122nd General Meeting of the KCS

Type Symposium
Area Current Trends in Drug Repositioning
Room No. Room 306B
Time THU 16:30-:
Code MEDI-3
Subject CXCR4 hetromer as a drug target for precision cancer therapeutics
Authors Dongseung Seen
R&D center, GPCR Therapeutics, Korea
Abstract CXC receptor 4 (CXCR4) is a member of the chemokine receptor family GPCR. CXCR4 responds to its ligand CXCL12/SDF-1, and has essential roles in the embryonic development of the hematopoietic, cardiovascular, and nervous systems. CXCR4 was discovered as a co-receptor for HIV, and has important roles in the homing of hematopoietic stem cells to the bone marrow, inflammation, immune surveillance of tissues, and tissue regeneration in adult. Overexpression of CXCR4 is regarded as a poor prognosis marker in many different types of human cancers including breast cancer, lung cancer, brain cancer, etc. CXCR4 plays pivotal roles in the proliferation, survival, and invasiveness of cancer cells. Various drugs targeting CXCR4 has been developed from AMD-3100, but development of CXCR4 antagonists as anti-cancer drugs is an ongoing challenge. To avoid potential side effects associated with conventional CXCR4 antagonists and to develop more efficient anti-cancer drugs targeting CXCR4, new paradigm for designing CXCR4 inhibitor is required. CXCR4 forms heteromers with different GPCRs. There exists a need for developing CXCR4 inhibitors for use as GPCR heteromer-targeting cancer therapeutics with higher efficacy and lower side effects. GPCR therapeutics Inc. was founded to develop CXCR4 heteromer inhibitors and has been validating using drug repositioning strategy. For the development of CXCR4 inhibitors, GPCR therapeutics and Samsung medical center have been collaborating in patient derived xenograft and antibody discovery. Up to now, GPCR therapeutics Inc. fund-raised about 12 million dollars from 7 Venture capitals in 2015 and 2016. Now, 25 persons work for GPCR therapeutics Inc.
E-mail seenbio@gpcr.co.kr