微管蛋白结合配体靶向癌细胞的机制：治疗潜力和临床试验的新进展

Title:Mechanisms of Tubulin Binding Ligands to Target Cancer Cells: Updates on their Therapeutic Potential and Clinical Trials

Volume: 17 Issue: 4

关键词: 微管蛋白抑制剂，微管稳定剂，微管蛋白聚合/解聚，抗癌，联合治疗，微管蛋白结合配体。

摘要: Background: A number of chemically diverse substances bind to the tubulin and inhibit cell proliferation by disrupting microtubule dynamics. There are four binding sites for the ligands binding to the tubulin; taxane/epothilone and laulimalide/peloruside binding ligands stabilize microtubule while vinca and colchicine binding site agents promote microtubule depolymerization. Most of the tubulin binding ligands disturb the tubulin-microtubule dynamic equilibrium but these may exhibit anticancer activities through different mechanisms. Taxanes and epothilones are widely used cytotoxic agents and are found effective against different types of human malignancies. However, taxanes are susceptible to pgp mediated multi-drug resistance, dose limiting hematopoietic toxicity and cumulative neurotoxicity. Vinca alkaloids are already in clinical practice, but ligands binding to the colchicine site are still in the different stages of clinical trials.

Cite this article as:

Mechanisms of Tubulin Binding Ligands to Target Cancer Cells: Updates on their Therapeutic Potential and Clinical Trials, Current Cancer Drug Targets 2017; 17 (4) . https://dx.doi.org/10.2174/1568009616666160928110818