Drug target interaction of tubulin-binding drugs in cancer therapy.
Microtubules and their component protein, tubulin, constitute a popular target for the treatment of cancer. Many drugs that are presently used in clinics or in clinical trials and drugs that show promise as anticancer drugs bind to tubulin and microtubules. There are three conventional binding sites on beta-tubulin where many of these drugs bind. The binding properties, conformational changes upon binding, association constants and thermodynamic parameters for the drug-tubulin interaction on these three sites are discussed. The antiproliferative activities of these drugs and the possible correlation with the binding properties are also described.
Sengupta
Suparna
S
Rajiv Gandhi Centre for Biotechnology, Cancer Biology Division, Poojappura, Trivandrum 695014, India. sengupta_suparna@hotmail.com
Thomas
Sannu Ann
SA
D000970:Antineoplastic Agents / Q000008:administration & dosage / Q000378:metabolism*; D000971:Antineoplastic Combined Chemotherapy Protocols / Q000008:administration & dosage*; D016503:Drug Delivery Systems / Q000379:methods*; D004347:Drug Interactions / Q000502:physiology; D006801:Humans; D009369:Neoplasms / Q000188:drug therapy / Q000378:metabolism*; D011485:Protein Binding / Q000187:drug effects / Q000502:physiology; D014404:Tubulin / Q000008:administration & dosage / Q000378:metabolism*
D000970:Antineoplastic Agents; D014404:Tubulin