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Structural determinants of dual incretin receptor agonism by tirzepatide.
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.
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: stutsman c.
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
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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: stutsman c.
JCI Insight. 2020 Sep 3;5(17):e140532. doi: 10.1172/jci.insight.140532.
JCI Insight. 2020.
PMID: 32730231
Free PMC article.
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Positive Allosteric Modulation of the Glucagon-like Peptide-1 Receptor by Diverse Electrophiles.
Bueno AB, Showalter AD, Wainscott DB, Stutsman C, Marín A, Ficorilli J, Cabrera O, Willard FS, Sloop KW.
Bueno AB, et al. Among authors: stutsman c.
J Biol Chem. 2016 May 13;291(20):10700-15. doi: 10.1074/jbc.M115.696039. Epub 2016 Mar 14.
J Biol Chem. 2016.
PMID: 26975372
Free PMC article.
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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: stutsman c.
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
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Tirzepatide induces a thermogenic-like amino acid signature in brown adipose tissue.
Samms RJ, Zhang G, He W, Ilkayeva O, Droz BA, Bauer SM, Stutsman C, Pirro V, Collins KA, Furber EC, Coskun T, Sloop KW, Brozinick JT, Newgard CB.
Samms RJ, et al. Among authors: stutsman c.
Mol Metab. 2022 Oct;64:101550. doi: 10.1016/j.molmet.2022.101550. Epub 2022 Jul 31.
Mol Metab. 2022.
PMID: 35921984
Free PMC article.
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