Biological ActivityTAT-cyclo-CLLFVY is a selective HIF-1 dimerization inhibitor. Blocks protein-protein interaction of recombinant HIF-1α, but not HIF-2α, with HIF-1β (IC50 = 1.3 μM). Inhibits hypoxia-induced HIF-1 activity, and decreases VEGF and CAIX expression in osteosarcoma and breast cancer cells in vitro. Also reduces tubularization of hypoxic HUVECs.
(Modifications: Lactam bridge: Cys-1 to Tyr-6), Disulfide bridge: 1-1*)
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Complete Your Research
A cyclic peptide inhibitor of HIF-1 heterodimerization that inhibits hypoxia signaling in cancer cells.
Miranda E, Nordgren IK, Male AL et al.
J Am Chem Soc.
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