A, Elepano M, Bhardwaj S, Patel S, Silber BM, Guan S, DeArmond SJ, Renslo AR, Prusiner SB
• Tetrafluorophenoxymethyl ketone cruzain inhibitors with improved pharmacokinetic properties as therapeutic leads for Chagas' disease.
  Bioorganic & medicinal chemistry letters 2015 Neitz RJ, Bryant C, Chen S, Gut J, Hugo Caselli E, Ponce S, Chowdhury S, Xu H, Arkin MR, Ellman JA, Renslo AR
• Ligand-Induced Proton Transfer and Low-Barrier Hydrogen Bond Revealed by X-ray Crystallography.
  Journal of the American Chemical Society 2015 Nichols DA, Hargis JC, Sanishvili R, Jaishankar P, Defrees K, Smith EW, Wang KK, Prati F, Renslo AR, Woodcock HL, Chen Y
• Pharmacological dimerization and activation of the exchange factor eIF2B antagonizes the integrated stress response.
  eLife 2015 Sidrauski C, Tsai JC, Kampmann M, Hearn BR, Vedantham P, Jaishankar P, Sokabe M, Mendez AS, Newton BW, Tang EL, Verschueren E, Johnson JR, Krogan NJ, Fraser CS, Weissman JS, Renslo AR, Walter P
• A Fragment-Based Ligand Screen Against Part of a Large Protein Machine: The ND1 Domains of the AAA+ ATPase p97/VCP.
  Journal of biomolecular screening 2015 Chimenti MS, Bulfer SL, Neitz RJ, Renslo AR, Jacobson MP, James TL, Arkin MR, Kelly MJ
• Protease inhibitors targeting coronavirus and filovirus entry.
  Antiviral research 2015 Zhou Y, Vedantham P, Lu K, Agudelo J, Carrion R, Nunneley JW, Barnard D, Pöhlmann S, McKerrow JH, Renslo AR, Simmons G
• Simple plate-based, parallel synthesis of disulfide fragments using the CuAAC click reaction.
  ACS combinatorial science 2014 Turner DM, Tom CT, Renslo AR
• Efficient and stereocontrolled synthesis of 1,2,4-trioxolanes useful for ferrous iron-dependent drug delivery.
  Organic letters 2014 Fontaine SD, DiPasquale AG, Renslo AR
• Drug delivery to the malaria parasite using an arterolane-like scaffold.
  ChemMedChem 2014 Fontaine SD, Spangler B, Gut J, Lauterwasser EM, Rosenthal PJ, Renslo AR
• Lead identification to clinical candidate selection: drugs for Chagas disease.
  Journal of biomolecular screening 2014 Neitz RJ, Chen S, Supek F, Yeh V, Kellar D, Gut J, Bryant C, Gallardo-Godoy A, Molteni V, Roach SL, Khare S, Stinson M, Chatterjee AK, Robertson S, Renslo AR, Arkin M, Glynne R, McKerrow J, Siqueira-…
• Broad-spectrum allosteric inhibition of herpesvirus proteases.
  Biochemistry 2014 Gable JE, Lee GM, Jaishankar P, Hearn BR, Waddling CA, Renslo AR, Craik CS
• Hsp90 inhibitors as new leads to target parasitic diarrheal diseases.
  Antimicrobial agents and chemotherapy 2014 Debnath A, Shahinas D, Bryant C, Hirata K, Miyamoto Y, Hwang G, Gut J, Renslo AR, Pillai DR, Eckmann L, Reed SL, McKerrow JH
• UCSF Small Molecule Discovery Center: innovation, collaboration and chemical biology in the Bay Area.
  Combinatorial chemistry & high throughput screening 2014 Arkin MR, Ang KK, Chen S, Davies J, Merron C, Tang Y, Wilson CG, Renslo AR
• Successes and challenges in phenotype-based lead discovery for prion diseases.
  Journal of medicinal chemistry 2014 Ghaemmaghami S, Russo M, Renslo AR
• Fragment-based inhibitor discovery against β-lactamase.
  Future medicinal chemistry 2014 Nichols DA, Renslo AR, Chen Y
• Novel compounds lowering the cellular isoform of the human prion protein in cultured human cells.
  Bioorganic & medicinal chemistry 2014 Silber BM, Gever JR, Rao S, Li Z, Renslo AR, Widjaja K, Wong C, Giles K, Freyman Y, Elepano M, Irwin JJ, Jacobson MP, Prusiner SB
• Antimalarial Drug Discovery: From Quinine to the Dream of Eradication.
