☰

Hans Edward Purkey - Publications

Affiliations: 
2002 Scripps Research Institute, La Jolla, La Jolla, CA, United States 
Tree Info Similar researchers PubMed Report error

43 high-probability publications. We are testing a new system for linking publications to authors. You can help! If you notice any inaccuracies, please sign in and mark papers as correct or incorrect matches. If you identify any major omissions or other inaccuracies in the publication list, please let us know.

Year Citation  Score
2022 Hanan EJ, Braun MG, Heald RA, MacLeod C, Chan C, Clausen S, Edgar KA, Eigenbrot C, Elliott R, Endres N, Friedman LS, Gogol E, Gu XH, Thibodeau RH, Jackson PS, ... ... Purkey HE, et al. Discovery of GDC-0077 (Inavolisib), a Highly Selective Inhibitor and Degrader of Mutant PI3Kα. Journal of Medicinal Chemistry. PMID 36455032 DOI: 10.1021/acs.jmedchem.2c01422  0.342
2022 Wei B, Robarge K, Labadie SS, Chen J, Corson LB, DiPasquale A, Dragovich PS, Eigenbrot C, Evangelista M, Fauber BP, Hitz A, Hong R, Wah Lai K, Liu W, Ma S, ... ... Purkey HE, et al. Structure-based Optimization of Hydroxylactam as Potent, Cell-Active Inhibitors of Lactate Dehydrogenase. Bioorganic & Medicinal Chemistry Letters. 128576. PMID 35065235 DOI: 10.1016/j.bmcl.2022.128576  0.396
2020 Crawford JJ, Lee W, Johnson AR, Delatorre KJ, Chen J, Eigenbrot C, Heidmann J, Kakiuchi-Kiyota S, Katewa A, Kiefer JR, Liu L, Lubach JW, Misner D, Purkey H, Reif K, et al. Stereochemical Differences in Fluorocyclopropyl Amides Enable Tuning of Btk Inhibition and Off-Target Activity. Acs Medicinal Chemistry Letters. 11: 1588-1597. PMID 32832028 DOI: 10.1021/Acsmedchemlett.0C00249  0.406
2019 Bronner SM, Merrick KA, Murray J, Salphati L, Moffat JG, Pang J, Sneeringer CJ, Dompe N, Cyr P, Purkey H, Boenig GL, Li J, Kolesnikov A, Larouche-Gauthier R, Lai KW, et al. Design of a brain-penetrant CDK4/6 inhibitor for glioblastoma. Bioorganic & Medicinal Chemistry Letters. PMID 31307887 DOI: 10.1016/J.Bmcl.2019.06.021  0.37
2019 Ladi E, Everett C, Stivala CE, Daniels BE, Durk MR, Harris SF, Huestis M, Purkey HE, Staben ST, Augustin M, Blaesse M, Steinbacher S, Eidenschenk C, Pappu R, Siu M. Design and Evaluation of Highly-Selective Human Immunoproteasome Inhibitors Reveals a Compensatory Process that Preserves Immune Cell Viability. Journal of Medicinal Chemistry. PMID 31283222 DOI: 10.1021/Acs.Jmedchem.9B00509  0.337
2018 Ho H, Miu A, Alexander MK, Garcia NK, Oh A, Zilberleyb I, Reichelt M, Austin CD, Tam C, Shriver S, Hu H, Labadie SS, Liang J, Wang L, Wang J, ... ... Purkey HE, et al. Structural basis for dual-mode inhibition of the ABC transporter MsbA. Nature. PMID 29720648 DOI: 10.1038/S41586-018-0083-5  0.381
2016 Purkey HE, Robarge K, Chen J, Chen Z, Corson LB, Ding CZ, DiPasquale AG, Dragovich PS, Eigenbrot C, Evangelista M, Fauber BP, Gao Z, Ge H, Hitz A, Ho Q, et al. Cell Active Hydroxylactam Inhibitors of Human Lactate Dehydrogenase with Oral Bioavailability in Mice. Acs Medicinal Chemistry Letters. 7: 896-901. PMID 27774125 DOI: 10.1021/Acsmedchemlett.6B00190  0.39
