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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 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
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.
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.
Synthetic protease-activated class B GPCRs.
Willard FS, Meredith TD, Showalter AD, Ma W, Ho JD, Sauder JM, Sloop KW. Willard FS, et al. Among authors: showalter ad. Biochem Biophys Res Commun. 2020 Sep 10;530(1):246-251. doi: 10.1016/j.bbrc.2020.07.021. Epub 2020 Aug 5. Biochem Biophys Res Commun. 2020. PMID: 32828294
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: showalter ad. 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
28 results