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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: hu x. 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.
A target-agnostic screen identifies approved drugs to stabilize the endoplasmic reticulum-resident proteome.
Henderson MJ, Trychta KA, Yang SM, Bäck S, Yasgar A, Wires ES, Danchik C, Yan X, Yano H, Shi L, Wu KJ, Wang AQ, Tao D, Zahoránszky-Kőhalmi G, Hu X, Xu X, Maloney D, Zakharov AV, Rai G, Urano F, Airavaara M, Gavrilova O, Jadhav A, Wang Y, Simeonov A, Harvey BK. Henderson MJ, et al. Among authors: hu x. Cell Rep. 2021 Apr 27;35(4):109040. doi: 10.1016/j.celrep.2021.109040. Cell Rep. 2021. PMID: 33910017 Free PMC article.
Structure-Based Engineering of Irreversible Inhibitors against Histone Lysine Demethylase KDM5A.
Horton JR, Woodcock CB, Chen Q, Liu X, Zhang X, Shanks J, Rai G, Mott BT, Jansen DJ, Kales SC, Henderson MJ, Cyr M, Pohida K, Hu X, Shah P, Xu X, Jadhav A, Maloney DJ, Hall MD, Simeonov A, Fu H, Vertino PM, Cheng X. Horton JR, et al. Among authors: hu x. J Med Chem. 2018 Dec 13;61(23):10588-10601. doi: 10.1021/acs.jmedchem.8b01219. Epub 2018 Nov 15. J Med Chem. 2018. PMID: 30392349 Free PMC article.
Dynamic Imaging of LDH Inhibition in Tumors Reveals Rapid In Vivo Metabolic Rewiring and Vulnerability to Combination Therapy.
Oshima N, Ishida R, Kishimoto S, Beebe K, Brender JR, Yamamoto K, Urban D, Rai G, Johnson MS, Benavides G, Squadrito GL, Crooks D, Jackson J, Joshi A, Mott BT, Shrimp JH, Moses MA, Lee MJ, Yuno A, Lee TD, Hu X, Anderson T, Kusewitt D, Hathaway HH, Jadhav A, Picard D, Trepel JB, Mitchell JB, Stott GM, Moore W, Simeonov A, Sklar LA, Norenberg JP, Linehan WM, Maloney DJ, Dang CV, Waterson AG, Hall M, Darley-Usmar VM, Krishna MC, Neckers LM. Oshima N, et al. Among authors: hu x. Cell Rep. 2020 Feb 11;30(6):1798-1810.e4. doi: 10.1016/j.celrep.2020.01.039. Cell Rep. 2020. PMID: 32049011 Free PMC article.
Insights into the Action of Inhibitor Enantiomers against Histone Lysine Demethylase 5A.
Horton JR, Liu X, Wu L, Zhang K, Shanks J, Zhang X, Rai G, Mott BT, Jansen DJ, Kales SC, Henderson MJ, Pohida K, Fang Y, Hu X, Jadhav A, Maloney DJ, Hall MD, Simeonov A, Fu H, Vertino PM, Yan Q, Cheng X. Horton JR, et al. Among authors: hu x. J Med Chem. 2018 Apr 12;61(7):3193-3208. doi: 10.1021/acs.jmedchem.8b00261. Epub 2018 Mar 23. J Med Chem. 2018. PMID: 29537847 Free PMC article.
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