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Substituted 3-imidazo[1,2-a]pyridin-3-yl- 4-(1,2,3,4-tetrahydro-[1,4]diazepino-[6,7,1-hi]indol-7-yl)pyrrole-2,5-diones as highly selective and potent inhibitors of glycogen synthase kinase-3.
Engler TA, Henry JR, Malhotra S, Cunningham B, Furness K, Brozinick J, Burkholder TP, Clay MP, Clayton J, Diefenbacher C, Hawkins E, Iversen PW, Li Y, Lindstrom TD, Marquart AL, McLean J, Mendel D, Misener E, Briere D, O'Toole JC, Porter WJ, Queener S, Reel JK, Owens RA, Brier RA, Eessalu TE, Wagner JR, Campbell RM, Vaughn R. Engler TA, et al. Among authors: briere d. J Med Chem. 2004 Jul 29;47(16):3934-7. doi: 10.1021/jm049768a. J Med Chem. 2004. PMID: 15267232
The development of potent and selective bisarylmaleimide GSK3 inhibitors.
Engler TA, Malhotra S, Burkholder TP, Henry JR, Mendel D, Porter WJ, Furness K, Diefenbacher C, Marquart A, Reel JK, Li Y, Clayton J, Cunningham B, McLean J, O'toole JC, Brozinick J, Hawkins E, Misener E, Briere D, Brier RA, Wagner JR, Campbell RM, Anderson BD, Vaughn R, Bennett DB, Meier TI, Cook JA. Engler TA, et al. Among authors: briere d. Bioorg Med Chem Lett. 2005 Feb 15;15(4):899-903. doi: 10.1016/j.bmcl.2004.12.063. Bioorg Med Chem Lett. 2005. PMID: 15686883
2-Alkoxydihydrocinnamates as PPAR agonists. Activity modulation by the incorporation of phenoxy substituents.
Martín JA, Brooks DA, Prieto L, González R, Torrado A, Rojo I, López de Uralde B, Lamas C, Ferritto R, Dolores Martín-Ortega M, Agejas J, Parra F, Rizzo JR, Rhodes GA, Robey RL, Alt CA, Wendel SR, Zhang TY, Reifel-Miller A, Montrose-Rafizadeh C, Brozinick JT, Hawkins E, Misener EA, Briere DA, Ardecky R, Fraser JD, Warshawsky AM. Martín JA, et al. Among authors: briere da. Bioorg Med Chem Lett. 2005 Jan 3;15(1):51-5. doi: 10.1016/j.bmcl.2004.10.042. Bioorg Med Chem Lett. 2005. PMID: 15582409
Discovery of an Orally Efficacious Positive Allosteric Modulator of the Glucagon-like Peptide-1 Receptor.
Willard FS, Wainscott DB, Showalter AD, Stutsman C, Ma W, Cardona GR, Zink RW, Corkins CM, Chen Q, Yumibe N, Agejas J, Cumming GR, Minguez JM, Jiménez A, Mateo AI, Castaño AM, Briere DA, Sloop KW, Bueno AB. Willard FS, et al. Among authors: briere da. J Med Chem. 2021 Mar 25;64(6):3439-3448. doi: 10.1021/acs.jmedchem.1c00029. Epub 2021 Mar 15. J Med Chem. 2021. PMID: 33721487
The novel dual glucose-dependent insulinotropic polypeptide and glucagon-like peptide-1 (GLP-1) receptor agonist tirzepatide transiently delays gastric emptying similarly to selective long-acting GLP-1 receptor agonists.
Urva S, Coskun T, Loghin C, Cui X, Beebe E, O'Farrell L, Briere DA, Benson C, Nauck MA, Haupt A. Urva S, et al. Diabetes Obes Metab. 2020 Oct;22(10):1886-1891. doi: 10.1111/dom.14110. Epub 2020 Jul 13. Diabetes Obes Metab. 2020. PMID: 32519795 Free PMC article.
LY3298176, a novel dual GIP and GLP-1 receptor agonist for the treatment of type 2 diabetes mellitus: From discovery to clinical proof of concept.
Coskun T, Sloop KW, Loghin C, Alsina-Fernandez J, Urva S, Bokvist KB, Cui X, Briere DA, Cabrera O, Roell WC, Kuchibhotla U, Moyers JS, Benson CT, Gimeno RE, D'Alessio DA, Haupt A. Coskun T, et al. Among authors: d alessio da, briere da. Mol Metab. 2018 Dec;18:3-14. doi: 10.1016/j.molmet.2018.09.009. Epub 2018 Oct 3. Mol Metab. 2018. PMID: 30473097 Free PMC article. Clinical Trial.
37 results