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The Discovery, Preclinical, and Early Clinical Development of Potent and Selective GPR40 Agonists for the Treatment of Type 2 Diabetes Mellitus (LY2881835, LY2922083, and LY2922470).
Hamdouchi C, Kahl SD, Patel Lewis A, Cardona GR, Zink RW, Chen K, Eessalu TE, Ficorilli JV, Marcelo MC, Otto KA, Wilbur KL, Lineswala JP, Piper JL, Coffey DS, Sweetana SA, Haas JV, Brooks DA, Pratt EJ, Belin RM, Deeg MA, Ma X, Cannady EA, Johnson JT, Yumibe NP, Chen Q, Maiti P, Montrose-Rafizadeh C, Chen Y, Reifel Miller A. Hamdouchi C, et al. Among authors: wilbur kl. J Med Chem. 2016 Dec 22;59(24):10891-10916. doi: 10.1021/acs.jmedchem.6b00892. Epub 2016 Nov 11. J Med Chem. 2016. PMID: 27749056
Discovery of LY3104607: A Potent and Selective G Protein-Coupled Receptor 40 (GPR40) Agonist with Optimized Pharmacokinetic Properties to Support Once Daily Oral Treatment in Patients with Type 2 Diabetes Mellitus.
Hamdouchi C, Maiti P, Warshawsky AM, DeBaillie AC, Otto KA, Wilbur KL, Kahl SD, Patel Lewis A, Cardona GR, Zink RW, Chen K, Cr S, Lineswala JP, Neathery GL, Bouaichi C, Diseroad BA, Campbell AN, Sweetana SA, Adams LA, Cabrera O, Ma X, Yumibe NP, Montrose-Rafizadeh C, Chen Y, Miller AR. Hamdouchi C, et al. Among authors: wilbur kl. J Med Chem. 2018 Feb 8;61(3):934-945. doi: 10.1021/acs.jmedchem.7b01411. Epub 2018 Jan 5. J Med Chem. 2018. PMID: 29236497
Structural basis for GPR40 allosteric agonism and incretin stimulation.
Ho JD, Chau B, Rodgers L, Lu F, Wilbur KL, Otto KA, Chen Y, Song M, Riley JP, Yang HC, Reynolds NA, Kahl SD, Lewis AP, Groshong C, Madsen RE, Conners K, Lineswala JP, Gheyi T, Saflor MD, Lee MR, Benach J, Baker KA, Montrose-Rafizadeh C, Genin MJ, Miller AR, Hamdouchi C. Ho JD, et al. Among authors: wilbur kl. Nat Commun. 2018 Apr 25;9(1):1645. doi: 10.1038/s41467-017-01240-w. Nat Commun. 2018. PMID: 29695780 Free PMC article.
A peroxisome proliferator-activated receptor alpha/gamma dual agonist with a unique in vitro profile and potent glucose and lipid effects in rodent models of type 2 diabetes and dyslipidemia.
Reifel-Miller A, Otto K, Hawkins E, Barr R, Bensch WR, Bull C, Dana S, Klausing K, Martin JA, Rafaeloff-Phail R, Rafizadeh-Montrose C, Rhodes G, Robey R, Rojo I, Rungta D, Snyder D, Wilbur K, Zhang T, Zink R, Warshawsky A, Brozinick JT. Reifel-Miller A, et al. Mol Endocrinol. 2005 Jun;19(6):1593-605. doi: 10.1210/me.2005-0015. Epub 2005 Apr 14. Mol Endocrinol. 2005. PMID: 15831517