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.
本发明涉及与癌症相关的CXC受体4(CXCR4)-G蛋白偶联受体(
GPCR)异构体(CXCR4-
GPCR异构体)的
抑制剂,其中CXCR4与其他G蛋白偶联受体(
GPCRx)形成功能性异构体。更具体地说,本发明涉及与 CXCR4 形成异构体的
GPCRx,在 CXCR4 激动剂和
GPCRx 激动剂的共同刺激下,会导致 CXCR4 下游信号的增强。本发明还提供了CXCR4-
GPCRx异构体相互作用
GPCR伙伴的
抑制剂或CXCR4-
GPCRx异构体特异性
抑制剂的用途,包括CXCR4-
GPCRx异构体形成
抑制剂和CXCR4-
GPCRx异构体特异性
抗体,以及在癌症诊断和/或治疗中的用途。