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Discovery of 4-(benzylaminomethylene)isoquinoline-1,3-(2H,4H)-diones and 4-[(pyridylmethyl)aminomethylene]isoquinoline-1,3-(2H,4H)-diones as potent and selective inhibitors of the cyclin-dependent kinase 4.
Tsou HR, Liu X, Birnberg G, Kaplan J, Otteng M, Tran T, Kutterer K, Tang Z, Suayan R, Zask A, Ravi M, Bretz A, Grillo M, McGinnis JP, Rabindran SK, Ayral-Kaloustian S, Mansour TS. Tsou HR, et al. Among authors: bretz a. J Med Chem. 2009 Apr 23;52(8):2289-310. doi: 10.1021/jm801026e. J Med Chem. 2009. PMID: 19317452
Discovery of trifluoromethyl(pyrimidin-2-yl)azetidine-2-carboxamides as potent, orally bioavailable TGR5 (GPBAR1) agonists: structure-activity relationships, lead optimization, and chronic in vivo efficacy.
Phillips DP, Gao W, Yang Y, Zhang G, Lerario IK, Lau TL, Jiang J, Wang X, Nguyen DG, Bhat BG, Trotter C, Sullivan H, Welzel G, Landry J, Chen Y, Joseph SB, Li C, Gordon WP, Richmond W, Johnson K, Bretz A, Bursulaya B, Pan S, McNamara P, Seidel HM. Phillips DP, et al. Among authors: bretz a. J Med Chem. 2014 Apr 24;57(8):3263-82. doi: 10.1021/jm401731q. Epub 2014 Apr 4. J Med Chem. 2014. PMID: 24666203
Discovery of Novel Quinoline-Based Proteasome Inhibitors for Human African Trypanosomiasis (HAT).
Koester DC, Marx VM, Williams S, Jiricek J, Dauphinais M, René O, Miller SL, Zhang L, Patra D, Chen YL, Cheung H, Gable J, Lakshminarayana SB, Osborne C, Galarneau JR, Kulkarni U, Richmond W, Bretz A, Xiao L, Supek F, Wiesmann C, Honnappa S, Be C, Mäser P, Kaiser M, Ritchie R, Barrett MP, Diagana TT, Sarko C, Rao SPS. Koester DC, et al. Among authors: bretz a. J Med Chem. 2022 Sep 8;65(17):11776-11787. doi: 10.1021/acs.jmedchem.2c00791. Epub 2022 Aug 22. J Med Chem. 2022. PMID: 35993839 Free PMC article.
Pradigastat disposition in humans: in vivo and in vitro investigations.
Upthagrove A, Chen J, Meyers CD, Kulmatycki K, Bretz A, Wang L, Peng L, Palamar S, Lin M, Majumdar T, Tran P, Einolf HJ. Upthagrove A, et al. Among authors: bretz a. Xenobiotica. 2017 Dec;47(12):1077-1089. doi: 10.1080/00498254.2016.1263405. Epub 2016 Dec 12. Xenobiotica. 2017. PMID: 27855567
Triglyceride Lowering with Pemafibrate to Reduce Cardiovascular Risk.
Das Pradhan A, Glynn RJ, Fruchart JC, MacFadyen JG, Zaharris ES, Everett BM, Campbell SE, Oshima R, Amarenco P, Blom DJ, Brinton EA, Eckel RH, Elam MB, Felicio JS, Ginsberg HN, Goudev A, Ishibashi S, Joseph J, Kodama T, Koenig W, Leiter LA, Lorenzatti AJ, Mankovsky B, Marx N, Nordestgaard BG, Páll D, Ray KK, Santos RD, Soran H, Susekov A, Tendera M, Yokote K, Paynter NP, Buring JE, Libby P, Ridker PM; PROMINENT Investigators. Das Pradhan A, et al. N Engl J Med. 2022 Nov 24;387(21):1923-1934. doi: 10.1056/NEJMoa2210645. Epub 2022 Nov 5. N Engl J Med. 2022. PMID: 36342113 Clinical Trial.
CRISPR-Cas9-based target validation for p53-reactivating model compounds.
Wanzel M, Vischedyk JB, Gittler MP, Gremke N, Seiz JR, Hefter M, Noack M, Savai R, Mernberger M, Charles JP, Schneikert J, Bretz AC, Nist A, Stiewe T. Wanzel M, et al. Among authors: bretz ac. Nat Chem Biol. 2016 Jan;12(1):22-8. doi: 10.1038/nchembio.1965. Epub 2015 Nov 23. Nat Chem Biol. 2016. PMID: 26595461 Free PMC article.
31 results