NCIt definition : The acetate salt form of sotrastaurin, an orally available pan-protein kinase C (PKC)
inhibitor with potential immunosuppressive and antineoplastic activities. Sotrastaurin
inhibits both T- and B-cell activations via PKC theta and beta isozymes, respectively.
Both PKCs are important in the activation of nuclear factor-kappaB (NF-kB). Inhibition
of PKC beta in B-cells results in prevention of NF-kB-mediated signaling and down
regulation of NF-kB target genes. This may eventually lead to an induction of G1 cell
cycle arrest and tumor cell apoptosis in susceptible tumor cells. This agent may act
synergistically with other chemotherapeutic agents. PKC, a family of serine/threonine
protein kinases overexpressed in certain types of cancer cells, is involved in cell
differentiation, mitogenesis, inflammation, and the activation and survival of lymphocytes.;
Semantic type(s)