recent publications
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academic article
- 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
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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
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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
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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
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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
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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
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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
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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
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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
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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