Insights into the impact of phenolic residue incorporation at each position along secretin for receptor binding and biological activity.
Regul. Pept., Nov (2012)
Glucagon-like peptide-1 receptor dimerization differentially regulates agonist signaling but does not affect small molecule allostery.
Proc. Natl. Acad. Sci. U.S.A., Nov;109(45):18607-12 (2012)
Sensitivity of cholecystokinin receptors to membrane cholesterol content.
Front Endocrinol (Lausanne)., 3:123 (2012)
Mapping spatial approximations between the amino terminus of secretin and each of the extracellular loops of its receptor using cysteine trapping.
FASEB J., Dec;26(12):5092-105 (2012)
Predicting the effects of amino acid replacements in peptide hormones on their binding affinities for class B GPCRs and application to the design of secretin receptor antagonists.
J. Comput. Aided Mol. Des., Jul;26(7):835-45 (2012)
Molecular basis for binding and subtype selectivity of 1,4-benzodiazepine antagonist ligands of the cholecystokinin receptor.
J. Biol. Chem., May;287(22):18618-35 (2012)
Modulation of Î²-catenin signaling by glucagon receptor activation.
PLoS ONE., 7(3):e33676 (2012)
Differential determinants for coupling of distinct G proteins with the class B secretin receptor.
Am. J. Physiol., Cell Physiol., Apr;302(8):C1202-12 (2012)
Second extracellular loop of human glucagon-like peptide-1 receptor (GLP-1R) has a critical role in GLP-1 peptide binding and receptor activation.
J. Biol. Chem., Feb;287(6):3642-58 (2012)
Second extracellular loop of human glucagon-like peptide-1 receptor (GLP-1R) differentially regulates orthosteric but not allosteric agonist binding and function.
J. Biol. Chem., Feb;287(6):3659-73 (2012)
Site of action of a pentapeptide agonist at the glucagon-like peptide-1 receptor. Insight into a small molecule agonist-binding pocket.
Bioorg. Med. Chem. Lett., Jan;22(1):638-41 (2012)
Ligand-induced internalization of the type 1 cholecystokinin receptor independent of recognized signaling activity.
Am. J. Physiol., Cell Physiol., Feb;302(3):C615-27 (2012)
Differential sensitivity of types 1 and 2 cholecystokinin receptors to membrane cholesterol.
J. Lipid Res., Jan;53(1):137-48 (2012)
Quiescin sulfhydryl oxidase 1 promotes invasion of pancreatic tumor cells mediated by matrix metalloproteinases.
Mol. Cancer Res., Dec;9(12):1621-31 (2011)
Lactam constraints provide insights into the receptor-bound conformation of secretin and stabilize a receptor antagonist.
Biochemistry., Sep;50(38):8181-92 (2011)
Polymorphism and ligand dependent changes in human glucagon-like peptide-1 receptor (GLP-1R) function: allosteric rescue of loss of function mutation.
Mol. Pharmacol., Sep;80(3):486-97 (2011)
Molecular basis of secretin docking to its intact receptor using multiple photolabile probes distributed throughout the pharmacophore.
J. Biol. Chem., Jul;286(27):23888-99 (2011)
Ligand binding and activation of the secretin receptor, a prototypic family B G protein-coupled receptor.
Br. J. Pharmacol., May;166(1):18-26 (2012)
Refinement of glucagon-like peptide 1 docking to its intact receptor using mid-region photolabile probes and molecular modeling.
J. Biol. Chem., May;286(18):15895-907 (2011)
Fluorescence polarization screening for allosteric small molecule ligands of the cholecystokinin receptor.
Assay Drug Dev Technol., Aug;9(4):394-402 (2011)