GPCR HETEROMER INHIBITORS AND USES THEREOF

GPCR HETEROMER INHIBITORS AND USES THEREOF

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 tha...

Ausführliche Beschreibung

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Bibliographische Detailangaben
Hauptverfasser: YANG, Chang Soo, YANG, Jiwon, LEE, Jiyeong, SEEN, DongSeung, LEE, DongJin, KIM, Eunhee, KIM, SoHui, SEO, HyeonGyu
Format: Patent
Sprache:eng
Schlagworte:
CHEMISTRY
HUMAN NECESSITIES
HYGIENE
INVESTIGATING OR ANALYSING MATERIALS BY DETERMINING THEIRCHEMICAL OR PHYSICAL PROPERTIES
MEASURING
MEDICAL OR VETERINARY SCIENCE
METALLURGY
ORGANIC CHEMISTRY
PEPTIDES
PHYSICS
PREPARATIONS FOR MEDICAL, DENTAL, OR TOILET PURPOSES
SPECIFIC THERAPEUTIC ACTIVITY OF CHEMICAL COMPOUNDS ORMEDICINAL PREPARATIONS
TESTING
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Beschreibung
Zusammenfassung: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.