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Purkey, Hans

Graduate Student

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Positions

• 2016 - Senior Scientist, Genentech

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• Doctoral Dissertation

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  • Bronner, S. M., Merrick, K. A., Murray, J., Salphati, L., Moffat, J. G., Pang, J., Sneeringer, C. J., Dompe, N., Cyr, P., Purkey, H., Boenig, G. D., Li, J., et al. Design of a brain-penetrant CDK4/6 inhibitor for glioblastoma Bioorganic & Medicinal Chemistry Letters  2019 29:2294-2301  DOI:10.1016/j.bmcl.2019.06.021  PMID:31307887
  • Ladi, E., Everett, C., Stivala, C. E., Daniels, B. E., Durk, M. R., Harris, S. F., Huestis, M. P., Purkey, H. E., Staben, S. T., Augustin, M., Blaesse, M., Steinbacher, S., et al. Design and evaluation of highly selective human immunoproteasome inhibitors reveal a compensatory process that preserves immune cell viability Journal of Medicinal Chemistry  2019 62:7032-7041  DOI:10.1021/acs.jmedchem.9b00509  PMID:31283222
  • Alexander, M. K., Miu, A., Oh, A., Reichelt, M., Ho, H., Chalouni, C., Labadie, S., Wang, L., Liang, J., Nickerson, N. N., Hu, H., Yu, L., et al. Disrupting gram-negative bacterial outer membrane biosynthesis through inhibition of the lipopolysaccharide transporter MsbA Antimicrobial Agents and Chemotherapy  2018 62:e01142-18  DOI:10.1128/aac.01142-18  PMID:30104274  PMCID:PMC6201111
  • Ho, H., Miu, A., Alexander, M. K., Garcia, N. K., Oh, A., Zilberleyb, I., Reichelt, M., Austin, C. D., Tam, C., Shriver, S., Hu, H., Labadie, S. S., et al. Structural basis for dual-mode inhibition of the ABC transporter MsbA Nature  2018 557:196-201  DOI:10.1038/s41586-018-0083-5  PMID:29720648
  • Chan, B. K., Hanan, E. J., Bowman, K. K., Bryan, M. C., Burdick, D., Chan, E., Chen, Y., Clausen, S., Dela Vega, T., Dotson, J., Eigenbrot, C., Elliott, R. L., et al. Discovery of a noncovalent, mutant-selective epidermal growth factor receptor inhibitor Journal of Medicinal Chemistry  2016 59:9080-9093  DOI:10.1021/acs.jmedchem.6b00995  PMID:27564586
  • Purkey, H. E., Robarge, K., Chen, J., Chen, Z., Corson, L. B., Ding, C. Z., DiPasquale, A. G., Dragovich, P. S., Eigenbrot, C., Evangelista, M., Fauber, B. P., Gao, Z., et al. Cell active hydroxylactam inhibitors of human lactate dehydrogenase with oral bioavailability in mice ACS Medicinal Chemistry Letters  2016 7:896-901  DOI:10.1021/acsmedchemlett.6b00190  PMID:27774125  PMCID:PMC5066143
  • Boudreau, A., Purkey, H. E., Hitz, A., Robarge, K., Peterson, D., Labadie, S., Kwong, M., Hong, R., Gao, M., Del Nagro, C., Pusapati, R., Ma, S., et al. Metabolic plasticity underpins innate and acquired resistance to LDHA inhibition Nature Chemical Biology  2016 12:779-786  DOI:10.1038/nchembio.2143  PMID:27479743
  • Hanan, E. J., Baumgardner, M., Bryan, M. C., Chen, Y., Eigenbrot, C., Fan, P., Gu, X. H., La, H., Malek, S., Purkey, H. E., Schaefer, G., Schmidt, S., 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  2016 26:534-539  DOI:10.1016/j.bmcl.2015.11.078  PMID:26639762