  ACS medicinal chemistry letters 2013 Renslo AR
• Tailoring small molecules for an allosteric site on procaspase-6.
  ChemMedChem 2013 Murray J, Giannetti AM, Steffek M, Gibbons P, Hearn BR, Cohen F, Tam C, Pozniak C, Bravo B, Lewcock J, Jaishankar P, Ly CQ, Zhao X, Tang Y, Chugha P, Arkin MR, Flygare J, Renslo AR
• Modulating caspase activity: beyond the active site.
  Current opinion in structural biology 2013 Murray J, Renslo AR
• Ferrous iron-dependent drug delivery enables controlled and selective release of therapeutic agents in vivo.
  Proceedings of the National Academy of Sciences of the United States of America 2013 Deu E, Chen IT, Lauterwasser EM, Valderramos J, Li H, Edgington LE, Renslo AR, Bogyo M
• Drug resistance confounding prion therapeutics.
  Proceedings of the National Academy of Sciences of the United States of America 2013 Berry DB, Lu D, Geva M, Watts JC, Bhardwaj S, Oehler A, Renslo AR, DeArmond SJ, Prusiner SB, Giles K
• Development of an ex vivo lymph node explant model for identification of novel molecules active against Leishmania major.
  Antimicrobial agents and chemotherapy 2013 Peniche AG, Osorio Y, Renslo AR, Frantz DE, Melby PC, Travi BL
• Antiprion compounds that reduce PrP(Sc) levels in dividing and stationary-phase cells.
  Bioorganic & medicinal chemistry 2013 Silber BM, Gever JR, Li Z, Gallardo-Godoy A, Renslo AR, Widjaja K, Irwin JJ, Rao S, Jacobson MP, Ghaemmaghami S, Prusiner SB
• Biaryl amides and hydrazones as therapeutics for prion disease in transgenic mice.
  The Journal of pharmacology and experimental therapeutics 2013 Lu D, Giles K, Li Z, Rao S, Dolghih E, Gever JR, Geva M, Elepano ML, Oehler A, Bryant C, Renslo AR, Jacobson MP, Dearmond SJ, Silber BM, Prusiner SB
• Hypothemycin, a fungal natural product, identifies therapeutic targets in Trypanosoma brucei [corrected].
  eLife 2013 Nishino M, Choy JW, Gushwa NN, Oses-Prieto JA, Koupparis K, Burlingame AL, Renslo AR, McKerrow JH, Taunton J
• Genetic and neural mechanisms that inhibit Drosophila from mating with other species.
  Cell 2013 Fan P, Manoli DS, Ahmed OM, Chen Y, Agarwal N, Kwong S, Cai AG, Neitz J, Renslo A, Baker BS, Shah NM
• A high-throughput functional screen identifies small molecule regulators of temperature- and mechano-sensitive K2P channels.
  ACS chemical biology 2013 Bagriantsev SN, Ang KH, Gallardo-Godoy A, Clark KA, Arkin MR, Renslo AR, Minor DL
• Pharmacological brake-release of mRNA translation enhances cognitive memory.
  eLife 2013 Sidrauski C, Acosta-Alvear D, Khoutorsky A, Vedantham P, Hearn BR, Li H, Gamache K, Gallagher CM, Ang KK, Wilson C, Okreglak V, Ashkenazi A, Hann B, Nader K, Arkin MR, Renslo AR, Sonenberg N, Walter P
• 2-Aminothiazoles with improved pharmacotherapeutic properties for treatment of prion disease.
  ChemMedChem 2013 Li Z, Silber BM, Rao S, Gever JR, Bryant C, Gallardo-Godoy A, Dolghih E, Widjaja K, Elepano M, Jacobson MP, Prusiner SB, Renslo AR
• Pharmacokinetics and metabolism of 2-aminothiazoles with antiprion activity in mice.
  Pharmaceutical research 2013 Silber BM, Rao S, Fife KL, Gallardo-Godoy A, Renslo AR, Dalvie DK, Giles K, Freyman Y, Elepano M, Gever JR, Li Z, Jacobson MP, Huang Y, Benet LZ, Prusiner SB
• Chemical-biological characterization of a cruzain inhibitor reveals a second target and a mammalian off-target.
  Beilstein journal of organic chemistry 2013 Choy JW, Bryant C, Calvet CM, Doyle PS, Gunatilleke SS, Leung SS, Ang KK, Chen S, Gut J, Oses-Prieto JA, Johnston JB, Arkin MR, Burlingame AL, Taunton J, Jacobson MP, McKerrow JM, Podust LM, Renslo AR
• Mechanistic and structural understanding of uncompetitive inhibitors of caspase-6.
