The tubulysin analogue KEMTUB10 induces apoptosis in @entity0 cells via @entity876 , XXXX and @entity588 .

@entity1 @entity0 @entity588 @entity18847 @entity5 @entity1311 @entity876 @entity22030
PURPOSE: Tubulysins are natural @entity18847 that inhibit tubulin polymerisation. Tubulysins are very potent inhibitors of @entity1 @entity5 cell growth, but restricted availability has limited their characterisation and development as anti- @entity5 compounds. KEMTUB10 was recently developed as a synthetic analogue of natural tubulysins. METHODS: The cell cytotoxicity of KEMTUB10 was studied in cell lines that represent the main @entity0 sub-types. The KEMTUB10 pro-apoptotic mechanism of action was studied in MCF7 and MDAMB231 cells. RESULTS: KEMTUB10 exerts a potent cytotoxic effect in cells representing the main @entity0 sub-types. KEMTUB10 blocks cells in the G2/M phase of the cell cycle and is a strong stimulator of apoptosis/cell death. KEMTUB10-induced apoptosis involves @entity876 and @entity22030 , and to some extent @entity588 phosphorylation. CONCLUSIONS: KEMTUB10 is a promising new anti-mitotic that exerts a potent cytotoxic effect in @entity0 cells, blocks cells in the G2/M phase of the cell cycle and stimulates apoptosis/cell death. KEMTUB10 has a distinct mode of action to @entity1311 , appears to be sensitive to different molecular factors in cells and is likely subject to different mechanisms of acquired resistance. KEMTUB10 has the potential to be an important addition to the anti- @entity5 therapeutic armoury.
