Understanding the polypharmacology of Proteinase-activated receptor (PAR) pepducins and investigating their biophysical association using mass spectrometry imaging (MSI) technologies

• Published in: Proceedings for Annual Meeting of The Japanese Pharmacological Society Vol. WCP2018; p. OR26-5
• Main Author: Cunningham, Margaret R
• Format: Journal Article
• Language: English
• Published: Japanese Pharmacological Society 2018
• Subjects: G protein-coupled receptor (GPCR); Pepducins; Proteinase-activated receptors (PARs)

Background: Conventional antiplatelet therapies consist of drugs that target surface proteins called G protein-coupled receptors (GPCRs), Competitive antagonists, such as Vorapaxar, which inhibits proteinase-activated receptor-1 (PAR1), has been associated with severe bleeding [1]. High affinity, co...