  PloS one 2012 Heise CE, Murray J, Augustyn KE, Bravo B, Chugha P, Cohen F, Giannetti AM, Gibbons P, Hannoush RN, Hearn BR, Jaishankar P, Ly CQ, Shah K, Stanger K, Steffek M, Tang Y, Zhao X, Lewcock JW, Renslo AR, …
• Ferrous iron-dependent delivery of therapeutic agents to the malaria parasite.
  Future medicinal chemistry 2012 Mahajan SS, Gut J, Rosenthal PJ, Renslo AR
• Predicting and improving the membrane permeability of peptidic small molecules.
  Journal of medicinal chemistry 2012 Rafi SB, Hearn BR, Vedantham P, Jacobson MP, Renslo AR
• Structure-based design of potent and ligand-efficient inhibitors of CTX-M class A β-lactamase.
  Journal of medicinal chemistry 2012 Nichols DA, Jaishankar P, Larson W, Smith E, Liu G, Beyrouthy R, Bonnet R, Renslo AR, Chen Y
• Investigating the antimalarial action of 1,2,4-trioxolanes with fluorescent chemical probes.
  Journal of medicinal chemistry 2011 Hartwig CL, Lauterwasser EM, Mahajan SS, Hoke JM, Cooper RA, Renslo AR
• Drug discovery for neglected tropical diseases at the Sandler Center.
  Future medicinal chemistry 2011 Robertson SA, Renslo AR
• Predicting binding to p-glycoprotein by flexible receptor docking.
  PLoS computational biology 2011 Dolghih E, Bryant C, Renslo AR, Jacobson MP
• Mining a cathepsin inhibitor library for new antiparasitic drug leads.
  PLoS neglected tropical diseases 2011 Ang KK, Ratnam J, Gut J, Legac J, Hansell E, Mackey ZB, Skrzypczynska KM, Debnath A, Engel JC, Rosenthal PJ, McKerrow JH, Arkin MR, Renslo AR
• Simple one-pot synthesis of disulfide fragments for use in disulfide-exchange screening.
  ACS combinatorial science 2011 Burlingame MA, Tom CT, Renslo AR
• Identification of small molecule lead compounds for visceral leishmaniasis using a novel ex vivo splenic explant model system.
  PLoS neglected tropical diseases 2011 Osorio Y, Travi BL, Renslo AR, Peniche AG, Melby PC
• A fragmenting hybrid approach for targeted delivery of multiple therapeutic agents to the malaria parasite.
  ChemMedChem 2011 Mahajan SS, Deu E, Lauterwasser EM, Leyva MJ, Ellman JA, Bogyo M, Renslo AR
• 2-Aminothiazoles as therapeutic leads for prion diseases.
  Journal of medicinal chemistry 2011 Gallardo-Godoy A, Gever J, Fife KL, Silber BM, Prusiner SB, Renslo AR
• Antibacterial oxazolidinones: emerging structure-toxicity relationships.
  Expert review of anti-infective therapy 2010 Renslo AR
• N-Aryl-2-oxazolidinone-5-carboxamides and Their Derivatives. US Patent 7,645,781
  N-Aryl-2-oxazolidinone-5-carboxamides and Their Derivatives. US Patent 7,645,781 2010 Thomas, RC, Poel, T-J, Barbachyn, MR, Gordeev, MF, Luehr, GW, Renslo, A, Singh, U, Joysula, VPVN
• Small-Molecule Inhibitors of the Androgen Receptor US Patent 7,696,227
  Small-Molecule Inhibitors of the Androgen Receptor US Patent 7,696,227 2010 Diamond, M, Jones, J, Renslo, A
• Discovery of 2-aminothiazoles as potent antiprion compounds.
  Journal of virology 2009 Ghaemmaghami S, May BC, Renslo AR, Prusiner SB
• Novel non-peptidic vinylsulfones targeting the S2 and S3 subsites of parasite cysteine proteases.
  Bioorganic & medicinal chemistry letters 2009 Bryant C, Kerr ID, Debnath M, Ang KK, Ratnam J, Ferreira RS, Jaishankar P, Zhao D, Arkin MR, McKerrow JH, Brinen LS, Renslo AR
• Divergent modes of enzyme inhibition in a homologous structure-activity series.
  Journal of medicinal chemistry 2009 Ferreira RS, Bryant C, Ang KK, McKerrow JH, Shoichet BK, Renslo AR
• Drug discovery for schistosomiasis: hit and lead compounds identified in a library of known drugs by medium-throughput phenotypic screening.
