Discovery and preclinical development of AR453588 as an anti-diabetic glucokinase activator.

Autor: Hinklin RJ; Array BioPharma Inc., 3200 Walnut St., Boulder, CO 80301, United States. Electronic address: rhinklin@arraybiopharma.com., Baer BR; Array BioPharma Inc., 3200 Walnut St., Boulder, CO 80301, United States., Boyd SA; Array BioPharma Inc., 3200 Walnut St., Boulder, CO 80301, United States., Chicarelli MD; Array BioPharma Inc., 3200 Walnut St., Boulder, CO 80301, United States., Condroski KR; Array BioPharma Inc., 3200 Walnut St., Boulder, CO 80301, United States., DeWolf WE Jr; Array BioPharma Inc., 3200 Walnut St., Boulder, CO 80301, United States., Fischer J; Array BioPharma Inc., 3200 Walnut St., Boulder, CO 80301, United States., Frank M; Array BioPharma Inc., 3200 Walnut St., Boulder, CO 80301, United States., Hingorani GP; Array BioPharma Inc., 3200 Walnut St., Boulder, CO 80301, United States., Lee PA; Array BioPharma Inc., 3200 Walnut St., Boulder, CO 80301, United States., Neitzel NA; Array BioPharma Inc., 3200 Walnut St., Boulder, CO 80301, United States., Pratt SA; Array BioPharma Inc., 3200 Walnut St., Boulder, CO 80301, United States., Singh A; Array BioPharma Inc., 3200 Walnut St., Boulder, CO 80301, United States., Sullivan FX; Array BioPharma Inc., 3200 Walnut St., Boulder, CO 80301, United States., Turner T; Array BioPharma Inc., 3200 Walnut St., Boulder, CO 80301, United States., Voegtli WC; Array BioPharma Inc., 3200 Walnut St., Boulder, CO 80301, United States., Wallace EM; Array BioPharma Inc., 3200 Walnut St., Boulder, CO 80301, United States., Williams L; Array BioPharma Inc., 3200 Walnut St., Boulder, CO 80301, United States., Aicher TD; Array BioPharma Inc., 3200 Walnut St., Boulder, CO 80301, United States.

Publikováno v: Bioorganic & medicinal chemistry [Bioorg Med Chem] 2020 Jan 01; Vol. 28 (1), pp. 115232. Date of Electronic Publication: 2019 Dec 02.

Novel Series of Potent Glucokinase Activators Leading to the Discovery of AM-2394.

Autor: Dransfield PJ; Departments of Therapeutic Discovery, Metabolic Disorders, and Pharmacokinetics and Drug Metabolism, Amgen Inc. , 1120 Veterans Boulevard, South San Francisco, California 94080, United States., Pattaropong V; Departments of Therapeutic Discovery, Metabolic Disorders, and Pharmacokinetics and Drug Metabolism, Amgen Inc. , 1120 Veterans Boulevard, South San Francisco, California 94080, United States., Lai S; Departments of Therapeutic Discovery, Metabolic Disorders, and Pharmacokinetics and Drug Metabolism, Amgen Inc. , 1120 Veterans Boulevard, South San Francisco, California 94080, United States., Fu Z; Departments of Therapeutic Discovery, Metabolic Disorders, and Pharmacokinetics and Drug Metabolism, Amgen Inc. , 1120 Veterans Boulevard, South San Francisco, California 94080, United States., Kohn TJ; Departments of Therapeutic Discovery, Metabolic Disorders, and Pharmacokinetics and Drug Metabolism, Amgen Inc. , 1120 Veterans Boulevard, South San Francisco, California 94080, United States., Du X; Departments of Therapeutic Discovery, Metabolic Disorders, and Pharmacokinetics and Drug Metabolism, Amgen Inc. , 1120 Veterans Boulevard, South San Francisco, California 94080, United States., Cheng A; Departments of Therapeutic Discovery, Metabolic Disorders, and Pharmacokinetics and Drug Metabolism, Amgen Inc. , 1120 Veterans Boulevard, South San Francisco, California 94080, United States., Xiong Y; Departments of Therapeutic Discovery, Metabolic Disorders, and Pharmacokinetics and Drug Metabolism, Amgen Inc. , 1120 Veterans Boulevard, South San Francisco, California 94080, United States., Komorowski R; Departments of Metabolic Disorders, Comparative Biology and Safety Sciences and Pharmacokinetics and Drug Metabolism, Amgen Inc. , One Amgen Center Drive, Thousand Oaks, California 91320, United States., Jin L; Departments of Therapeutic Discovery, Metabolic Disorders, and Pharmacokinetics and Drug Metabolism, Amgen Inc. , 1120 Veterans Boulevard, South San Francisco, California 94080, United States., Conn M; Departments of Therapeutic Discovery, Metabolic Disorders, and Pharmacokinetics and Drug Metabolism, Amgen Inc. , 1120 Veterans Boulevard, South San Francisco, California 94080, United States., Tien E; Departments of Metabolic Disorders, Comparative Biology and Safety Sciences and Pharmacokinetics and Drug Metabolism, Amgen Inc. , One Amgen Center Drive, Thousand Oaks, California 91320, United States., DeWolf WE Jr; Array BioPharma Inc. , 3200 Walnut Street, Boulder, Colorado 80301, United States., Hinklin RJ; Array BioPharma Inc. , 3200 Walnut Street, Boulder, Colorado 80301, United States., Aicher TD; Array BioPharma Inc. , 3200 Walnut Street, Boulder, Colorado 80301, United States., Kraser CF; Array BioPharma Inc. , 3200 Walnut Street, Boulder, Colorado 80301, United States., Boyd SA; Array BioPharma Inc. , 3200 Walnut Street, Boulder, Colorado 80301, United States., Voegtli WC; Array BioPharma Inc. , 3200 Walnut Street, Boulder, Colorado 80301, United States., Condroski KR; Array BioPharma Inc. , 3200 Walnut Street, Boulder, Colorado 80301, United States., Veniant-Ellison M; Departments of Metabolic Disorders, Comparative Biology and Safety Sciences and Pharmacokinetics and Drug Metabolism, Amgen Inc. , One Amgen Center Drive, Thousand Oaks, California 91320, United States., Medina JC; Departments of Therapeutic Discovery, Metabolic Disorders, and Pharmacokinetics and Drug Metabolism, Amgen Inc. , 1120 Veterans Boulevard, South San Francisco, California 94080, United States., Houze J; Departments of Therapeutic Discovery, Metabolic Disorders, and Pharmacokinetics and Drug Metabolism, Amgen Inc. , 1120 Veterans Boulevard, South San Francisco, California 94080, United States., Coward P; Departments of Therapeutic Discovery, Metabolic Disorders, and Pharmacokinetics and Drug Metabolism, Amgen Inc. , 1120 Veterans Boulevard, South San Francisco, California 94080, United States.

