Taxanes

TaxanesMechanism of Action
Paclitaxel, docetaxel Stabilizes microtubules and causes mitotic arrest and apoptosis
1 2 3 4 5 6
  1. Taxanes bind to and polymerize bII-tubulins, resulting in microtubule stabilization, arrest in the G2/M phase of the cell cycle, and cell death. Paclitaxel and docetaxel are inactive in cells with TUBB3 microtubules.
  2. The inhibitor of apoptosis protein survivin promotes progression through G2/M and interferes with induction of cell death.
  3. ESR1 transcriptionally increases the levels of survivin
  4. BRCA1 blocks ESR1 function and decreases survivin expression.
  5. PGP effluxes taxanes thereby decreasing their intra-cellular concentrations.
  6. SPARC binds albumin in nab-paclitaxel to locally increase the paclitaxel levels.

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Green squares, sensitivity markers. Red squares, resistance markers