  PLoS neglected tropical diseases 2009 Abdulla MH, Ruelas DS, Wolff B, Snedecor J, Lim KC, Xu F, Renslo AR, Williams J, McKerrow JH, Caffrey CR
• When Medical Need is not Matched by Market Opportunity
  Pharma Focus Asia 2008 Renslo, AR
• Potency and selectivity of P2/P3-modified inhibitors of cysteine proteases from trypanosomes.
  Bioorganic & medicinal chemistry letters 2007 Jaishankar P, Hansell E, Zhao DM, Doyle PS, McKerrow JH, Renslo AR
• A practical synthesis of differentially protected 2-(hydroxymethyl)piperazines.
  The Journal of organic chemistry 2007 Gao H, Renslo AR
• A distal methyl substituent attenuates mitochondrial protein synthesis inhibition in oxazolidinone antibacterials.
  Bioorganic & medicinal chemistry letters 2007 Renslo AR, Atuegbu A, Herradura P, Jaishankar P, Ji M, Leach KL, Huband MD, Dermyer MR, Wu L, Vara Prasad JV, Gordeev MF
• Antimicrobial [3.1.0] bicyclohexylphenyl-oxazolidinone derivatives and analogues. US Patent 7,279,494
  Antimicrobial [3.1.0] bicyclohexylphenyl-oxazolidinone derivatives and analogues. US Patent 7,279,494 2007 Renslo, AR, Gordeev, MF, Patel, DV, Gao, H, and Josyula, VPVN
• The Echinocandins: Total and Semi-Synthetic Approaches in Anti-fungal Drug Discovery
  Anti-infective Agents in Medicinal Chemistry 2007 Renslo, AR
• Drug discovery and development for neglected parasitic diseases.
  Nature chemical biology 2006 Renslo AR, McKerrow JH
• Synthesis and structure-activity studies of antibacterial oxazolidinones containing dihydrothiopyran or dihydrothiazine C-rings.
  Bioorganic & medicinal chemistry letters 2006 Renslo AR, Luehr GW, Lam S, Westlund NE, Gómez M, Hackbarth CJ, Patel DV, Gordeev MF
• Recent developments in the identification of novel oxazolidinone antibacterial agents.
  Bioorganic & medicinal chemistry 2006 Renslo AR, Luehr GW, Gordeev MF
• Conformational constraint in oxazolidinone antibacterials. Part 2: Synthesis and structure-activity studies of oxa-, aza-, and thiabicyclo[3.1.0]hexylphenyl oxazolidinones.
  Bioorganic & medicinal chemistry letters 2006 Renslo AR, Gao H, Jaishankar P, Venkatachalam R, Gómez M, Blais J, Huband M, Vara Prasad JV, Gordeev MF
• Antimicrobial Dihydrothiazine and Dihydrothiopyran Oxazolidinones. US Patent 7,101,874
  Antimicrobial Dihydrothiazine and Dihydrothiopyran Oxazolidinones. US Patent 7,101,874 2006 Gordeev, MF, Renslo, A, Luehr, GW, Lam, S, Westlund, NE, and Patel, DV
• N-Aryl-2-oxazolidinone-5-carboxamides and Their Derivatives. US Patent 7,141,588
  N-Aryl-2-oxazolidinone-5-carboxamides and Their Derivatives. US Patent 7,141,588 2006 Thomas, RC, Poel, T-J, Barbachyn, MR, Gordeev, MF, Luehr, GW, Renslo, A, Singh, U, Joysula, VPVN
• Conformational constraint in oxazolidinone antibacterials. Synthesis and structure-activity studies of (azabicyclo[3.1.0]hexylphenyl)oxazolidinones.
  Journal of medicinal chemistry 2005 Renslo AR, Jaishankar P, Venkatachalam R, Hackbarth C, Lopez S, Patel DV, Gordeev MF
• Synthesis of aza-, oxa-, and thiabicyclo[3.1.0]hexane heterocycles from a common synthetic intermediate.
  Organic letters 2005 Renslo AR, Gao H, Jaishankar P, Venkatachalam R, Gordeev MF
• Antimicrobial [3.1.0] Bicyclic Oxazolidinone Derivatives. US Patent 6,875,784
  Antimicrobial [3.1.0] Bicyclic Oxazolidinone Derivatives. US Patent 6,875,784 2005 Gordeev, MF, Renslo, A, and Patel, DV.