Publikováno v: ACS medicinal chemistry letters [ACS Med Chem Lett] 2016 May 23; Vol. 7 (7), pp. 714-8. Date of Electronic Publication: 2016 May 23 (Print Publication: 2016).

Characterization of a novel glucokinase activator in rat and mouse models.

Autor: Lu M; Department of Medicine, University of California San Diego, La Jolla, California, United States of America., Li P; Department of Medicine, University of California San Diego, La Jolla, California, United States of America., Bandyopadhyay G; Department of Medicine, University of California San Diego, La Jolla, California, United States of America., Lagakos W; Department of Medicine, University of California San Diego, La Jolla, California, United States of America., Dewolf WE Jr; Array BioPharma Inc., Boulder, Colorado, United States of America., Alford T; Array BioPharma Inc., Boulder, Colorado, United States of America., Chicarelli MJ; Array BioPharma Inc., Boulder, Colorado, United States of America., Williams L; Array BioPharma Inc., Boulder, Colorado, United States of America., Anderson DA; Array BioPharma Inc., Boulder, Colorado, United States of America., Baer BR; Array BioPharma Inc., Boulder, Colorado, United States of America., McVean M; Array BioPharma Inc., Boulder, Colorado, United States of America., Conn M; Amgen Inc., South San Francisco, California, United States of America., Véniant MM; Amgen Inc., Thousand Oaks, California, United States of America., Coward P; Amgen Inc., South San Francisco, California, United States of America.

Publikováno v: PloS one [PLoS One] 2014 Feb 12; Vol. 9 (2), pp. e88431. Date of Electronic Publication: 2014 Feb 12 (Print Publication: 2014).

The kinetic model of the shikimate pathway as a tool to optimize enzyme assays for high-throughput screening.

Autor: Noble M; Assay Methodology Development, GlaxoSmithKline, New Frontiers Science Park, Harlow, Essex, United Kingdom., Sinha Y, Kolupaev A, Demin O, Earnshaw D, Tobin F, West J, Martin JD, Qiu C, Liu WS, DeWolf WE Jr, Tew D, Goryanin II

Publikováno v: Biotechnology and bioengineering [Biotechnol Bioeng] 2006 Nov 05; Vol. 95 (4), pp. 560-73.

Indole naphthyridinones as inhibitors of bacterial enoyl-ACP reductases FabI and FabK.

Autor: Seefeld MA; GlaxoSmithKline Pharmaceuticals, 1250 South Collegeville Road, P.O. Box 5089, Collegeville, Pennsylvania 19426, USA. Mark_A_Seefeld@gsk.com, Miller WH, Newlander KA, Burgess WJ, DeWolf WE Jr, Elkins PA, Head MS, Jakas DR, Janson CA, Keller PM, Manley PJ, Moore TD, Payne DJ, Pearson S, Polizzi BJ, Qiu X, Rittenhouse SF, Uzinskas IN, Wallis NG, Huffman WF

Publikováno v: Journal of medicinal chemistry [J Med Chem] 2003 Apr 24; Vol. 46 (9), pp. 1627-35.