  • Bryan, M. C., Burdick, D. J., Chan, B. K., Chen, Y., Clausen, S., Dotson, J., Eigenbrot, C., Elliott, R., Hanan, E. J., Heald, R., Jackson, P., La, H., et al. Pyridones as highly selective, noncovalent inhibitors of T790M double mutants of EGFR ACS Medicinal Chemistry Letters  2016 7:100-104  DOI:10.1021/acsmedchemlett.5b00428  PMID:26819674  PMCID:PMC4716594
  • Heald, R., Bowman, K. K., Bryan, M. C., Burdick, D., Chan, B., Chan, E., Chen, Y., Clausen, S., Dominguez-Fernandez, B., Eigenbrot, C., Elliott, R., Hanan, E. J., et al. Noncovalent mutant selective epidermal growth factor receptor inhibitors: a lead optimization case study Journal of Medicinal Chemistry  2015 58:8877-8895  DOI:10.1021/acs.jmedchem.5b01412
  • Labadie, S., Dragovich, P. S., Chen, J., Fauber, B. P., Boggs, J., Corson, L. B., Ding, C. Z., Eigenbrot, C., Ge, H., Ho, Q., Lai, K. W., Ma, S., 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  2015 25:75-82  DOI:10.1016/j.bmcl.2014.11.008  PMID:25466195
  • Fauber, B. P., Dragovich, P. S., Chen, J., Corson, L. B., Ding, C. Z., Eigenbrot, C., Labadie, S., Malek, S., Peterson, D., Purkey, H. E., Robarge, K., Sideris, S., et al. Identification of 3,6-disubstituted dihydropyrones as inhibitors of human lactate dehydrogenase Bioorganic & Medicinal Chemistry Letters  2014 24:5683-5687  DOI:10.1016/j.bmcl.2014.10.067  PMID:25467161
  • Thomas, A. A., Hunt, K. W., Newhouse, B., Watts, R. J., Liu, X., Vigers, G., Smith, D., Rhodes, S. P., Brown, K. D., Otten, J. N., Burkard, M., Cox, A. A., et al. 8-Tetrahydropyran-2-yl chromans: highly selective beta-site amyloid precursor protein cleaving enzyme 1 (BACE1) inhibitors Journal of Medicinal Chemistry  2014 57:10112-10129  DOI:10.1021/jm5015132  PMID:25411915
  • Hanan, E. J., Eigenbrot, C., Bryan, M. C., Burdick, D. J., Chan, B. K., Chen, Y., Dotson, J., Heald, R. A., Jackson, P. S., La, H., Lainchbury, M. D., Malek, 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  2014 57:10176-10191  DOI:10.1021/jm501578n  PMID:25383627  PMCID:PMC4266342
  • Tao, Z. F., Hasvold, L., Wang, L., Wang, X., Petros, A. M., Park, C. H., Boghaert, E. R., Catron, N. D., Chen, J., Colman, P. M., Czabotar, P. E., Deshayes, K., et al. Discovery of a potent and selective BCL-X-L inhibitor with in vivo activity ACS Medicinal Chemistry Letters  2014 5:1088-1093  DOI:10.1021/ml5001867  PMID:25313317
  • Dragovich, P. S., Fauber, B. P., Boggs, J., Chen, J., Corson, L. B., Ding, C. Z., Eigenbrot, C., Ge, H., Giannetti, A. M., Hunsaker, T., Labadie, S., Li, C., et al. Identification of substituted 3-hydroxy-2-mercaptocyclohex-2-enones as potent inhibitors of human lactate dehydrogenase Bioorganic & Medicinal Chemistry Letters  2014 24:3764-3771  DOI:10.1016/j.bmcl.2014.06.076  PMID:25037916
  • Volgraf, M., Chan, L., Huestis, M. P., Purkey, H. E., Burkard, M., Do, M. G., Harris, J., Hunt, K. W., Liu, X., Lyssikatos, J. P., Rana, S., Thomas, A. A., et al. Synthesis, characterization, and PK/PD studies of a series of spirocyclic pyranochromene BACE1 inhibitors Bioorganic & Medicinal Chemistry Letters  2014 24:2477-2480  DOI:10.1016/j.bmcl.2014.04.012  PMID:24780121
