| abstract |
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 ADRB2 that form heteromers with CXCR4, which upon co-stimulation with CXCR4 agonists and ADRB2 agonists leads to enhanced signaling downstream of CXCR4. This invention also provides for pharmaceutical compositions and kits comprising a CXCR4 inhibitor and an ADRB2 inhibitor, and methods for treating and using the same, and in the diagnosis and/or therapy for cancer. |