KSPWFTTL is an immunodominant epitope derived from the p15E transmembrane protein. It is Kb-restricted and can enhance the susceptibility of a tumor cell line to cytotoxic T lymphocytes targeting anti-AKR/Gross MuLV.
MK-0731, a synthetic small molecule with potential antineoplastic activity, selectively inhibits kinesin spindle protein (KSP), leading to the inhibition of mitotic spindle assembly, induction of cell cycle arrest during the mitotic phase and apoptosis in
Filanesib (ARRY-520) targets the kinesin spindle protein (KSP) with potential antineoplastic activity. ARRY-520 specifically inhibits KSP (kinesin-5 or Eg5), resulting in activation of the spindle assembly checkpoint, induction of cell cycle arrest during
AZD4877 is a synthetic kinesin spindle protein (KSP) inhibitor with potential antineoplastic activity. KSP inhibitor AZD4877 selectively inhibits microtubule motor protein KSP (also called kinesin-5 or Eg5), which may result in the inhibition of mitotic spindle assembly; activation of the spindle assembly checkpoint; induction of cell cycle arrest during the mitotic phase; and cell death in tumor cells that are actively dividing. Because KSP is not involved in postmitotic processes, such as neuronal transport, this agent may be less likely to cause the peripheral neuropathy often associated with the tubulin-targeting agents. Eg5 is essential for the formation of bipolar spindles and the proper segregation of sister chromatids during mitosis.
CK0106023 was specific inhibitor of KSP. In tumor-bearing mice, CK0106023 exhibited antitumor activity comparable to or exceeding that of paclitaxel and caused the formation of monopolar mitotic figures identical to those produced in cultured cells. KSP was most abundant in proliferating human tissues and was absent from cultured postmitotic neurons.