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. 2019 Apr 12;10:155. doi: 10.3389/fendo.2019.00155

Figure 3.

Figure 3

Albumin affinity of fatty-acid derivatized peptides vs. native GLP-1. (A) Derivatives of Aib8, Arg34 GLP-1(7-37) with C12 to C22 di-acids and attached to Lys26 using γGlu- and OEG-based linkers. GLP-1R binding at 0 and 2% HSA using baby BHK cells expressing the human GLP-1R, and in vitro potency measured in BHK cells that express both the human GLP-1R and a luciferase reporter system; (B) HSA binding of GLP-1 derivatives, assessed using analytical ultracentrifugation; (C) In vivo protraction in rats following intravenous administration of 32 (5.5 nmol/kg), semaglutide (4.2 nmol/kg), 19 (3.3 nmol/kg), 16 (5.5 nmol/kg), and 15 (5.3 nmol/kg). BHK, baby hamster kidney; EC50, effective concentration; GLP-1, glucagon-like peptide-1; GLP-1R, glucagon-like peptide-1 receptor; HSA, human serum albumin. Adapted with permission from Lau et al. (53). Copyright 2018, American Chemical Society.