This invention relates to inhibitors of CXC receptor 4 (CXCR4)-G protein-coupled receptor (GPCR) heteromers (CXCR4-GPCR heteromers) associated with cancers, where CXCR4 forms a functional heteromer with other G protein-coupled receptors (GPCRx). More specifically, this invention relates to GPCRx that form heteromers with CXCR4, which upon co-stimulation with CXCR4 agonists and GPCRx agonists leads to enhanced signaling downstream of CXCR4. This invention also provides for the use of inhibitors of the interacting GPCR partner of the CXCR4-GPCRx heteromer or CXCR4-GPCRx heteromer-specific inhibitors including inhibitors of the formation of the CXCR4-GPCRx heteromer and CXCR4-GPCRx heteromer-specific antibodies, and in the diagnosis and/or therapy for cancer.本發明係關於與癌症相關聯之CXC受體4 (CXCR4)-G蛋白偶聯受體(GPCR)異聚體(CXCR4-GPCR異聚體)之抑制劑,其中CXCR4與其他G蛋白偶聯受體(GPCRx)形成功能性異聚體。更特定言之,本發明係關於與CXCR4形成異聚體之GPCRx,其當經CXCR4促效劑及GPCRx促效劑共刺激時會引起CXCR4之增強的信號傳遞下游。本發明亦提供包括形成該CXCR4-GPCRx異聚體及CXCR4-GPCRx異聚體特異性抗體之抑制劑的該CXCR4-GPCRx異聚體或CXCR4-GPCRx異聚體特異性抑制劑之相互作用GPCR搭配物之抑制劑在診斷及/或治療癌症中之用途。