2016 Chan BK, Hanan EJ, Bowman K, Bryan MC, Burdick DJ, Chan EW, Chen Y, Clausen S, Dela Vega T, Dotson J, Eigenbrot C, Elliott RL, Heald RA, Jackson PS, Knight JD, ... ... Purkey HE, et al. Discovery of a Non-Covalent, Mutant-Selective Epidermal Growth Factor Receptor Inhibitor. Journal of Medicinal Chemistry. PMID 27564586 DOI: 10.1021/Acs.Jmedchem.6B00995  0.412
2016 Boudreau A, Purkey HE, Hitz A, Robarge K, Peterson D, Labadie S, Kwong M, Hong R, Gao M, Del Nagro C, Pusapati R, Ma S, Salphati L, Pang J, Zhou A, et al. Metabolic plasticity underpins innate and acquired resistance to LDHA inhibition. Nature Chemical Biology. PMID 27479743 DOI: 10.1038/Nchembio.2143  0.361
2016 Heald R, Bowman KK, Bryan MC, Burdick D, Chan B, Chan E, Chen Y, Clausen S, Dominguez-Fernandez B, Eigenbrot C, Elliott R, Hanan EJ, Jackson P, Knight J, La H, ... ... Purkey H, et al. Correction to Noncovalent Mutant Selective Epidermal Growth Factor Receptor Inhibitors: A Lead Optimization Case Study. Journal of Medicinal Chemistry. PMID 26967667 DOI: 10.1021/Acs.Jmedchem.6B00301  0.301
2016 Bryan MC, Burdick DJ, Chan BK, Chen Y, Clausen S, Dotson J, Eigenbrot C, Elliott R, Hanan EJ, Heald R, Jackson P, La H, Lainchbury M, Malek S, Mann SE, ... Purkey HE, et al. Pyridones as Highly Selective, Noncovalent Inhibitors of T790M Double Mutants of EGFR. Acs Medicinal Chemistry Letters. 7: 100-4. PMID 26819674 DOI: 10.1021/Acsmedchemlett.5B00428  0.396
2015 Hanan EJ, Baumgardner M, Bryan MC, Chen Y, Eigenbrot C, Fan P, Gu XH, La H, Malek S, Purkey HE, Schaefer G, Schmidt S, Sideris S, Yen I, Yu C, et al. 4-Aminoindazolyl-dihydrofuro[3,4-d]pyrimidines as non-covalent inhibitors of mutant epidermal growth factor receptor tyrosine kinase. Bioorganic & Medicinal Chemistry Letters. PMID 26639762 DOI: 10.1016/J.Bmcl.2015.11.078  0.326
2015 Heald RA, Chan BK, Bryan 2C, Eigenbrot C, Yu C, Burdick D, Hanan EJ, Chan E, Schaefer G, La H, Purkey H, Knight J, Yen I, Jackson P, Bowman K, et al. Noncovalent Mutant Selective Epidermal Growth Factor Receptor Inhibitors: A Lead Optimization Case History. Journal of Medicinal Chemistry. PMID 26455919 DOI: 10.1021/Acs.Jmedchem.5B01412  0.377
2015 Labadie S, Dragovich PS, Chen J, Fauber BP, Boggs J, Corson LB, Ding CZ, Eigenbrot C, Ge H, Ho Q, Lai KW, Ma S, Malek S, Peterson D, Purkey HE, et al. Optimization of 5-(2,6-dichlorophenyl)-3-hydroxy-2-mercaptocyclohex-2-enones as potent inhibitors of human lactate dehydrogenase. Bioorganic & Medicinal Chemistry Letters. 25: 75-82. PMID 25466195 DOI: 10.1016/J.Bmcl.2014.11.008  0.463
2014 Fauber BP, Dragovich PS, Chen J, Corson LB, Ding CZ, Eigenbrot C, Labadie S, Malek S, Peterson D, Purkey HE, Robarge K, Sideris S, Ultsch M, Wei B, Yen I, et al. Identification of 3,6-disubstituted dihydropyrones as inhibitors of human lactate dehydrogenase. Bioorganic & Medicinal Chemistry Letters. 24: 5683-7. PMID 25467161 DOI: 10.1016/J.Bmcl.2014.10.067  0.375
2014 Thomas AA, Hunt KW, Newhouse B, Watts RJ, Liu X, Vigers G, Smith D, Rhodes SP, Brown KD, Otten JN, Burkard M, Cox AA, Geck Do MK, Dutcher D, Rana S, ... ... Purkey HE, et al. 8-Tetrahydropyran-2-yl chromans: highly selective beta-site amyloid precursor protein cleaving enzyme 1 (BACE1) inhibitors. Journal of Medicinal Chemistry. 57: 10112-29. PMID 25411915 DOI: 10.1021/Jm5015132  0.458
