Antimicrotubular drugs binding to vinca domain of tubulin

被引:54
作者
Gupta, S [1 ]
Bhattacharyya, B [1 ]
机构
[1] Bose Inst, Dept Biochem, Kolkata 700054, W Bengal, India
关键词
tubulin; microtubules; spindle; anticancer drugs; vinblastine;
D O I
10.1023/A:1026045100219
中图分类号
Q2 [细胞生物学];
学科分类号
071009 ; 090102 ;
摘要
Studies on vinca domain binding drugs were done in great details by a number of workers as it is recognized as a potential target for anticancer drug development. Their structures, properties, mode of action, success and failures as potential anticancer drug have been discussed in short details in this review. Among these drugs rhizoxin and maytansine are competitive inhibitors, and bind at the vinblastine binding site of tubulin where as others are non-competitive inhibitors. Besides binding, these drugs also differ in the extent of GTP hydrolysis, GTP exchange and in the stabilization of colchicine binding site. The toxicity level of these drugs towards the host cells and the extent of efflux of drugs by the P-glycoprotein mediated pump are also discussed.
引用
收藏
页码:41 / 47
页数:7
相关论文
共 61 条
[1]  
Ali MA, 1998, ANTICANCER RES, V18, P1021
[2]  
Anderson HJ, 1997, CANCER CHEMOTH PHARM, V39, P223
[3]  
BAI R, 1991, J BIOL CHEM, V266, P15882
[4]   DOLASTATIN-10, A POWERFUL CYTOSTATIC PEPTIDE DERIVED FROM A MARINE ANIMAL - INHIBITION OF TUBULIN POLYMERIZATION MEDIATED THROUGH THE VINCA ALKALOID BINDING DOMAIN [J].
BAI, R ;
PETTIT, GR ;
HAMEL, E .
BIOCHEMICAL PHARMACOLOGY, 1990, 39 (12) :1941-1949
[5]   Interactions of the sponge-derived antimitotic tripeptide hemiasterlin with tubulin: Comparison with dolastatin 10 and cryptophycin 1 [J].
Bai, RL ;
Durso, NA ;
Sackett, DL ;
Hamel, E .
BIOCHEMISTRY, 1999, 38 (43) :14302-14310
[6]  
BAI RL, 1995, MOL PHARMACOL, V47, P965
[7]  
Bai RL, 1996, CANCER RES, V56, P4398
[8]   THE SPONGISTATINS, POTENTLY CYTOTOXIC INHIBITORS OF TUBULIN POLYMERIZATION, BIND IN A DISTINCT REGION OF THE VINCA DOMAIN [J].
BAI, RL ;
TAYLOR, GF ;
CICHACZ, ZA ;
HERALD, CL ;
KEPLER, JA ;
PETTIT, GR ;
HAMEL, E .
BIOCHEMISTRY, 1995, 34 (30) :9714-9721
[9]  
BAI RL, 1993, MOL PHARMACOL, V44, P757
[10]   TUBULIN AGGREGATION AND DISAGGREGATION - MEDIATION BY 2 DISTINCT VINBLASTINE-BINDING SITES [J].
BHATTACHARYYA, B ;
WOLFF, J .
PROCEEDINGS OF THE NATIONAL ACADEMY OF SCIENCES OF THE UNITED STATES OF AMERICA, 1976, 73 (07) :2375-2378