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Page 1
Structure-based optimization of hydroxylactam as potent, cell-active inhibitors of lactate dehydrogenase.
Wei B, Robarge K, Labadie SS, Chen J, Corson LB, DiPasquale A, Dragovich PS, Eigenbrot C, Evangelista M, Fauber BP, Hitz A, Hong R, Lai KW, Liu W, Ma S, Malek S, O'Brien T, Pang J, Peterson D, Salphati L, Sampath D, Sideris S, Ultsch M, Xu Z, Yen I, Yu D, Yue Q, Zhou A, Purkey HE. Wei B, et al. Among authors: corson lb. Bioorg Med Chem Lett. 2022 Mar 1;59:128576. doi: 10.1016/j.bmcl.2022.128576. Epub 2022 Jan 19. Bioorg Med Chem Lett. 2022. PMID: 35065235
Identification of substituted 2-thio-6-oxo-1,6-dihydropyrimidines as inhibitors of human lactate dehydrogenase.
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, Sideris S, Ultsch M, VanderPorten E, Wei B, Xu Q, Yen I, Yue Q, Zhang H, Zhang X. Dragovich PS, et al. Among authors: corson lb. Bioorg Med Chem Lett. 2013 Jun 1;23(11):3186-94. doi: 10.1016/j.bmcl.2013.04.001. Epub 2013 Apr 10. Bioorg Med Chem Lett. 2013. PMID: 23628333
Identification of 2-amino-5-aryl-pyrazines as inhibitors of human lactate dehydrogenase.
Fauber BP, Dragovich PS, Chen J, Corson LB, Ding CZ, Eigenbrot C, Giannetti AM, Hunsaker T, Labadie S, Liu Y, Liu Y, Malek S, Peterson D, Pitts K, Sideris S, Ultsch M, VanderPorten E, Wang J, Wei B, Yen I, Yue Q. Fauber BP, et al. Among authors: corson lb. Bioorg Med Chem Lett. 2013 Oct 15;23(20):5533-9. doi: 10.1016/j.bmcl.2013.08.060. Epub 2013 Aug 22. Bioorg Med Chem Lett. 2013. PMID: 24012183
Identification of substituted 3-hydroxy-2-mercaptocyclohex-2-enones as potent inhibitors of human lactate dehydrogenase.
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, Malek S, Peterson D, Pitts KE, Purkey HE, Robarge K, Salphati L, Sideris S, Ultsch M, VanderPorten E, Wang J, Wei B, Xu Q, Yen I, Yue Q, Zhang H, Zhang X, Zhou A. Dragovich PS, et al. Among authors: corson lb. Bioorg Med Chem Lett. 2014 Aug 15;24(16):3764-71. doi: 10.1016/j.bmcl.2014.06.076. Epub 2014 Jul 1. Bioorg Med Chem Lett. 2014. PMID: 25037916
Optimization of 5-(2,6-dichlorophenyl)-3-hydroxy-2-mercaptocyclohex-2-enones as potent inhibitors of human lactate dehydrogenase.
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, Robarge K, Salphati L, Sideris S, Ultsch M, VanderPorten E, Wei B, Xu Q, Yen I, Yue Q, Zhang H, Zhang X, Zhou A. Labadie S, et al. Among authors: corson lb. Bioorg Med Chem Lett. 2015 Jan 1;25(1):75-82. doi: 10.1016/j.bmcl.2014.11.008. Epub 2014 Nov 10. Bioorg Med Chem Lett. 2015. PMID: 25466195
Identification of 3,6-disubstituted dihydropyrones as inhibitors of human lactate dehydrogenase.
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, Yue Q, Zhou A. Fauber BP, et al. Among authors: corson lb. Bioorg Med Chem Lett. 2014 Dec 15;24(24):5683-5687. doi: 10.1016/j.bmcl.2014.10.067. Epub 2014 Oct 27. Bioorg Med Chem Lett. 2014. PMID: 25467161
Cell Active Hydroxylactam Inhibitors of Human Lactate Dehydrogenase with Oral Bioavailability in Mice.
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, Labadie SS, Lai KW, Liu W, Liu Y, Li C, Ma S, Malek S, O'Brien T, Pang J, Peterson D, Salphati L, Sideris S, Ultsch M, Wei B, Yen I, Yue Q, Zhang H, Zhou A. Purkey HE, et al. Among authors: corson lb. ACS Med Chem Lett. 2016 Aug 26;7(10):896-901. doi: 10.1021/acsmedchemlett.6b00190. eCollection 2016 Oct 13. ACS Med Chem Lett. 2016. PMID: 27774125 Free PMC article.
Metabolic plasticity underpins innate and acquired resistance to LDHA inhibition.
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, Lai T, Li Y, Chen Z, Wei B, Yen I, Sideris S, McCleland M, Firestein R, Corson L, Vanderbilt A, Williams S, Daemen A, Belvin M, Eigenbrot C, Jackson PK, Malek S, Hatzivassiliou G, Sampath D, Evangelista M, O'Brien T. Boudreau A, et al. Nat Chem Biol. 2016 Oct;12(10):779-86. doi: 10.1038/nchembio.2143. Epub 2016 Aug 1. Nat Chem Biol. 2016. PMID: 27479743
A pentacyclic aurora kinase inhibitor (AKI-001) with high in vivo potency and oral bioavailability.
Rawson TE, Rüth M, Blackwood E, Burdick D, Corson L, Dotson J, Drummond J, Fields C, Georges GJ, Goller B, Halladay J, Hunsaker T, Kleinheinz T, Krell HW, Li J, Liang J, Limberg A, McNutt A, Moffat J, Phillips G, Ran Y, Safina B, Ultsch M, Walker L, Wiesmann C, Zhang B, Zhou A, Zhu BY, Rüger P, Cochran AG. Rawson TE, et al. J Med Chem. 2008 Aug 14;51(15):4465-75. doi: 10.1021/jm800052b. Epub 2008 Jul 17. J Med Chem. 2008. PMID: 18630890
25 results