• Antimicrobial Dihydrothiazine and Dihydrothiopyran Oxazolidinones. US Patent 6,884,813
  Antimicrobial Dihydrothiazine and Dihydrothiopyran Oxazolidinones. US Patent 6,884,813 2005 Gordeev, MF, Renslo, A, Luehr, GW, Lam, S, Westlund, NE, and Patel, DV
• N-Aryl-2-oxazolidinone-5-carboxamides and Their Derivatives. US Patent 6,919,329
  N-Aryl-2-oxazolidinone-5-carboxamides and Their Derivatives. US Patent 6,919,329 2005 Thomas, RC, Poel, T-J, Barbachyn, MR, Gordeev, MF, Luehr, GW, Renslo, A, and Singh, U
• Intramolecular [4 + 2] cycloadditions of iminoacetonitriles: a new class of azadienophiles for hetero Diels-Alder reactions.
  Journal of the American Chemical Society 2003 Amos DT, Renslo AR, Danheiser RL
• Preparation of Substituted Pyridines via Regiocontrolled [4+2] Cycloadditions of Oximinosulfonates: Methyl 5-Methylpyridine-2-Carboxylate
  Org. Syn. 2003 Danheiser, RL, Renslo, AR, Amos, DT, and Wright, GT
• Isolation of an Acid/Base Complex in Solution Puts the Brakes on Nitrogen Inversion We are grateful for financial support from the Skaggs Research Foundation and the National Institutes of Health. We are pleased to acknowledge advice from Professors Stephen Craig and Dmitry Rudkevich.
  Angewandte Chemie (International ed. in English) 2001 Wash PL, Renslo AR, Rebek J
• Isolation of an Acid/Base Complex in Solution Puts the Brakes on Nitrogen Inversion
  Angew. Chem. Int. Ed. 2001 Wash, PL, Renslo, AR, and Rebek, J.
• Molecular Recognition with Introverted Functionality We are grateful for financial support from the Skaggs Research Foundation and the National Institutes of Health. We thank Prof. Dmitry Rudkevich and Dr. Paul Wash and Dr. Laura Pasternack for helpful advice and instrumental support.
  Angewandte Chemie (International ed. in English) 2000 Renslo AR, Rebek J
• Nanoscale Container Structures and Their Host - Guest Properties We are grateful for financial support from the Skaggs Research Foundation and the National Institutes of Health. Dr. Laura Pasternack and Dr. Takeharu Haino are sincerely acknowledged for assistance with the 2D NMR experiments and experimental advise, respectively.
  Angewandte Chemie (International ed. in English) 2000 Tucci FC, Renslo AR, Rudkevich DM, Rebek Jr J
• Molecular Recognition with Introverted Functionality
  Angew. Chem. Int. Ed. 2000 Renslo, AR and Rebek, J.
• Nanoscale Container Structures and their Host¬–Guest Properties
  Angew. Chem. Int. Ed. 2000 Tucci, FC, Renslo, AR, Rudkevich, DM, and Rebek, J.
• Synthesis and Assembly of Self-Complementary Cavitands
  J. Am. Chem. Soc. 2000 Renslo, AR, Tucci, FC, Rudkevich, DM, and Rebek, J.
• Encapsulation of Ion-Molecule Complexes: Second-Sphere Supramolecular Chemistry
  J. Am. Chem. Soc. 1999 Lützen, A, Renslo, AR, Schalley, CA, O’Leary, BM, and Rebek, J.
• Self-Complementary Cavitands
  J. Am. Chem. Soc. 1999 Renslo, AR, Rudkevich, DM, and Rebek, J.
• Silica-Promoted Diels–Alder Reactions in Carbon Dioxide from Gaseous to Supercritical Conditions
  J. Phys. Chem. B 1999 Weinstein, RD, Renslo, AR, Danheiser, RL, and Tester, JW
• Synthesis of Substituted Pyridines via Regiocontrolled [4+2] Cycloadditions of Oximinosulfonates
  J. Org. Chem. 1998 Renslo, AR and Danheiser, RL.
• Concerning the Regiochemical Course of the Diels-Alder Reaction in Supercritical Carbon Dioxide.
  The Journal of organic chemistry 1997 Renslo AR, Weinstein RD, Tester JW, Danheiser RL
• Concerning the Regiochemical Course of the Diels–Alder Reaction in Supercritical Carbon Dioxide
  J. Org. Chem. 1997 Renslo, AR, Weinstein, RD, Tester, JW, and Danheiser, RL.
• Kinetic Correlation of Diels–Alder Reactions in Supercritical Carbon Dioxide
  J. Phys. Chem. 1996 Weinstein, RD, Renslo, AR, Danheiser, RL, Harris, JG, and Tester, JW.