NCIt synonyms : Heat Shock Protein 90 Inhibitor NVP-BEP800;
NCIt definition : An orally bioavailable inhibitor of heat shock protein 90 (Hsp90), with potential
antineoplastic activity. Upon oral administration, Hsp90 inhibitor NVP-BEP800 specifically
binds to the NH(2)-terminal ATP-binding pocket of Hsp90 and specifically blocks Hsp90,
which inhibits its chaperone function and promotes the proteasomal degradation of
oncogenic signaling proteins involved in tumor cell proliferation and survival, including
ErbB2, B-Raf(V600E), Raf-1, and Akt. This prevents oncogenic pathway signaling mediated
by these proteins and leads to the inhibition of tumor cell proliferation. Hsp90,
a chaperone complex protein upregulated in a variety of tumor cell types, regulates
the folding and degradation of many oncogenic signaling proteins.;