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388 results

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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: evangelista m. 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
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. Among authors: evangelista m. Nat Chem Biol. 2016 Oct;12(10):779-86. doi: 10.1038/nchembio.2143. Epub 2016 Aug 1. Nat Chem Biol. 2016. PMID: 27479743
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: evangelista m. 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.
An integrated genomic screen identifies LDHB as an essential gene for triple-negative breast cancer.
McCleland ML, Adler AS, Shang Y, Hunsaker T, Truong T, Peterson D, Torres E, Li L, Haley B, Stephan JP, Belvin M, Hatzivassiliou G, Blackwood EM, Corson L, Evangelista M, Zha J, Firestein R. McCleland ML, et al. Among authors: evangelista m. Cancer Res. 2012 Nov 15;72(22):5812-23. doi: 10.1158/0008-5472.CAN-12-1098. Epub 2012 Nov 8. Cancer Res. 2012. PMID: 23139210
Metabolite profiling stratifies pancreatic ductal adenocarcinomas into subtypes with distinct sensitivities to metabolic inhibitors.
Daemen A, Peterson D, Sahu N, McCord R, Du X, Liu B, Kowanetz K, Hong R, Moffat J, Gao M, Boudreau A, Mroue R, Corson L, O'Brien T, Qing J, Sampath D, Merchant M, Yauch R, Manning G, Settleman J, Hatzivassiliou G, Evangelista M. Daemen A, et al. Among authors: evangelista m. Proc Natl Acad Sci U S A. 2015 Aug 11;112(32):E4410-7. doi: 10.1073/pnas.1501605112. Epub 2015 Jul 27. Proc Natl Acad Sci U S A. 2015. PMID: 26216984 Free PMC article.
Pan-Cancer Metabolic Signature Predicts Co-Dependency on Glutaminase and De Novo Glutathione Synthesis Linked to a High-Mesenchymal Cell State.
Daemen A, Liu B, Song K, Kwong M, Gao M, Hong R, Nannini M, Peterson D, Liederer BM, de la Cruz C, Sangaraju D, Jaochico A, Zhao X, Sandoval W, Hunsaker T, Firestein R, Latham S, Sampath D, Evangelista M, Hatzivassiliou G. Daemen A, et al. Among authors: evangelista m. Cell Metab. 2018 Sep 4;28(3):383-399.e9. doi: 10.1016/j.cmet.2018.06.003. Epub 2018 Jun 28. Cell Metab. 2018. PMID: 30043751 Free article.
Double genetic disruption of lactate dehydrogenases A and B is required to ablate the "Warburg effect" restricting tumor growth to oxidative metabolism.
Ždralević M, Brand A, Di Ianni L, Dettmer K, Reinders J, Singer K, Peter K, Schnell A, Bruss C, Decking SM, Koehl G, Felipe-Abrio B, Durivault J, Bayer P, Evangelista M, O'Brien T, Oefner PJ, Renner K, Pouysségur J, Kreutz M. Ždralević M, et al. Among authors: evangelista m. J Biol Chem. 2018 Oct 12;293(41):15947-15961. doi: 10.1074/jbc.RA118.004180. Epub 2018 Aug 29. J Biol Chem. 2018. PMID: 30158244 Free PMC article.
Combination drug scheduling defines a "window of opportunity" for chemopotentiation of gemcitabine by an orally bioavailable, selective ChK1 inhibitor, GNE-900.
Blackwood E, Epler J, Yen I, Flagella M, O'Brien T, Evangelista M, Schmidt S, Xiao Y, Choi J, Kowanetz K, Ramiscal J, Wong K, Jakubiak D, Yee S, Cain G, Gazzard L, Williams K, Halladay J, Jackson PK, Malek S. Blackwood E, et al. Among authors: evangelista m. Mol Cancer Ther. 2013 Oct;12(10):1968-80. doi: 10.1158/1535-7163.MCT-12-1218. Epub 2013 Jul 19. Mol Cancer Ther. 2013. PMID: 23873850
388 results