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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: coghlan mp. 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.
Genetically Predicted Glucose-Dependent Insulinotropic Polypeptide (GIP) Levels and Cardiovascular Disease Risk Are Driven by Distinct Causal Variants in the GIPR Region.
Bowker N, Hansford R, Burgess S, Foley CN, Auyeung VPW, Erzurumluoglu AM, Stewart ID, Wheeler E, Pietzner M, Gribble F, Reimann F, Bhatnagar P, Coghlan MP, Wareham NJ, Langenberg C. Bowker N, et al. Among authors: coghlan mp. Diabetes. 2021 Nov;70(11):2706-2719. doi: 10.2337/db21-0103. Epub 2021 Aug 23. Diabetes. 2021. PMID: 34426508 Free PMC article.
GIPR agonism mediates weight-independent insulin sensitization by tirzepatide in obese mice.
Samms RJ, Christe ME, Collins KA, Pirro V, Droz BA, Holland AK, Friedrich JL, Wojnicki S, Konkol DL, Cosgrove R, Furber EPC, Ruan X, O'Farrell LS, Long AM, Dogra M, Willency JA, Lin Y, Ding L, Cheng CC, Cabrera O, Briere DA, Alsina-Fernandez J, Gimeno RE, Moyers JS, Coskun T, Coghlan MP, Sloop KW, Roell WC. Samms RJ, et al. Among authors: coghlan mp. J Clin Invest. 2021 Jun 15;131(12):e146353. doi: 10.1172/JCI146353. J Clin Invest. 2021. PMID: 34003802 Free PMC article.
Structural basis for GLP-1 receptor activation by LY3502970, an orally active nonpeptide agonist.
Kawai T, Sun B, Yoshino H, Feng D, Suzuki Y, Fukazawa M, Nagao S, Wainscott DB, Showalter AD, Droz BA, Kobilka TS, Coghlan MP, Willard FS, Kawabe Y, Kobilka BK, Sloop KW. Kawai T, et al. Among authors: coghlan mp. Proc Natl Acad Sci U S A. 2020 Nov 24;117(47):29959-29967. doi: 10.1073/pnas.2014879117. Epub 2020 Nov 11. Proc Natl Acad Sci U S A. 2020. PMID: 33177239 Free PMC article.
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: coghlan mp. JCI Insight. 2020 Sep 3;5(17):e140532. doi: 10.1172/jci.insight.140532. JCI Insight. 2020. PMID: 32730231 Free PMC article.
How May GIP Enhance the Therapeutic Efficacy of GLP-1?
Samms RJ, Coghlan MP, Sloop KW. Samms RJ, et al. Among authors: coghlan mp. Trends Endocrinol Metab. 2020 Jun;31(6):410-421. doi: 10.1016/j.tem.2020.02.006. Epub 2020 Mar 16. Trends Endocrinol Metab. 2020. PMID: 32396843 Free article. Review.
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