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Adhesion G protein–coupled receptors—Candidate metabotropic mechanosensors and novel drug targets
Author(s) -
Langenhan Tobias
Publication year - 2020
Publication title -
basic and clinical pharmacology and toxicology
Language(s) - English
Resource type - Journals
SCImago Journal Rank - 0.805
H-Index - 90
eISSN - 1742-7843
pISSN - 1742-7835
DOI - 10.1111/bcpt.13223
Subject(s) - g protein coupled receptor , metabotropic glutamate receptor , metabotropic receptor , computational biology , drug discovery , superfamily , biology , neuroscience , receptor , chemistry , bioinformatics , biochemistry , agonist
While a wide range of G protein‐coupled receptors (GPCR) have emerged as prime targets for pharmacological intervention long ago, a distinct group of GPCR has only recently been identified and become a research subject to fundamental and clinical scientists. Adhesion‐type GPCR (aGPCR) are exceptional members of the GPCR superfamily in many aspects: structurally, they appear as chimeric surface molecules that possess signature domains of heptahelical (7TM) and adhesion proteins, many aGPCR are autoproteolytically processed, and several homologues have lately been shown to operate as mechanosensors. Bound together by the recent discovery of tethered agonism in aGPCR, these molecular and functional features have entered first models on how aGPCR are activated. Here, I briefly review recent discoveries pertaining to the role of aGPCR as metabotropic mechanosensors that control a large variety of processes in all major tissue types.