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The pharmacological basis for nonpeptide agonism of the GLP-1 receptor by orforglipron.
Sloop KW, Cox AL, Wainscott DB, White A, Droz BA, Stutsman C, Showalter AD, Suter TM, Dunbar JD, Snider BM, O'Farrell LS, Hewitt N, Ruble JC, Padgett LR, Woerly EM, Peterson JA, Coskun T, Liu Z, Coutant DE, Ai M, Emmerson PJ, Sangwung P, Willard FS. Sloop KW, et al. Among authors: emmerson pj. Sci Transl Med. 2024 Dec 18;16(778):eadp5765. doi: 10.1126/scitranslmed.adp5765. Epub 2024 Dec 18. Sci Transl Med. 2024. PMID: 39693407
Tirzepatide is an imbalanced and biased dual GIP and GLP-1 receptor agonist.
Willard FS, Douros JD, Gabe MB, Showalter AD, Wainscott DB, Suter TM, Capozzi ME, van der Velden WJ, Stutsman C, Cardona GR, Urva S, Emmerson PJ, Holst JJ, D'Alessio DA, Coghlan MP, Rosenkilde MM, Campbell JE, Sloop KW. Willard FS, et al. Among authors: emmerson pj. JCI Insight. 2020 Sep 3;5(17):e140532. doi: 10.1172/jci.insight.140532. JCI Insight. 2020. PMID: 32730231 Free PMC article.
Structural determinants of dual incretin receptor agonism by tirzepatide.
Sun B, Willard FS, Feng D, Alsina-Fernandez J, Chen Q, Vieth M, Ho JD, Showalter AD, Stutsman C, Ding L, Suter TM, Dunbar JD, Carpenter JW, Mohammed FA, Aihara E, Brown RA, Bueno AB, Emmerson PJ, Moyers JS, Kobilka TS, Coghlan MP, Kobilka BK, Sloop KW. Sun B, et al. Among authors: emmerson pj. Proc Natl Acad Sci U S A. 2022 Mar 29;119(13):e2116506119. doi: 10.1073/pnas.2116506119. Epub 2022 Mar 25. Proc Natl Acad Sci U S A. 2022. PMID: 35333651 Free PMC article.
Anorectic and aversive effects of GLP-1 receptor agonism are mediated by brainstem cholecystokinin neurons, and modulated by GIP receptor activation.
Costa A, Ai M, Nunn N, Culotta I, Hunter J, Boudjadja MB, Valencia-Torres L, Aviello G, Hodson DJ, Snider BM, Coskun T, Emmerson PJ, Luckman SM, D'Agostino G. Costa A, et al. Among authors: emmerson pj. Mol Metab. 2022 Jan;55:101407. doi: 10.1016/j.molmet.2021.101407. Epub 2021 Nov 26. Mol Metab. 2022. PMID: 34844019 Free PMC article.
GIPR Agonism Inhibits PYY-Induced Nausea-Like Behavior.
Samms RJ, Cosgrove R, Snider BM, Furber EC, Droz BA, Briere DA, Dunbar J, Dogra M, Alsina-Fernandez J, Borner T, De Jonghe BC, Hayes MR, Coskun T, Sloop KW, Emmerson PJ, Ai M. Samms RJ, et al. Among authors: emmerson pj. Diabetes. 2022 Jul 1;71(7):1410-1423. doi: 10.2337/db21-0848. Diabetes. 2022. PMID: 35499381 Free PMC article.
44 results