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Page 1
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: urban dj. 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.
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: urban d. 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.
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: urban dj. 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.
Discovery and lead identification of quinazoline-based BRD4 inhibitors.
Yang SM, Urban DJ, Yoshioka M, Strovel JW, Fletcher S, Wang AQ, Xu X, Shah P, Hu X, Hall MD, Jadhav A, Maloney DJ. Yang SM, et al. Among authors: urban dj. Bioorg Med Chem Lett. 2018 Nov 15;28(21):3483-3488. doi: 10.1016/j.bmcl.2018.08.039. Epub 2018 Aug 31. Bioorg Med Chem Lett. 2018. PMID: 30268702 Free PMC article.
Targeting Glycolysis through Inhibition of Lactate Dehydrogenase Impairs Tumor Growth in Preclinical Models of Ewing Sarcoma.
Yeung C, Gibson AE, Issaq SH, Oshima N, Baumgart JT, Edessa LD, Rai G, Urban DJ, Johnson MS, Benavides GA, Squadrito GL, Yohe ME, Lei H, Eldridge S, Hamre J 3rd, Dowdy T, Ruiz-Rodado V, Lita A, Mendoza A, Shern JF, Larion M, Helman LJ, Stott GM, Krishna MC, Hall MD, Darley-Usmar V, Neckers LM, Heske CM. Yeung C, et al. Among authors: urban dj. Cancer Res. 2019 Oct 1;79(19):5060-5073. doi: 10.1158/0008-5472.CAN-19-0217. Epub 2019 Aug 20. Cancer Res. 2019. PMID: 31431459 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: urban dj. 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.
Discovery and Optimization of 2H-1λ2-Pyridin-2-one Inhibitors of Mutant Isocitrate Dehydrogenase 1 for the Treatment of Cancer.
Rohde JM, Karavadhi S, Pragani R, Liu L, Fang Y, Zhang W, McIver A, Zheng H, Liu Q, Davis MI, Urban DJ, Lee TD, Cheff DM, Hollingshead M, Henderson MJ, Martinez NJ, Brimacombe KR, Yasgar A, Zhao W, Klumpp-Thomas C, Michael S, Covey J, Moore WJ, Stott GM, Li Z, Simeonov A, Jadhav A, Frye S, Hall MD, Shen M, Wang X, Patnaik S, Boxer MB. Rohde JM, et al. Among authors: urban dj. J Med Chem. 2021 Apr 22;64(8):4913-4946. doi: 10.1021/acs.jmedchem.1c00019. Epub 2021 Apr 6. J Med Chem. 2021. PMID: 33822623 Free PMC article.
Structural Basis for KDM5A Histone Lysine Demethylase Inhibition by Diverse Compounds.
Horton JR, Liu X, Gale M, Wu L, Shanks JR, Zhang X, Webber PJ, Bell JSK, Kales SC, Mott BT, Rai G, Jansen DJ, Henderson MJ, Urban DJ, Hall MD, Simeonov A, Maloney DJ, Johns MA, Fu H, Jadhav A, Vertino PM, Yan Q, Cheng X. Horton JR, et al. Among authors: urban dj. Cell Chem Biol. 2016 Jul 21;23(7):769-781. doi: 10.1016/j.chembiol.2016.06.006. Epub 2016 Jul 14. Cell Chem Biol. 2016. PMID: 27427228 Free PMC article.
Assessing inhibitors of mutant isocitrate dehydrogenase using a suite of pre-clinical discovery assays.
Urban DJ, Martinez NJ, Davis MI, Brimacombe KR, Cheff DM, Lee TD, Henderson MJ, Titus SA, Pragani R, Rohde JM, Liu L, Fang Y, Karavadhi S, Shah P, Lee OW, Wang A, McIver A, Zheng H, Wang X, Xu X, Jadhav A, Simeonov A, Shen M, Boxer MB, Hall MD. Urban DJ, et al. Sci Rep. 2017 Oct 6;7(1):12758. doi: 10.1038/s41598-017-12630-x. Sci Rep. 2017. PMID: 28986582 Free PMC article.
46 results