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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: neckers lm. 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.
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: neckers lm. 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.
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: neckers lm. 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.
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. 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.
Inhibition of NAD+-Dependent Metabolic Processes Induces Cellular Necrosis and Tumor Regression in Rhabdomyosarcoma Models.
McKay-Corkum GB, Collins VJ, Yeung C, Ito T, Issaq SH, Holland D, Vulikh K, Zhang Y, Lee U, Lei H, Mendoza A, Shern JF, Yohe ME, Yamamoto K, Wilson K, Ji J, Karim BO, Thomas CJ, Krishna MC, Neckers LM, Heske CM. McKay-Corkum GB, et al. Among authors: neckers lm. Clin Cancer Res. 2023 Nov 1;29(21):4479-4491. doi: 10.1158/1078-0432.CCR-23-0200. Clin Cancer Res. 2023. PMID: 37616468 Free PMC article.
Pseudohypoxic pathways in renal cell carcinoma.
Bratslavsky G, Sudarshan S, Neckers L, Linehan WM. Bratslavsky G, et al. Clin Cancer Res. 2007 Aug 15;13(16):4667-71. doi: 10.1158/1078-0432.CCR-06-2510. Clin Cancer Res. 2007. PMID: 17699843 Review.
254 results