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

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

Volume: 17 Issue: 4

Author(s): Bhupinder Kumar, Rakesh Kumar, Ira Skvortsova*Vinod Kumar*

Affiliation:

• Laboratory for Experimental and Translational Research on Radiation Oncology (EXTRO-Lab), Department of Therapeutic Radiology and Oncology, Innsbruck Medical University, Anichstr. 35, A-6020 Innsbruck,Austria

• Laboratory of Organic and Medicinal Chemistry, Centre for Pharmaceutical Sciences and Natural Product, Central University of Punjab, Bathinda, Punjab,India

Keywords: Tubulin inhibitor, microtubule stabilizing agents, tubulin polymerization/depolymerization, anticancer, combination therapy, tubulin binding ligands.

Abstract: 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:

Kumar Bhupinder, Kumar Rakesh, Skvortsova Ira*, Kumar Vinod*, 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