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Article

The activation mechanism and antibody binding mode for orphan GPR20

28 Feb 2023

Abstract excerpt

GPR20 is a class-A orphan G protein-coupled receptor (GPCR) and a potential therapeutic target for gastrointestinal stromal tumors (GIST) owing to its differentially high expression. An antibody-drug conjugate (ADC) containing a GPR20-binding antibody (Ab046) was recently developed in clinical trials for GIST treatment. GPR20 constitutively activates Gi proteins in the absence of any known ligand, but it remains...

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PMID: 36849514
DOI: 10.1038/s41421-023-00520-8

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