2014 Hanan EJ, Eigenbrot C, Bryan MC, Burdick DJ, Chan BK, Chen Y, Dotson J, Heald RA, Jackson PS, La H, Lainchbury MD, Malek S, Purkey HE, Schaefer G, Schmidt S, et al. Discovery of selective and noncovalent diaminopyrimidine-based inhibitors of epidermal growth factor receptor containing the T790M resistance mutation. Journal of Medicinal Chemistry. 57: 10176-91. PMID 25383627 DOI: 10.1021/Jm501578N  0.387
2014 Tao ZF, Hasvold L, Wang L, Wang X, Petros AM, Park CH, Boghaert ER, Catron ND, Chen J, Colman PM, Czabotar PE, Deshayes K, Fairbrother WJ, Flygare JA, Hymowitz SG, ... ... Purkey HE, et al. Discovery of a Potent and Selective BCL-XL Inhibitor with in Vivo Activity. Acs Medicinal Chemistry Letters. 5: 1088-93. PMID 25313317 DOI: 10.1021/Ml5001867  0.451
2014 Dragovich PS, Fauber BP, Boggs J, Chen J, Corson LB, Ding CZ, Eigenbrot C, Ge H, Giannetti AM, Hunsaker T, Labadie S, Li C, Liu Y, Liu Y, Ma S, ... ... Purkey HE, et al. Identification of substituted 3-hydroxy-2-mercaptocyclohex-2-enones as potent inhibitors of human lactate dehydrogenase. Bioorganic & Medicinal Chemistry Letters. 24: 3764-71. PMID 25037916 DOI: 10.1016/J.Bmcl.2014.06.076  0.418
2014 Volgraf M, Chan L, Huestis MP, Purkey HE, Burkard M, Geck Do M, Harris J, Hunt KW, Liu X, Lyssikatos JP, Rana S, Thomas AA, Vigers GP, Siu M. Synthesis, characterization, and PK/PD studies of a series of spirocyclic pyranochromene BACE1 inhibitors. Bioorganic & Medicinal Chemistry Letters. 24: 2477-80. PMID 24780121 DOI: 10.1016/J.Bmcl.2014.04.012  0.397
2014 Thomas AA, Hunt KW, Volgraf M, Watts RJ, Liu X, Vigers G, Smith D, Sammond D, Tang TP, Rhodes SP, Metcalf AT, Brown KD, Otten JN, Burkard M, Cox AA, ... ... Purkey HE, et al. Discovery of 7-tetrahydropyran-2-yl chromans: β-site amyloid precursor protein cleaving enzyme 1 (BACE1) inhibitors that reduce amyloid β-protein (Aβ) in the central nervous system. Journal of Medicinal Chemistry. 57: 878-902. PMID 24397738 DOI: 10.1021/Jm401635N  0.459
2014 O'Brien T, Purkey H, Hitz A, Peterson D, Boudreau A, Delnagro C, Kwong M, Hong R, Gao M, Pang J, Vanderbilt A, Williams S, Salphati L, Sampath D, Hatzivassiliou G, et al. Abstract 964: Inhibiting glycolysis with an LDHA inhibitor: A new solution to an old problem Cancer Research. 74: 964-964. DOI: 10.1158/1538-7445.Am2014-964  0.372
2014 Boudreau A, Peterson D, Moffat J, Liu B, Kwong M, Gao M, Purkey H, O'Brien T, Hatzivassiliou G, Daemen A, Evangelista M. Abstract 1423: Resistance to LDHA inhibitors requires signaling through the AMPK/mTOR/S6K pathway leading to increased oxidative phosphorylation Cancer Research. 74: 1423-1423. DOI: 10.1158/1538-7445.Am2014-1423  0.332
2013 Dragovich PS, Fauber BP, Corson LB, Ding CZ, Eigenbrot C, Ge H, Giannetti AM, Hunsaker T, Labadie S, Liu Y, Malek S, Pan B, Peterson D, Pitts K, Purkey HE, et al. Identification of substituted 2-thio-6-oxo-1,6-dihydropyrimidines as inhibitors of human lactate dehydrogenase. Bioorganic & Medicinal Chemistry Letters. 23: 3186-94. PMID 23628333 DOI: 10.1016/J.Bmcl.2013.04.001  0.397
