Tigris cancer research is focused on oncology therapeutics.
Tigris' pipeline consists of novel agents targeting key pathways in cancer growth such as p53/apoptosis, angiogenesis, Rho GTPases as well as PI3K/Akt and survivin.
AFP-464 is a lysyl derivative of aminoflavone currently in Phase I development. Aminoflavone induces CYP1A1/1A2 and CYP1B1 protein expression and is converted to metabolites that are covalently bound to DNA, resulting in phosphorylation of p53 with induction of the p53 downstream target p21 Waf1/Cip1 and apoptosis.
GGTI-2418 is a synthetic peptidomimetic inhibitor of geranylgeranyltransferase I (GGTase I). GGTase I inhibitors block Rho function in cancer cells and induces a G1 phase cell cycle arrest. It also induces apoptosis by a mechanism involving down regulation of the expression of survivin and suppression of the activation of PI3K/Akt.
GFB-204 is a selective inhibitor of VEGFR and PDGFR tyrosine phosphorylation. It binds to VEGF and PDGF, blocks binding of VEGF and PDGF to their receptors and subsequently inhibits Flk-1 and PDGFR tyrosine phosphorylation and stimulation of the protein kinases Erk1, Erk2, and Akt.
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