September 2022 "Introduction Protease activated receptors 1 (PAR1) and 4 (PAR4) agonists are used to Here we show that C1INH affects platelet activation through PAR1 and PAR4 agonists. The platelet suspensions were exposed to PAR1 agonists SFLLRN, TFLLR and TFLLRN; PAR4 agonists AYPGKF

November 2022 "Some G protein-coupled receptor (GPCR) ligands act as "biased agonists" that preferentially

October 2022 GPCR Agonist-to-Antagonist Conversion: Enabling the Design of Nucleoside Functional Switches that a thiophene modification at the C8 position in the common adenine scaffold converted an A2AAR agonist In contrast to A2AAR agonists, which simultaneously interact with both Ser2777.42 and His2787.43, 2 only can expand the repertoire of adenosine receptor antagonists that can be designed based on available agonist

< GPCR News < GPCRs in Oncology and Immunology Agonists of galanin subtype 2 receptor may prevent pancreatic cancer and agonists of angiotensin II type 2 receptor may prevent colorectal cancer Published date June Recently, a (methyl)lanthionine-stabilized, highly receptor-specific agonist of galanin subtype 2 (GAL2 Furthermore, a lanthionine-constrained agonist of angiotensin II type 2 (AT2) receptor inhibited PDX Importantly, a (methyl)lanthionine-stabilized GAL2 receptor-specific agonist enhances expression of GAL2

We found that adhesion GPCRs are activated by a tethered peptide agonist mechanism that differed from sequence that is clipped by exogenous proteases to reveal a new N-terminus that serves as the tethered agonist themselves and the two resultant fragments of the receptor remain together to conceal the tethered peptide agonist the two fragments aided by protein binding ligands and cell movement serves to decrypt the tethered agonist

participated and initiated methodologies for development of pharmacologically active anti-GPCR antibodies like agonist , antagonist, inverse agonist or blocker.