Inverse agonist efficacy of selatogrel blunts constitutive P2Y12 receptor signaling by inducing the inactive receptor conformation

Autor:	Véronique Pons, Cédric Garcia, Naomi Tidten-Luksch, Aengus Mac Sweeney, Eva Caroff, Céline Galés, Markus A. Riederer
Rok vydání:	2022
Předmět:	Pharmacology Blood Platelets Adenosine Diphosphate Ticagrelor Platelet Aggregation Purinergic P2Y Receptor Antagonists Humans Platelet Activation Biochemistry
Zdroj:	Biochemical pharmacology. 206
ISSN:	1873-2968
Popis:	Selatogrel is a potent inhibitor of adenosine diphosphate (ADP) binding to the P2Y12 receptor, preventing platelet activation. We have previously shown that the P2Y12 receptor constitutively activates Gi- and Go-protein-mediated signaling in human platelets. Here, we report that selatogrel acts as an inverse agonist of the P2Y12 receptor. Specifically, using bioluminescence resonance energy transfer2 (BRET2) probes, selatogrel, ticagrelor, and elinogrel were shown to stabilize the inactive form of the G
Databáze:	OpenAIRE
Externí odkaz:	https://explore.openaire.eu/search/publication?articleId=doi_dedup___::e10834c4b2d30ebb1004f17c4db090b6 https://pubmed.ncbi.nlm.nih.gov/36306820 Zobrazit plný text záznamu Full Text from ScienceDirect