G protein-coupled receptor 20 (GPR20) is an orphan GPCR. GPR20 expression is regulated by FOXF1 and ETV1 transcription factors that play critical roles in KIT-driven initiation, proliferation, and survival of gastrointestinal stromal tumor.
An antibody-drug conjugate (ADC) is being developed for the treatment of gastrointestinal stromal tumor. This ADC is comprised of a monoclonal antibody that targets the GPR20 antigen and a topoisomerase I inhibitor payload. In vitro studies, the candidate showed anti-tumor activity in GPR20 expressing tumor cells.
G-protein coupled receptor 20 (GPR20)
Gastrointestinal stromal tumor
Mechanism of Action
DNA topoisomerase I inhibitors
More Detail Available Upon Request
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