NCIt definition : The orally bioavailable mesylate salt of the 17-allylaminogeldanamycin (17-AAG) small-molecule
inhibitor of several receptor protein tyrosine kinases with potential antiangiogenic
and antineoplastic activities. Telatinib binds to and inhibits the vascular endothelial
growth factor receptors (VEGFRs) type 2 and 3, platelet-derived growth factor receptor
beta (PDGFRb) and c-Kit, which may result in the inhibition of angiogenesis and cellular
proliferation in tumors in which these receptors are upregulated. These telatinib-inhibited
receptor protein tyrosine kinases are overexpressed or mutated in many tumor cell
types and may play key roles in tumor angiogenesis and tumor cell proliferation. 17-AAG
is a synthetic analogue of the benzoquinone ansamycin antibiotic geldanamycin and
has also been found to inhibit the molecular chaperone Hsp90.;
Semantic type(s)