Cynthia Stutsman
YOU?
Author Swipe
View article: Glycaemic and bodyweight effects of <i>GIPR</i> coding variation reflect differences in both surface expression and intrinsic functional impairment
Glycaemic and bodyweight effects of <i>GIPR</i> coding variation reflect differences in both surface expression and intrinsic functional impairment Open
The glucose-dependent insulinotropic polypeptide receptor (GIPR) is the target of several approved and investigational drugs for type 2 diabetes and obesity. Missense coding variation in GIPR could confer phenotypic effects through altered…
View article: Tirzepatide induces a thermogenic-like amino acid signature in brown adipose tissue
Tirzepatide induces a thermogenic-like amino acid signature in brown adipose tissue Open
View article: Structural determinants of dual incretin receptor agonism by tirzepatide
Structural determinants of dual incretin receptor agonism by tirzepatide Open
Significance Tirzepatide is a dual agonist of the glucose-dependent insulinotropic polypeptide receptor (GIPR) and the glucagon-like peptide-1 receptor (GLP-1R), which are incretin receptors that regulate carbohydrate metabolism. This inve…
View article: Discovery of an Orally Efficacious Positive Allosteric Modulator of the Glucagon-like Peptide-1 Receptor
Discovery of an Orally Efficacious Positive Allosteric Modulator of the Glucagon-like Peptide-1 Receptor Open
The identification of LSN3318839, a positive allosteric modulator of the glucagon-like peptide-1 receptor (GLP-1R), is described. LSN3318839 increases the potency and efficacy of the weak metabolite GLP-1(9-36)NH2 to become a fu…
View article: Tirzepatide is an imbalanced and biased dual GIP and GLP-1 receptor agonist
Tirzepatide is an imbalanced and biased dual GIP and GLP-1 receptor agonist Open
Tirzepatide (LY3298176) is a dual GIP and GLP-1 receptor agonist under development for the treatment of type 2 diabetes mellitus (T2DM), obesity, and nonalcoholic steatohepatitis. Early phase trials in T2DM indicate that tirzepatide improv…
View article: Positive Allosteric Modulation of the Glucagon-like Peptide-1 Receptor by Diverse Electrophiles
Positive Allosteric Modulation of the Glucagon-like Peptide-1 Receptor by Diverse Electrophiles Open