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Page 1
Identification and Preclinical Pharmacology of the γ-Secretase Modulator BMS-869780.
Toyn JH, Thompson LA, Lentz KA, Meredith JE Jr, Burton CR, Sankaranararyanan S, Guss V, Hall T, Iben LG, Krause CM, Krause R, Lin XA, Pierdomenico M, Polson C, Robertson AS, Denton RR, Grace JE, Morrison J, Raybon J, Zhuo X, Snow K, Padmanabha R, Agler M, Esposito K, Harden D, Prack M, Varma S, Wong V, Zhu Y, Zvyaga T, Gerritz S, Marcin LR, Higgins MA, Shi J, Wei C, Cantone JL, Drexler DM, Macor JE, Olson RE, Ahlijanian MK, Albright CF. Toyn JH, et al. Among authors: harden d. Int J Alzheimers Dis. 2014;2014:431858. doi: 10.1155/2014/431858. Epub 2014 Jul 8. Int J Alzheimers Dis. 2014. PMID: 25097793 Free PMC article.
Discovery of a novel series of quinolone α7 nicotinic acetylcholine receptor agonists.
McDonald IM, Mate RA, Zusi FC, Huang H, Post-Munson DJ, Ferrante MA, Gallagher L, Bertekap RL Jr, Knox RJ, Robertson BJ, Harden DG, Morgan DG, Lodge NJ, Dworetzky SI, Olson RE, Macor JE. McDonald IM, et al. Bioorg Med Chem Lett. 2013 Mar 15;23(6):1684-8. doi: 10.1016/j.bmcl.2013.01.070. Epub 2013 Jan 29. Bioorg Med Chem Lett. 2013. PMID: 23414838
A Small Molecule Inhibitor Selectively Induces Apoptosis in Cells Transformed by High Risk Human Papilloma Viruses.
Sheaffer AK, Lee MS, Qi H, Chaniewski S, Zheng X, Farr GA, Esposito K, Harden D, Lei M, Schweizer L, Friborg J, Agler M, McPhee F, Gentles R, Beno BR, Chupak L, Mason S. Sheaffer AK, et al. Among authors: harden d. PLoS One. 2016 Jun 9;11(6):e0155909. doi: 10.1371/journal.pone.0155909. eCollection 2016. PLoS One. 2016. PMID: 27280728 Free PMC article.
Rapid Compound Integrity Assessment for High-Throughput Screening Hit Triaging.
Shou WZ, Gerritz SW, Harden D, Lawrence RM, Chase P, Chin J, Surti N, Lippy JS, Weller HN, Nielsen J, Weerakoon D. Shou WZ, et al. Among authors: harden d. SLAS Discov. 2021 Feb;26(2):242-247. doi: 10.1177/2472555220919097. Epub 2020 May 13. SLAS Discov. 2021. PMID: 32400264 Free article.
Fluorine substitution can block CYP3A4 metabolism-dependent inhibition: identification of (S)-N-[1-(4-fluoro-3- morpholin-4-ylphenyl)ethyl]-3- (4-fluorophenyl)acrylamide as an orally bioavailable KCNQ2 opener devoid of CYP3A4 metabolism-dependent inhibition.
Wu YJ, Davis CD, Dworetzky S, Fitzpatrick WC, Harden D, He H, Knox RJ, Newton AE, Philip T, Polson C, Sivarao DV, Sun LQ, Tertyshnikova S, Weaver D, Yeola S, Zoeckler M, Sinz MW. Wu YJ, et al. Among authors: harden d. J Med Chem. 2003 Aug 28;46(18):3778-81. doi: 10.1021/jm034111v. J Med Chem. 2003. PMID: 12930139
Screening Hit to Clinical Candidate: Discovery of BMS-963272, a Potent, Selective MGAT2 Inhibitor for the Treatment of Metabolic Disorders.
Turdi H, Chao H, Hangeland JJ, Ahmad S, Meng W, Brigance R, Zhao G, Wang W, Moore F, Ye XY, Mathur A, Hou X, Kempson J, Wu DR, Li YX, Azzara AV, Ma Z, Chu CH, Chen L, Cullen MJ, Rooney S, Harvey S, Kopcho L, Panemangelor R, Abell L, O'Malley K, Keim WJ, Dierks E, Chang S, Foster K, Apedo A, Harden D, Dabros M, Gao Q, Pelleymounter MA, Whaley JM, Robl JA, Cheng D, Lawrence RM, Devasthale P. Turdi H, et al. Among authors: harden d. J Med Chem. 2021 Oct 14;64(19):14773-14792. doi: 10.1021/acs.jmedchem.1c01356. Epub 2021 Oct 6. J Med Chem. 2021. PMID: 34613725
Blockade of protease-activated receptor-4 (PAR4) provides robust antithrombotic activity with low bleeding.
Wong PC, Seiffert D, Bird JE, Watson CA, Bostwick JS, Giancarli M, Allegretto N, Hua J, Harden D, Guay J, Callejo M, Miller MM, Lawrence RM, Banville J, Guy J, Maxwell BD, Priestley ES, Marinier A, Wexler RR, Bouvier M, Gordon DA, Schumacher WA, Yang J. Wong PC, et al. Among authors: harden d. Sci Transl Med. 2017 Jan 4;9(371):eaaf5294. doi: 10.1126/scitranslmed.aaf5294. Sci Transl Med. 2017. PMID: 28053157
56 results