GPCR/G Protein

G-Protein antagonist peptide acetate is a truncated substance P-related peptide, competes with receptor for G protein binding. G-Protein antagonist peptide acetate inhibits the activation of Gi or Go by M2 muscarinic cholinergic receptor (M2 mAChR) or of Gs by beta-adrenergic receptor in the reconstituted phospholipid vesicles, assayed by receptor-promoted GTP hydrolysis

Using specific antisera raised against synthetic peptides, we find that three distinct GTP-binding protein alpha subunits remain bound to the plasma membrane even after activation with nonhydrolyzable GTP analog. Trypsin cleaves each alpha subunit at a si

Substance P-related peptide that inhibits binding of G proteins to their receptors. Competitively and reversibly inhibits M2 muscarinic receptor activation of Gi or Go and inhibits Gs activation by β-adrenoceptors.

VPM-p15, a synthetic peptide agonist targeting the adhesion G protein-coupled receptor (GPCR) G2 (ADGRG2)—an orphan GPCR implicated in male infertility—facilitates cAMP accumulation in HEK293 cells expressing human ADGRG2, demonstrating efficacy with an EC50 value of 1.41 µM.

Neuromedin S (human), a 33-amino acid neuropeptide, serves as an endogenous ligand for the orphan G-protein coupled receptor (GPCR) FM-4 TGR-1, and acts on the neuromedin U (NMU) receptor 2 (NMUR2) to regulate body weight homeostasis [1].