Sakowicz R, Berdelis M S, Ray K, Blackburn C L, Hopmann C, Faulkner D J, Goldstein L S
Department of Pharmacology, Division of Cellular and Molecular Medicine, Howard Hughes Medical Institute, University of California, San Diego, 9500 Gilman Drive, La Jolla, CA 92093-0683, USA.
Science. 1998 Apr 10;280(5361):292-5. doi: 10.1126/science.280.5361.292.
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.
驱动蛋白超家族的运动蛋白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运输的过程至关重要。一种名为阿多西硫酸盐-2的化合物是从海洋海绵Haliclona(也称为Adocia)物种中分离出来的,它通过靶向驱动蛋白的运动结构域并模拟微管的活性来抑制驱动蛋白活性。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,而阿多西硫酸盐-2应作为驱动蛋白功能特异性抑制剂的原型。