Adhesion G protein-coupled receptor G2 (ADGRG2) (ADGRG2)

Adhesion G protein-coupled receptor G2 (ADGRG2), also known as GPR64, is an orphan receptor belonging to the adhesion G protein-coupled receptor family (UniProt Q8IZP9). It is primarily expressed in the human epididymis, where it plays a critical role in fluid resorption and male fertility (NCBI Gene ID 10149). In a pathological context, ADGRG2 is significantly overexpressed in several malignancies, most notably Ewing sarcoma and certain types of prostate and parathyroid cancers (Richter et al., 2013, Leukemia). This restricted expression profile makes it an attractive candidate for targeted therapies, such as antibody-drug conjugates (ADCs) and CAR-T cell therapies, aimed at treating aggressive cancers (The Human Protein Atlas). Research indicates that ADGRG2 may promote tumor cell proliferation and metastasis, and its mRNA levels are often used as a biomarker for target engagement in experimental treatments (PubMed PMID: 23459451). Silencing of the GPR64 gene via RNA interference has been shown to inhibit tumor growth in preclinical models, further validating its role as a therapeutic target. The receptor's large extracellular domain facilitates the binding of therapeutic antibodies, making it a versatile target for various modalities.

Other names

G-protein coupled receptor 64GPR64HE6Human epididymis-specific protein 6EDDM6

Targeted cell killing via antibody-drug conjugates (ADCs) or CAR-T cell-mediated cytotoxicity; potential for RNA interference-mediated gene silencing.