Research progress in medicines on protease-activated receptor 2 / 药学学报

Protease-activated receptor 2 (PAR2) is a member of protease-activated receptors (PARs). PAR2 distributed in tissues and cells (such as skin, airway epithelial cell, pancreas, etc.) has a broad biological effects, and is involved in pathogenesis of many diseases, such as mechanical pain, asthma, pain of pancreatic cancer, inflammation, pruritus, etc. Intervention of PAR2 will help us to identify the role of PAR2 in the mechanisms of diseases and in the development of new drugs. This article concentrates on the research progress of agonist, antagonist, and pepducin on PAR2.

Peptides Corresponding to Intracellular Regions of GPCR as a New Generation of Selective Drugs.

In the G protein-coupled receptors (GPCRs) relatively short regions of their intracellular loops and cytoplasmic C-terminal domain are responsible for specific interaction with G-proteins. GPCR-derived peptides corresponding to these regions are able to influence the activity of signal pathways involving the cognate receptors. Modified by hydrophobic radicals, these peptides turn into their cell-penetrating analogs, pepducins, possessing the activity both in vitro and in vivo. This review is devoted to the analysis of the available data and the prospects for GPCR-peptides and their lipophilic derivatives to be used in experimental and clinical medicine in the treatment of vascular diseases, cancers, inflammation, and endocrine dysfunctions.