title: An overview of tubulin inhibitors that interact with the colchicine binding site.
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.
authors: Department of Pharmaceutical Sciences, Health Science Center, University of Tennessee, 847 Monroe Ave, Memphis, TN 38163, USA.
authors: Yan
authors: Y
authors: Lu
authors: Jianjun
authors: J
authors: Chen
authors: Min
authors: M
authors: Xiao
authors: Wei
authors: W
authors: Li
authors: Duane D
authors: DD
authors: Miller
mesh_terms: D000818:Animals; D000970:Antineoplastic Agents / Q000494:pharmacology / Q000627:therapeutic use; D001665:Binding Sites; D003078:Colchicine / Q000378:metabolism*; D006801:Humans; D011485:Protein Binding; D014404:Tubulin / Q000378:metabolism*; D050257:Tubulin Modulators / Q000494:pharmacology* / Q000627:therapeutic use*
chemical_list: D000970:Antineoplastic Agents; D014404:Tubulin; D050257:Tubulin Modulators; D003078:Colchicine