A marine natural product inhibitor of kinesin motors.
A marine natural product inhibitor of kinesin motors.
复制标题
DOI：
10.1126/science.280.5361.292
复制
发表时间：
1998-04
期刊：
影响因子：
56.9
通讯作者：
R. Sakowicz;M. S. Berdelis;K. Ray;C. L. Blackburn;C. Hopmann;D. Faulkner;L. Goldstein
中科院分区：
文献类型：
--
作者：
R. Sakowicz;M. S. Berdelis;K. Ray;C. L. Blackburn;C. Hopmann;D. Faulkner;L. Goldstein
运动蛋白驱动蛋白超家族的成员对于有丝分裂和减数分裂纺锤体组织、染色体分离、细胞器和囊泡运输以及许多其他需要基于微管的运输的过程是必需的。一种名为adociasulfate-2的化合物是从一种海洋海绵Haliclona（也被称为Aliccia）物种中分离出来的，它通过靶向其运动域并模拟微管的活性来抑制驱动蛋白的活性。因此，驱动蛋白-微管相互作用位点可能是小分子调节剂的有用靶点，adociasulfate-2应该作为驱动蛋白功能特异性抑制剂的原型。
Members of the kinesin superfamily of motor proteins are essential for mitotic and meiotic spindle organization, chromosome segregation, organelle and vesicle transport, and many other processes that require microtubule-based transport. A compound, adociasulfate-2, was isolated from a marine sponge, Haliclona (also known as Adocia) species, that inhibited kinesin activity by targeting its motor domain and mimicking the activity of the microtubule. Thus, the kinesin-microtubule interaction site could be a useful target for small molecule modulators, and adociasulfate-2 should serve as an archetype for specific inhibitors of kinesin functions.