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Targeting GLP-1 receptor trafficking to improve agonist efficacy.
Jones B, Buenaventura T, Kanda N, Chabosseau P, Owen BM, Scott R, Goldin R, Angkathunyakul N, Corrêa IR Jr, Bosco D, Johnson PR, Piemonti L, Marchetti P, Shapiro AMJ, Cochran BJ, Hanyaloglu AC, Inoue A, Tan T, Rutter GA, Tomas A, Bloom SR. Jones B, et al. Nat Commun. 2018 Apr 23;9(1):1602. doi: 10.1038/s41467-018-03941-2. Nat Commun. 2018. PMID: 29686402 Free PMC article.
Glucagon-like peptide-1 receptor (GLP-1R) activation promotes insulin secretion from pancreatic beta cells, causes weight loss, and is an important pharmacological target in type 2 diabetes (T2D). ...Our study identifies a set of agents w
Glucagon-like peptide-1 receptor (GLP-1R) activation promotes insulin secretion from pancreatic beta cell
Ureidopeptide GLP-1 analogues with prolonged activity in vivo via signal bias and altered receptor trafficking.
Fremaux J, Venin C, Mauran L, Zimmer R, Koensgen F, Rognan D, Bitsi S, Lucey MA, Jones B, Tomas A, Guichard G, Goudreau SR. Fremaux J, et al. Chem Sci. 2019 Sep 11;10(42):9872-9879. doi: 10.1039/c9sc02079a. eCollection 2019 Nov 14. Chem Sci. 2019. PMID: 32015811 Free PMC article.
The high demand of the pharmaceutical industry for new modalities to address the diversification of biological targets with large surfaces of interaction led us to investigate the replacement of alpha-amino acid residues with ureido units at selected positions in peptides …
The high demand of the pharmaceutical industry for new modalities to address the diversification of biological targets with large sur …