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Page 1
LY3437943, a novel triple glucagon, GIP, and GLP-1 receptor agonist for glycemic control and weight loss: From discovery to clinical proof of concept.
Coskun T, Urva S, Roell WC, Qu H, Loghin C, Moyers JS, O'Farrell LS, Briere DA, Sloop KW, Thomas MK, Pirro V, Wainscott DB, Willard FS, Abernathy M, Morford L, Du Y, Benson C, Gimeno RE, Haupt A, Milicevic Z. Coskun T, et al. Among authors: wainscott db. Cell Metab. 2022 Sep 6;34(9):1234-1247.e9. doi: 10.1016/j.cmet.2022.07.013. Epub 2022 Aug 18. Cell Metab. 2022. PMID: 35985340 Free 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: wainscott db. 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: wainscott db. 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: wainscott db. 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.
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: wainscott db. 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 incretin co-agonist tirzepatide requires GIPR for hormone secretion from human islets.
El K, Douros JD, Willard FS, Novikoff A, Sargsyan A, Perez-Tilve D, Wainscott DB, Yang B, Chen A, Wothe D, Coupland C, Tschöp MH, Finan B, D'Alessio DA, Sloop KW, Müller TD, Campbell JE. El K, et al. Among authors: wainscott db. Nat Metab. 2023 Jun;5(6):945-954. doi: 10.1038/s42255-023-00811-0. Epub 2023 Jun 5. Nat Metab. 2023. PMID: 37277609 Free PMC article.
Discovery of selective N-[3-(1-methyl-piperidine-4-carbonyl)-phenyl]-benzamide-based 5-HT₁ F receptor agonists: Evolution from bicyclic to monocyclic cores.
Zhang D, Blanco MJ, Ying BP, Kohlman D, Liang SX, Victor F, Chen Q, Krushinski J, Filla SA, Hudziak KJ, Mathes BM, Cohen MP, Zacherl D, Nelson DL, Wainscott DB, Nutter SE, Gough WH, Schaus JM, Xu YC. Zhang D, et al. Among authors: wainscott db. Bioorg Med Chem Lett. 2015 Oct 1;25(19):4337-41. doi: 10.1016/j.bmcl.2015.07.042. Epub 2015 Jul 22. Bioorg Med Chem Lett. 2015. PMID: 26271587
36 results