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Page 1
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: showalter ad. Sci Transl Med. 2024 Dec 18;16(778):eadp5765. doi: 10.1126/scitranslmed.adp5765. Epub 2024 Dec 18. Sci Transl Med. 2024. PMID: 39693407
Structural insights into probe-dependent positive allosterism of the GLP-1 receptor.
Bueno AB, Sun B, Willard FS, Feng D, Ho JD, Wainscott DB, Showalter AD, Vieth M, Chen Q, Stutsman C, Chau B, Ficorilli J, Agejas FJ, Cumming GR, Jiménez A, Rojo I, Kobilka TS, Kobilka BK, Sloop KW. Bueno AB, et al. Among authors: showalter ad. Nat Chem Biol. 2020 Oct;16(10):1105-1110. doi: 10.1038/s41589-020-0589-7. Epub 2020 Jul 20. Nat Chem Biol. 2020. PMID: 32690941
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: showalter ad. JCI Insight. 2020 Sep 3;5(17):e140532. doi: 10.1172/jci.insight.140532. JCI Insight. 2020. PMID: 32730231 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: showalter ad. 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.
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: showalter ad. 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.
Progesterone receptor membrane component 1 is a functional part of the glucagon-like peptide-1 (GLP-1) receptor complex in pancreatic β cells.
Zhang M, Robitaille M, Showalter AD, Huang X, Liu Y, Bhattacharjee A, Willard FS, Han J, Froese S, Wei L, Gaisano HY, Angers S, Sloop KW, Dai FF, Wheeler MB. Zhang M, et al. Among authors: showalter ad. Mol Cell Proteomics. 2014 Nov;13(11):3049-62. doi: 10.1074/mcp.M114.040196. Epub 2014 Jul 20. Mol Cell Proteomics. 2014. PMID: 25044020 Free PMC article.
29 results