Jeffrey Neitz, PhD
Specialist
Pharmaceutical Chemistry
School of Pharmacy

Publications (25)

Top publication keywords:
NaphthalenesEstrogen Receptor alphaKetonesSchistosomicidesMitogen-Activated Protein Kinase 10Schistosoma mansoniThionesTrypanosoma cruziProtozoan ProteinsHydrocarbons, FluorinatedChagas DiseaseTrypanocidal AgentsDrug DiscoveryEnzyme InhibitorsHigh-Throughput Screening Assays

• Identifying ligands for the PHD1 finger of KDM5A through high-throughput screening.
  RSC chemical biology 2023 Ortiz G, Longbotham JE, Qin SL, Zhang MY, Lee GM, Neitz RJ, Kelly MJS, Arkin MR, Fujimori DG
• 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
• A Systematic Approach to the Discovery of Protein-Protein Interaction Stabilizers.
  ACS central science 2023 Kenanova DN, Visser EJ, Virta JM, Sijbesma E, Centorrino F, Vickery HR, Zhong M, Neitz RJ, Brunsveld L, Ottmann C, Arkin MR
• 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, …

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• 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, …
• TPT sulfonate, a single, oral dose schistosomicidal prodrug: In vivo efficacy, disposition and metabolic profiling.
  International journal for parasitology. Drugs and drug resistance 2018 Wolfe AR, Neitz RJ, Burlingame M, Suzuki BM, Lim KC, Scheideler M, Nelson DL, Benet LZ, Caffrey CR
• Optimization of Phenyl Indole Inhibitors of the AAA+ ATPase p97.
  ACS medicinal chemistry letters 2018 LaPorte MG, Burnett JC, Colombo R, Bulfer SL, Alverez C, Chou TF, Neitz RJ, Green N, Moore WJ, Yue Z, Li S, Arkin MR, Wipf P, Huryn DM
• 2.3 Å resolution cryo-EM structure of human p97 and mechanism of allosteric inhibition.
  Science (New York, N.Y.) 2016 Banerjee S, Bartesaghi A, Merk A, Rao P, Bulfer SL, Yan Y, Green N, Mroczkowski B, Neitz RJ, Wipf P, Falconieri V, Deshaies RJ, Milne JL, Huryn D, Arkin M, Subramaniam S
• Structure-Bioactivity Relationship for Benzimidazole Thiophene Inhibitors of Polo-Like Kinase 1 (PLK1), a Potential Drug Target in Schistosoma mansoni.
  PLoS neglected tropical diseases 2016 Long T, Neitz RJ, Beasley R, Kalyanaraman C, Suzuki BM, Jacobson MP, Dissous C, McKerrow JH, Drewry DH, Zuercher WJ, Singh R, Caffrey CR
• Allosteric Indole Amide Inhibitors of p97: Identification of a Novel Probe of the Ubiquitin Pathway.
  ACS medicinal chemistry letters 2015 Alverez C, Bulfer SL, Chakrasali R, Chimenti MS, Deshaies RJ, Green N, Kelly M, LaPorte MG, Lewis TS, Liang M, Moore WJ, Neitz RJ, Peshkov VA, Walters MA, Zhang F, Arkin MR, Wipf P, Huryn DM
• Structure-Activity Study of Bioisosteric Trifluoromethyl and Pentafluorosulfanyl Indole Inhibitors of the AAA ATPase p97.
  ACS medicinal chemistry letters 2015 Alverez C, Arkin MR, Bulfer SL, Colombo R, Kovaliov M, LaPorte MG, Lim C, Liang M, Moore WJ, Neitz RJ, Yan Y, Yue Z, Huryn DM, Wipf P
• Utilizing Chemical Genomics to Identify Cytochrome b as a Novel Drug Target for Chagas Disease.
  PLoS pathogens 2015 Khare S, Roach SL, Barnes SW, Hoepfner D, Walker JR, Chatterjee AK, Neitz RJ, Arkin MR, McNamara CW, Ballard J, Lai Y, Fu Y, Molteni V, Yeh V, McKerrow JH, Glynne RJ, Supek F