  • Thomas, A. A., Hunt, K. W., Volgraf, M., Watts, R. J., Liu, X., Vigers, G., Smith, D., Sammond, D., Tang, T. P., Rhodes, S. P., Metcalf, A. T., Brown, K. D., 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  2014 57:878-902  DOI:10.1021/jm401635n  PMID:24397738
  • Huestis, M. P., Liu, W., Volgraf, M., Purkey, H. E., Yu, C., Wang, W. R., Smith, D., Vigers, G., Dutcher, D., Hunt, K. W., Siu, M. Diethylaminosulfur trifluoride-mediated intramolecular cyclization of 2-hydroxycycloalkylureas to fused bicyclic aminooxazoline compounds and evaluation of their biochemical activity against beta-secretase-1 (BACE-1) Tetrahedron Letters  2013 54:5802-5807  DOI:10.1016/j.tetlet.2013.07.136
  • Dragovich, P. S., Fauber, B. P., Corson, L. B., Ding, C. Z., Eigenbrot, C., Ge, H., Giannetti, A. M., Hunsaker, T., Labadie, S., Liu, Y., Malek, S., Pan, B., et al. Identification of substituted 2-thio-6-oxo-1,6-dihydropyrimidines as inhibitors of human lactate dehydrogenase Bioorganic & Medicinal Chemistry Letters  2013 23:3186-3194  DOI:10.1016/j.bmcl.2013.04.001  PMID:23628333
  • Hunt, K. W., Cook, A. W., Watts, R. J., Clark, C. T., Vigers, G., Smith, D., Metcalf, A. T., Gunawardana, I. W., Burkard, M., Cox, A. A., Do, M. K. G., Dutcher, D., 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  2013 56:3379-3403  DOI:10.1021/jm4002154  PMID:23537249
  • Long, D. D., Frieman, B., Hegde, S. S., Hill, C. M., Jiang, L., Kintz, S., Marquess, D. G., Purkey, H., Shaw, J. P., Steinfeld, T., Wilson, M. S., 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  2013 23:939-943  DOI:10.1016/j.bmcl.2012.12.058  PMID:23317571
  • Ameriks, M. K., Bembenek, S. D., Burdett, M. T., Choong, I. C., Edwards, J. P., Gebauer, D., Gu, Y., Karlsson, L., Purkey, H. E., Staker, B. L., Sun, S., Thurmond, R. L., et al. Diazinones as P2 replacements for pyrazole-based cathepsin S inhibitors Bioorganic & Medicinal Chemistry Letters  2010 20:4060-4064  DOI:10.1016/j.bmcl.2010.05.086  PMID:20541404
  • Fucini, R. V., Hanan, E. J., Romanowski, M. J., Elling, R. A., Lew, W., Barr, K. J., Zhu, J., Yoburn, J. C., Liu, Y., Fahr, B. T., Fan, J., Lu, Y., et al. Design and synthesis of 2-amino-pyrazolopyridines as Polo-like kinase 1 inhibitors Bioorganic & Medicinal Chemistry Letters  2008 18:5648-5652  DOI:10.1016/j.bmcl.2008.08.095  PMID:18793847
  • Hanan, E. J., Fucini, R. V., Romanowski, M. J., Elling, R. A., Lew, W., Purkey, H. E., VanderPorten, E. C., Yang, W. Design and synthesis of 2-amino-isoxazolopyridines as Polo-like kinase inhibitors Bioorganic & Medicinal Chemistry Letters  2008 18:5186-5189  DOI:10.1016/j.bmcl.2008.08.091  PMID:18790636
  • Fahr, B. T., O'Brien, T., Pham, P., Waal, N. D., Baskaran, S., Raimundo, B. C., Lam, J. W., Sopko, M. M., Purkey, H. E., Romanowski, M. J. Tethering identifies fragment that yields potent inhibitors of human caspase-1 Bioorganic & Medicinal Chemistry Letters  2006 16:559-562  DOI:10.1016/j.bmcl.2005.10.048  PMID:16274992
  • Petrassi, H. M., Johnson, S. M., Purkey, H. E., Chiang, K. P., Walkup, T., Jiang, X., Powers, E. T., Kelly, J. W. Potent and selective structure-based dibenzofuran inhibitors of transthyretin amyloidogenesis: Kinetic stabilization of the native state Journal of the American Chemical Society  2005 127:6662-6671  DOI:10.1021/ja044351f  PMID:15869287
