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Discovery and Optimization of Potent, Cell-Active Pyrazole-Based Inhibitors of Lactate Dehydrogenase (LDH).
Rai G, Brimacombe KR, Mott BT, Urban DJ, Hu X, Yang SM, Lee TD, Cheff DM, Kouznetsova J, Benavides GA, Pohida K, Kuenstner EJ, Luci DK, Lukacs CM, Davies DR, Dranow DM, Zhu H, Sulikowski G, Moore WJ, Stott GM, Flint AJ, Hall MD, Darley-Usmar VM, Neckers LM, Dang CV, Waterson AG, Simeonov A, Jadhav A, Maloney DJ. Rai G, et al. Among authors: davies dr. J Med Chem. 2017 Nov 22;60(22):9184-9204. doi: 10.1021/acs.jmedchem.7b00941. Epub 2017 Nov 9. J Med Chem. 2017. PMID: 29120638 Free PMC article.
Pyrazole-Based Lactate Dehydrogenase Inhibitors with Optimized Cell Activity and Pharmacokinetic Properties.
Rai G, Urban DJ, Mott BT, Hu X, Yang SM, Benavides GA, Johnson MS, Squadrito GL, Brimacombe KR, Lee TD, Cheff DM, Zhu H, Henderson MJ, Pohida K, Sulikowski GA, Dranow DM, Kabir M, Shah P, Padilha E, Tao D, Fang Y, Christov PP, Kim K, Jana S, Muttil P, Anderson T, Kunda NK, Hathaway HJ, Kusewitt DF, Oshima N, Cherukuri M, Davies DR, Norenberg JP, Sklar LA, Moore WJ, Dang CV, Stott GM, Neckers L, Flint AJ, Darley-Usmar VM, Simeonov A, Waterson AG, Jadhav A, Hall MD, Maloney DJ. Rai G, et al. Among authors: davies dr. J Med Chem. 2020 Oct 8;63(19):10984-11011. doi: 10.1021/acs.jmedchem.0c00916. Epub 2020 Sep 27. J Med Chem. 2020. PMID: 32902275 Free PMC article.
Optimization of ether and aniline based inhibitors of lactate dehydrogenase.
Christov PP, Kim K, Jana S, Romaine IM, Rai G, Mott BT, Allweil AA, Lamers A, Brimacombe KR, Urban DJ, Lee TD, Hu X, Lukacs CM, Davies DR, Jadhav A, Hall MD, Green N, Moore WJ, Stott GM, Flint AJ, Maloney DJ, Sulikowski GA, Waterson AG. Christov PP, et al. Among authors: davies dr. Bioorg Med Chem Lett. 2021 Jun 1;41:127974. doi: 10.1016/j.bmcl.2021.127974. Epub 2021 Mar 24. Bioorg Med Chem Lett. 2021. PMID: 33771585 Free PMC article.
Brucella melitensis Methionyl-tRNA-Synthetase (MetRS), a Potential Drug Target for Brucellosis.
Ojo KK, Ranade RM, Zhang Z, Dranow DM, Myers JB, Choi R, Nakazawa Hewitt S, Edwards TE, Davies DR, Lorimer D, Boyle SM, Barrett LK, Buckner FS, Fan E, Van Voorhis WC. Ojo KK, et al. Among authors: davies dr. PLoS One. 2016 Aug 8;11(8):e0160350. doi: 10.1371/journal.pone.0160350. eCollection 2016. PLoS One. 2016. PMID: 27500735 Free PMC article.
Discovery of 4-[(2S)-2-{[4-(4-chlorophenoxy)phenoxy]methyl}-1-pyrrolidinyl]butanoic acid (DG-051) as a novel leukotriene A4 hydrolase inhibitor of leukotriene B4 biosynthesis.
Sandanayaka V, Mamat B, Mishra RK, Winger J, Krohn M, Zhou LM, Keyvan M, Enache L, Sullins D, Onua E, Zhang J, Halldorsdottir G, Sigthorsdottir H, Thorlaksdottir A, Sigthorsson G, Thorsteinnsdottir M, Davies DR, Stewart LJ, Zembower DE, Andresson T, Kiselyov AS, Singh J, Gurney ME. Sandanayaka V, et al. Among authors: davies dr. J Med Chem. 2010 Jan 28;53(2):573-85. doi: 10.1021/jm900838g. J Med Chem. 2010. PMID: 19950900
Naegleria fowleri: Protein structures to facilitate drug discovery for the deadly, pathogenic free-living amoeba.
Tillery L, Barrett K, Goldstein J, Lassner JW, Osterhout B, Tran NL, Xu L, Young RM, Craig J, Chun I, Dranow DM, Abendroth J, Delker SL, Davies DR, Mayclin SJ, Calhoun B, Bolejack MJ, Staker B, Subramanian S, Phan I, Lorimer DD, Myler PJ, Edwards TE, Kyle DE, Rice CA, Morris JC, Leahy JW, Manetsch R, Barrett LK, Smith CL, Van Voorhis WC. Tillery L, et al. Among authors: davies dr. PLoS One. 2021 Mar 24;16(3):e0241738. doi: 10.1371/journal.pone.0241738. eCollection 2021. PLoS One. 2021. PMID: 33760815 Free PMC article.
474 results