Matches in SemOpenAlex for { <https://semopenalex.org/work/W4213223693> ?p ?o ?g. }
- W4213223693 endingPage "1709" @default.
- W4213223693 startingPage "1695" @default.
- W4213223693 abstract "Adhesion G protein-coupled receptors (aGPCRs) form a sub-group within the GPCR superfamily. Their distinctive structure contains an abnormally large N-terminal, extracellular region with a GPCR autoproteolysis-inducing (GAIN) domain. In most aGPCRs, the GAIN domain constitutively cleaves the receptor into two fragments. This process is often required for aGPCR signalling. Over the last two decades, much research has focussed on aGPCR-ligand interactions, in an attempt to deorphanize the family. Most ligands have been found to bind to regions N-terminal to the GAIN domain. These receptors may bind a variety of ligands, ranging across membrane-bound proteins and extracellular matrix components. Recent advancements have revealed a conserved method of aGPCR activation involving a tethered ligand within the GAIN domain. Evidence for this comes from increased activity in receptor mutants exposing the tethered ligand. As a result, G protein-coupling partners of aGPCRs have been more extensively characterised, making use of their tethered ligand to create constitutively active mutants. This has led to demonstrations of aGPCR function in, for example, neurodevelopment and tumour growth. However, questions remain around the ligands that may bind many aGPCRs, how this binding is translated into changes in the GAIN domain, and the exact mechanism of aGPCR activation following GAIN domain conformational changes. This review aims to examine the current knowledge around aGPCR activation, including ligand binding sites, the mechanism of GAIN domain-mediated receptor activation and how aGPCR transmembrane domains may relate to activation. Other aspects of aGPCR signalling will be touched upon, such as downstream effectors and physiological roles." @default.
- W4213223693 created "2022-02-24" @default.
- W4213223693 creator A5010605024 @default.
- W4213223693 creator A5013962788 @default.
- W4213223693 creator A5041785901 @default.
- W4213223693 creator A5076475814 @default.
- W4213223693 date "2021-07-20" @default.
- W4213223693 modified "2023-10-17" @default.
- W4213223693 title "Emerging roles of adhesion G protein-coupled receptors" @default.
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