  • O'Brien, T., Fahr, B. T., Sopko, M. M., Lam, J. W., Waal, N. D., Raimundo, B. C., Purkey, H. E., Pham, P., Romanowski, M. J. Structural analysis of caspase-1 inhibitors derived from Tethering Acta Crystallographica Section F-Structural Biology and Crystallization Communications  2005 61:451-458  DOI:10.1107/s1744309105010109  PMID:16511067  PMCID:PMC1952309
  • Johnson, S. M., Petrassi, H. M., Palaninathan, S. K., Mohamedmohaideen, N. N., Purkey, H. E., Nichols, C., Chiang, K. P., Walkup, T., Sacchettini, J. C., Sharpless, K. B., Kelly, J. W. Bisaryloxime ethers as potent inhibitors of transthyretin amyloid fibril formation Journal of Medicinal Chemistry  2005 48:1576-1587  DOI:10.1021/jm049274d  PMID:15743199
  • Razavi, H., Powers, E. T., Purkey, H. E., Adamski-Werner, S. L., Chiang, K. P., Dendle, M. T. A., Kelly, J. W. Design, synthesis, and evaluation of oxazole transthyretin amyloidogenesis inhibitors Bioorganic & Medicinal Chemistry Letters  2005 15:1075-1078  DOI:10.1016/j.bmcl.2004.12.022  PMID:15686915
  • Purkey, H. E., Palaninathan, S. K., Kent, K. C., Smith, C., Safe, S. H., Sacchettini, J. C., Kelly, J. W. Hydroxylated polychlorinated biphenyls selectively bind transthyretin in blood and inhibit amyloidogenesis: rationalizing rodent PCB toxicity Chemistry & Biology  2004 11:1719-1728  DOI:10.1016/j.chembiol.2004.10.009  PMID:15610856
  • Razavi, H., Palaninathan, S. K., Powers, E. T., Wiseman, R. L., Purkey, H. E., Mohamedmohaideen, N. N., Deechongkit, S., Chiang, K. P., Dendle, M. T. A., Sacchettini, J. C., Kelly, J. W. Benzoxazoles as transthyretin amyloid fibril inhibitors: Synthesis, evaluation, and mechanism of action Angewandte Chemie-International Edition  2003 42:2758-2761  DOI:10.1002/anie.200351179  PMID:12820260
  • McCammon, M. G., Scott, D. J., Keetch, C. A., Greene, L. H., Purkey, H. E., Petrassi, H. M., Kelly, J. W., Robinson, C. V. Screening transthyretin amyloid fibril inhibitors: Characterization of novel multiprotein, multiligand complexes by mass spectrometry Structure  2002 10:851-863  DOI:10.1016/s0969-2126(02)00771-2  PMID:12057199
  • Purkey, H. E., Dorrell, M. I., Kelly, J. W. 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  2001 98:5566-5571  DOI:10.1073/pnas.091431798  PMID:11344299  PMCID:PMC33253
  • Oza, V. B., Petrassi, H. M., Purkey, H. E., Kelly, J. W. Synthesis and evaluation of anthranilic acid-based transthyretin amyloid fibril inhibitors Bioorganic & Medicinal Chemistry Letters  1999 9:1-6  DOI:10.1016/s0960-894x(98)00696-9  PMID:9990446
  • Peterson, S. A., Klabunde, T., Lashuel, H. A., Purkey, H., Sacchettini, J. C., Kelly, J. W. Inhibiting transthyretin conformational changes that lead to amyloid fibril formation Proceedings of the National Academy of Sciences of the United States of America  1998 95:12956-12960  DOI:10.1073/pnas.95.22.12956  PMID:9789022

Background

education and training

• Ph.D. in Biology, Scripps Research 1996 - 2002
• B.S. in Chemistry, Harvey Mudd College 1992 - 1996

advisee of

• graduate advising relationship

  • Kelly, Jeffery, Ph.D.  candidacy, 1997 - 2002

Contact

full name

• Hans Edward Purkey

geographic location

• Scripps California