2013 Hunt KW, Cook AW, Watts RJ, Clark CT, Vigers G, Smith D, Metcalf AT, Gunawardana IW, Burkard M, Cox AA, Geck Do MK, Dutcher D, Thomas AA, Rana S, Kallan NC, ... ... Purkey H, et al. Spirocyclic β-site amyloid precursor protein cleaving enzyme 1 (BACE1) inhibitors: from hit to lowering of cerebrospinal fluid (CSF) amyloid β in a higher species. Journal of Medicinal Chemistry. 56: 3379-403. PMID 23537249 DOI: 10.1021/Jm4002154  0.432
2013 Long DD, Frieman B, Hegde SS, Hill CM, Jiang L, Kintz S, Marquess DG, Purkey H, Shaw JP, Steinfeld T, Wilson MS, Wrench K. A multivalent approach towards linked dual-pharmacology prostaglandin F receptor agonist/carbonic anhydrase-II inhibitors for the treatment of glaucoma. Bioorganic & Medicinal Chemistry Letters. 23: 939-43. PMID 23317571 DOI: 10.1016/J.Bmcl.2012.12.058  0.335
2013 Huestis MP, Liu W, Volgraf M, Purkey HE, Yu C, Wang W, Smith D, Vigers G, Dutcher D, Hunt KW, Siu M. Diethylaminosulfur trifluoride-mediated intramolecular cyclization of 2-hydroxycycloalkylureas to fused bicyclic aminooxazoline compounds and evaluation of their biochemical activity against β-secretase-1 (BACE-1) Tetrahedron Letters. 54: 5802-5807. DOI: 10.2210/Pdb4L7G/Pdb  0.338
2010 Ameriks MK, Bembenek SD, Burdett MT, Choong IC, Edwards JP, Gebauer D, Gu Y, Karlsson L, Purkey HE, Staker BL, Sun S, Thurmond RL, Zhu J. Diazinones as P2 replacements for pyrazole-based cathepsin S inhibitors. Bioorganic & Medicinal Chemistry Letters. 20: 4060-4. PMID 20541404 DOI: 10.1016/J.Bmcl.2010.05.086  0.341
2009 Zhong M, Bui M, Shen W, Baskaran S, Allen DA, Elling RA, Flanagan WM, Fung AD, Hanan EJ, Harris SO, Heumann SA, Hoch U, Ivy SN, Jacobs JW, Lam S, ... ... Purkey HE, et al. 2-Aminobenzimidazoles as potent Aurora kinase inhibitors. Bioorganic & Medicinal Chemistry Letters. 19: 5158-61. PMID 19646866 DOI: 10.1016/J.Bmcl.2009.07.016  0.433
2008 Fucini RV, Hanan EJ, Romanowski MJ, Elling RA, Lew W, Barr KJ, Zhu J, Yoburn JC, Liu Y, Fahr BT, Fan J, Lu Y, Pham P, Choong IC, VanderPorten EC, ... ... Purkey HE, et al. Design and synthesis of 2-amino-pyrazolopyridines as Polo-like kinase 1 inhibitors. Bioorganic & Medicinal Chemistry Letters. 18: 5648-52. PMID 18793847 DOI: 10.1016/J.Bmcl.2008.08.095  0.462
2008 Hanan EJ, Fucini RV, Romanowski MJ, Elling RA, Lew W, Purkey HE, VanderPorten EC, Yang W. Design and synthesis of 2-amino-isoxazolopyridines as Polo-like kinase inhibitors. Bioorganic & Medicinal Chemistry Letters. 18: 5186-9. PMID 18790636 DOI: 10.1016/j.bmcl.2008.08.091  0.326
2006 Fahr BT, O'Brien T, Pham P, Waal ND, Baskaran S, Raimundo BC, Lam JW, Sopko MM, Purkey HE, Romanowski MJ. Tethering identifies fragment that yields potent inhibitors of human caspase-1. Bioorganic & Medicinal Chemistry Letters. 16: 559-62. PMID 16274992 DOI: 10.1016/J.Bmcl.2005.10.048  0.419
2005 O'Brien T, Fahr BT, Sopko MM, Lam JW, Waal ND, Raimundo BC, Purkey HE, Pham P, Romanowski MJ. Structural analysis of caspase-1 inhibitors derived from Tethering. Acta Crystallographica. Section F, Structural Biology and Crystallization Communications. 61: 451-8. PMID 16511067 DOI: 10.1107/S1744309105010109  0.425
