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Page 1
Discovery of the First α-Amino-3-hydroxy-5-methyl-4-isoxazolepropionic Acid (AMPA) Receptor Antagonist Dependent upon Transmembrane AMPA Receptor Regulatory Protein (TARP) γ-8.
Gardinier KM, Gernert DL, Porter WJ, Reel JK, Ornstein PL, Spinazze P, Stevens FC, Hahn P, Hollinshead SP, Mayhugh D, Schkeryantz J, Khilevich A, De Frutos O, Gleason SD, Kato AS, Luffer-Atlas D, Desai PV, Swanson S, Burris KD, Ding C, Heinz BA, Need AB, Barth VN, Stephenson GA, Diseroad BA, Woods TA, Yu H, Bredt D, Witkin JM. Gardinier KM, et al. Among authors: diseroad ba. J Med Chem. 2016 May 26;59(10):4753-68. doi: 10.1021/acs.jmedchem.6b00125. Epub 2016 Apr 29. J Med Chem. 2016. PMID: 27067148
Synthesis and Pharmacological Characterization of C4β-Amide-Substituted 2-Aminobicyclo[3.1.0]hexane-2,6-dicarboxylates. Identification of (1 S,2 S,4 S,5 R,6 S)-2-Amino-4-[(3-methoxybenzoyl)amino]bicyclo[3.1.0]hexane-2,6-dicarboxylic Acid (LY2794193), a Highly Potent and Selective mGlu3 Receptor Agonist.
Monn JA, Henry SS, Massey SM, Clawson DK, Chen Q, Diseroad BA, Bhardwaj RM, Atwell S, Lu F, Wang J, Russell M, Heinz BA, Wang XS, Carter JH, Getman BG, Adragni K, Broad LM, Sanger HE, Ursu D, Catlow JT, Swanson S, Johnson BG, Shaw DB, McKinzie DL, Hao J. Monn JA, et al. Among authors: diseroad ba. J Med Chem. 2018 Mar 22;61(6):2303-2328. doi: 10.1021/acs.jmedchem.7b01481. Epub 2018 Feb 6. J Med Chem. 2018. PMID: 29350927
Synthesis and Pharmacological Characterization of 2-(2,6-Dichlorophenyl)-1-((1S,3R)-5-(3-hydroxy-3-methylbutyl)-3-(hydroxymethyl)-1-methyl-3,4-dihydroisoquinolin-2(1H)-yl)ethan-1-one (LY3154207), a Potent, Subtype Selective, and Orally Available Positive Allosteric Modulator of the Human Dopamine D1 Receptor.
Hao J, Beck JP, Schaus JM, Krushinski JH, Chen Q, Beadle CD, Vidal P, Reinhard MR, Dressman BA, Massey SM, Boulet SL, Cohen MP, Watson BM, Tupper D, Gardinier KM, Myers J, Johansson AM, Richardson J, Richards DS, Hembre EJ, Remick DM, Coates DA, Bhardwaj RM, Diseroad BA, Bender D, Stephenson G, Wolfangel CD, Diaz N, Getman BG, Wang XS, Heinz BA, Cramer JW, Zhou X, Maren DL, Falcone JF, Wright RA, Mitchell SN, Carter G, Yang CR, Bruns RF, Svensson KA. Hao J, et al. Among authors: diseroad ba. J Med Chem. 2019 Oct 10;62(19):8711-8732. doi: 10.1021/acs.jmedchem.9b01234. Epub 2019 Sep 30. J Med Chem. 2019. PMID: 31532644
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: diseroad ba. 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