Prostate cancer (PCa) is typically associated with genetic alterations involving androgen sensitivity and the androgen receptor (AR). Described herein is the expression, molecular regulation, subcellular localization and functional role of a G-protein coupled receptor, GPR158, wherein different four human PCa cell lines with variable alterations in the AR result in various degrees of androgen-responsiveness, androgen-sensitivity and AR expression. Elevation of GPR158 expression is an important oncogenic event that stimulates PCa cell proliferation and progression and thus GPR158 may represent an innovative therapeutic target, particularly for prevent and management of advanced stage PCa, such as castration-resistant prostate cancer (CRPC).
