An overview of tubulin inhibitors that interact with the colchicine binding site

Yan Lu, Jianjun Chen, Min Xiao, Wei Li, Duane Miller

Research output: Contribution to journalReview article

294 Citations (Scopus)

Abstract

Tubulin dynamics is a promising target for new chemotherapeutic agents. The colchicine binding site is one of the most important pockets for potential tubulin polymerization destabilizers. Colchicine binding site inhibitors (CBSI) exert their biological effects by inhibiting tubulin assembly and suppressing microtubule formation. A large number of molecules interacting with the colchicine binding site have been designed and synthesized with significant structural diversity. CBSIs have been modified as to chemical structure as well as pharmacokinetic properties, and tested in order to find a highly potent, low toxicity agent for treatment of cancers. CBSIs are believed to act by a common mechanism via binding to the colchicine site on tubulin. The present review is a synopsis of compounds that have been reported in the past decade that have provided an increase in our understanding of the actions of CBSIs.

Original languageEnglish (US)
Pages (from-to)2943-2971
Number of pages29
JournalPharmaceutical Research
Volume29
Issue number11
DOIs
StatePublished - Nov 1 2012

Fingerprint

Tubulin Modulators
Colchicine
Tubulin
Binding Sites
Pharmacokinetics
Microtubules
Polymerization
Toxicity
Molecules
Neoplasms

All Science Journal Classification (ASJC) codes

  • Biotechnology
  • Molecular Medicine
  • Pharmacology
  • Pharmaceutical Science
  • Organic Chemistry
  • Pharmacology (medical)

Cite this

An overview of tubulin inhibitors that interact with the colchicine binding site. / Lu, Yan; Chen, Jianjun; Xiao, Min; Li, Wei; Miller, Duane.

In: Pharmaceutical Research, Vol. 29, No. 11, 01.11.2012, p. 2943-2971.

Research output: Contribution to journalReview article

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