NCIt definition : A derivative of 4,5-diarylisoxazole and a third-generation heat shock protein 90 (Hsp90)
inhibitor with potential antineoplastic activity. Luminespib has been shown to bind
with high affinity to and inhibit Hsp90, resulting in the proteasomal degradation
of oncogenic client proteins; the inhibition of cell proliferation; and the elevation
of heat shock protein 72 (Hsp72) in a wide range of human tumor cell lines. Hsp90,
a 90 kDa molecular chaperone, plays a key role in the conformational maturation, stability
and function of other substrate or client proteins within the cell, many of which
are involved in signal transduction, cell cycle regulation and apoptosis, including
kinases, transcription factors and hormone receptors. Hsp72 exhibits anti-apoptotic
functions; its up-regulation may be used as a surrogate marker for Hsp90 inhibition.;