The uses and limitations of calmodulin antagonists.
The uses and limitations of calmodulin antagonists.
复制标题
钙调蛋白拮抗剂的用途和局限性。
DOI：
10.1016/0163-7258(89)90066-1
复制
发表时间：
1989
影响因子：
13.5
通讯作者：
Sedwick,WD
中科院分区：
文献类型：
--
作者：
Veigl,ML;Klevit,RE;Sedwick,WD
钙调素（CAM）通过调节Ca2+信号在细胞调控中发挥重要作用，这为开发能改变CAM功能的药物提供了巨大的动力。这些努力导致了一些有效的拮抗剂的钙调素功能的鉴定，但细胞内的钙调素的生理作用的演示仍然难以捉摸，因为缺乏特异性的这些代理。这些拮抗剂的开发进展，其作为钙调素抑制剂的活动，其与钙调素相互作用的结构基础，其用于治疗癌症，神经功能障碍和其他疾病，其特异性钙调素作为一个独特的药物靶点是本次审查的主题。
The potential of calmodulin (CAM) to play a pivotal role in cell regulation through modulation of Ca 2+ signals has provided great impetus to investigations directed toward development of drugs that can alter the function of this protein. These efforts have led to the identification of a number of potent antagonists of CaM function, but intracellular demonstration of the physiological roles of CaM has remained elusive because of the lack of specificity of these agents. Progress toward development of these antagonists, their activities as CaM inhibitors, the structural basis of their interaction with CaM, their utility for treatment of cancer, neurological dysfunction and other disease, and their specificity for CaM as a unique drug target are the subjects of this review.