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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: sloop kw. 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.
LY3298176, a novel dual GIP and GLP-1 receptor agonist for the treatment of type 2 diabetes mellitus: From discovery to clinical proof of concept.
Coskun T, Sloop KW, Loghin C, Alsina-Fernandez J, Urva S, Bokvist KB, Cui X, Briere DA, Cabrera O, Roell WC, Kuchibhotla U, Moyers JS, Benson CT, Gimeno RE, D'Alessio DA, Haupt A. Coskun T, et al. Among authors: sloop kw. Mol Metab. 2018 Dec;18:3-14. doi: 10.1016/j.molmet.2018.09.009. Epub 2018 Oct 3. Mol Metab. 2018. PMID: 30473097 Free PMC article. Clinical Trial.
How May GIP Enhance the Therapeutic Efficacy of GLP-1?
Samms RJ, Coghlan MP, Sloop KW. Samms RJ, et al. Among authors: sloop kw. 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.
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: sloop kw. 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: sloop kw. 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: sloop kw. 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: sloop kw. 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
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: sloop kw. J Clin Invest. 2021 Jun 15;131(12):e146353. doi: 10.1172/JCI146353. J Clin Invest. 2021. PMID: 34003802 Free PMC article.
87 results