2005 Petrassi HM, Johnson SM, Purkey HE, Chiang KP, Walkup T, Jiang X, Powers ET, Kelly JW. Potent and selective structure-based dibenzofuran inhibitors of transthyretin amyloidogenesis: kinetic stabilization of the native state. Journal of the American Chemical Society. 127: 6662-71. PMID 15869287 DOI: 10.1021/Ja044351F  0.751
2005 Johnson SM, Petrassi HM, Palaninathan SK, Mohamedmohaideen NN, Purkey HE, Nichols C, Chiang KP, Walkup T, Sacchettini JC, Sharpless KB, Kelly JW. Bisaryloxime ethers as potent inhibitors of transthyretin amyloid fibril formation. Journal of Medicinal Chemistry. 48: 1576-87. PMID 15743199 DOI: 10.1021/Jm049274D  0.771
2005 Razavi H, Powers ET, Purkey HE, Adamski-Werner SL, Chiang KP, Dendle MT, Kelly JW. Design, synthesis, and evaluation of oxazole transthyretin amyloidogenesis inhibitors. Bioorganic & Medicinal Chemistry Letters. 15: 1075-8. PMID 15686915 DOI: 10.1016/J.Bmcl.2004.12.022  0.698
2004 Purkey HE, Palaninathan SK, Kent KC, Smith C, Safe SH, Sacchettini JC, Kelly JW. Hydroxylated polychlorinated biphenyls selectively bind transthyretin in blood and inhibit amyloidogenesis: rationalizing rodent PCB toxicity. Chemistry & Biology. 11: 1719-28. PMID 15610856 DOI: 10.1016/J.Chembiol.2004.10.009  0.571
2003 Razavi H, Palaninathan SK, Powers ET, Wiseman RL, Purkey HE, Mohamedmohaideen NN, Deechongkit S, Chiang KP, Dendle MT, Sacchettini JC, Kelly JW. Benzoxazoles as transthyretin amyloid fibril inhibitors: synthesis, evaluation, and mechanism of action. Angewandte Chemie (International Ed. in English). 42: 2758-61. PMID 12820260 DOI: 10.1002/Anie.200351179  0.703
2002 McCammon MG, Scott DJ, Keetch CA, Greene LH, Purkey HE, Petrassi HM, Kelly JW, Robinson CV. Screening transthyretin amyloid fibril inhibitors: characterization of novel multiprotein, multiligand complexes by mass spectrometry. Structure (London, England : 1993). 10: 851-63. PMID 12057199 DOI: 10.1016/S0969-2126(02)00771-2  0.745
2001 Purkey HE, Dorrell MI, Kelly JW. Evaluating the binding selectivity of transthyretin amyloid fibril inhibitors in blood plasma. Proceedings of the National Academy of Sciences of the United States of America. 98: 5566-71. PMID 11344299 DOI: 10.1073/Pnas.091431798  0.656
2000 Kelly JW, Petrassi HM, Oza V, Purkey H, Koepf E, Raman P, Klabunde T, Sacchettini J. Structure-Based Design, Synthesis and Evaluation of Amyloid Fibril Inhibitors Biochemical Society Transactions. 28: A51-A51. DOI: 10.1042/Bst028A051  0.769
1999 Oza VB, Petrassi HM, Purkey HE, Kelly JW. Synthesis and evaluation of anthranilic acid-based transthyretin amyloid fibril inhibitors. Bioorganic & Medicinal Chemistry Letters. 9: 1-6. PMID 9990446 DOI: 10.1016/S0960-894X(98)00696-9  0.767
1998 Peterson SA, Klabunde T, Lashuel HA, Purkey H, Sacchettini JC, Kelly JW. Inhibiting transthyretin conformational changes that lead to amyloid fibril formation. Proceedings of the National Academy of Sciences of the United States of America. 95: 12956-60. PMID 9789022 DOI: 10.1073/Pnas.95.22.12956  0.686
Show low-probability matches.