Maraviroc
CCR5 antagonist / Potent and selective CCR5 antagonist with potent anti-HIV activity. It prevents HIV-1 gp120 binding to CCR5 preventing cell-cell fusion. Maraviroc inhibited MIP-1a (IC50 = 3.3 nM), MIP-1b (IC50 = 7.2 nM), and RANTES (IC50 = 5.2 nM) binding to CCR5-expressing HEK-293.1 Clinically useful antiretroviral drug. Many cancer cells express CCR5: Maraviroc blocked metastasis of basal breast2 and pancreatic cancer3 cells, induced cytotoxic and apoptotic effects in colorectal cancer cells4, reduced metastatic tumor growth in lungs5, and suppresses growth in acute ALL cells6. CCR5 inhibition with maraviroc induced macrophage repolarization with anti-tumoral effects.7
Biochemicals & reagents
376348-65-1
UK-427,857
1) Dorr et al. (2005), Maraviroc (UK-427,857), a Potent, Orally Bioavailable, and Selective Small-Molecule Inhibitor of Chemokine Receptor CCR5 with Broad-Spectrum Anti-Human Immunodeficiency Virus Type 1 Activity; Antimicrob.Agents Chemother. 49 4721 2) Velasco-Velazquez et al. (2012), CCR5 antagonist blocks metastasis of basal breast cancer cells; Cancer Res. 72 3839 3) Singh et al. (2018), CCR5/CCL5 axis interaction promotes migratory and invasiveness of pancreatic cancer cells; Sci.Rep. 8 1323 4) Pervaiz et al. (2015), CCR5 blockage by maraviroc induces cytotoxic and apoptotic effects in colorectal cancer cells; Med.Oncol. 32 158 5) Halvorsen et al. (2016), Maraviroc decreases CCL8-mediated migration of CCR5(+) regulatory T cells and reduces metastatic tumor growth in the lungs; Oncoimmunology 5 e1150398 6) Zi et al. (2017), Treatment with the C-C chemokine receptor type 5(CCR5)-inhibitor maraviroc suppresses growth and induces apoptosis of acute lymphoblastic leukemia cells; Am.J.Cancer Res. 7 869 7) Halama et al. (2016), Tumoral Immune Cell Exploitation in Colorectal Cancer Metastases Can Be targeted Effectively by Anti-CCR5 Therapy in Cancer Patients; Cancer Cell 29 587
-20°C
TARGET: GPCR -- PATHWAY: Cell adhesion; Cytokine -- RESEARCH AREA: Immunology -- DISEASE AREA: Cancer; Infectious disease