• 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
• 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
• 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-…
• Selective and brain-permeable polo-like kinase-2 (Plk-2) inhibitors that reduce α-synuclein phosphorylation in rat brain.
  ChemMedChem 2013 Aubele DL, Hom RK, Adler M, Galemmo RA, Bowers S, Truong AP, Pan H, Beroza P, Neitz RJ, Yao N, Lin M, Tonn G, Zhang H, Bova MP, Ren Z, Tam D, Ruslim L, Baker J, Diep L, Fitzgerald K, Hoffman J, Motter…
• Design and synthesis of hydroxyethylamine (HEA) BACE-1 inhibitors: prime side chromane-containing inhibitors.
  Bioorganic & medicinal chemistry letters 2013 Ng RA, Sun M, Bowers S, Hom RK, Probst GD, John V, Fang LY, Maillard M, Gailunas A, Brogley L, Neitz RJ, Tung JS, Pleiss MA, Konradi AW, Sham HL, Dappen MS, Adler M, Yao N, Zmolek W, Nakamura D, Quinn…
• Design and synthesis of highly selective, orally active Polo-like kinase-2 (Plk-2) inhibitors.
  Bioorganic & medicinal chemistry letters 2013 Bowers S, Truong AP, Ye M, Aubele DL, Sealy JM, Neitz RJ, Hom RK, Chan W, Dappen MS, Galemmo RA, Konradi AW, Sham HL, Zhu YL, Beroza P, Tonn G, Zhang H, Hoffman J, Motter R, Fauss D, Tanaka P, Bova MP…
• Novel cinnoline-based inhibitors of LRRK2 kinase activity.
  Bioorganic & medicinal chemistry letters 2012 Garofalo AW, Adler M, Aubele DL, Bowers S, Franzini M, Goldbach E, Lorentzen C, Neitz RJ, Probst GD, Quinn KP, Santiago P, Sham HL, Tam D, Truong AP, Ye XM, Ren Z
• Highly selective c-Jun N-terminal kinase (JNK) 3 inhibitors with in vitro CNS-like pharmacokinetic properties II. Central core replacement.
  Bioorganic & medicinal chemistry letters 2011 Neitz RJ, Konradi AW, Sham HL, Zmolek W, Wong K, Qin A, Lorentzen C, Nakamura D, Quinn KP, Sauer JM, Powell K, Ruslim L, Chereau D, Ren Z, Anderson J, Bard F, Yednock TA, Griswold-Prenner I
• Design and synthesis of a novel, orally active, brain penetrant, tri-substituted thiophene based JNK inhibitor.
  Bioorganic & medicinal chemistry letters 2011 Bowers S, Truong AP, Neitz RJ, Neitzel M, Probst GD, Hom RK, Peterson B, Galemmo RA, Konradi AW, Sham HL, Tóth G, Pan H, Yao N, Artis DR, Brigham EF, Quinn KP, Sauer JM, Powell K, Ruslim L, Ren Z, …
• Design and synthesis of disubstituted thiophene and thiazole based inhibitors of JNK.
  Bioorganic & medicinal chemistry letters 2010 Hom RK, Bowers S, Sealy JM, Truong AP, Probst GD, Neitzel ML, Neitz RJ, Fang L, Brogley L, Wu J, Konradi AW, Sham HL, Tóth G, Pan H, Yao N, Artis DR, Quinn K, Sauer JM, Powell K, Ren Z, Bard F, …
• Studies on the synthesis of landomycin A. Synthesis of the originally assigned structure of the aglycone, landomycinone, and revision of structure.
  The Journal of organic chemistry 2004 Roush WR, Neitz RJ
• Structure-activity relationships for inhibition of cysteine protease activity and development of Plasmodium falciparum by peptidyl vinyl sulfones.
  Antimicrobial agents and chemotherapy 2003 Shenai BR, Lee BJ, Alvarez-Hernandez A, Chong PY, Emal CD, Neitz RJ, Roush WR, Rosenthal PJ