Ohmi K, Yamashita S, Nonomura Y
Department of Pharmacology, Faculty of Medicine, University of Tokyo, Japan.
Biochem Biophys Res Commun. 1990 Dec 31;173(3):976-81. doi: 10.1016/s0006-291x(05)80881-2.
In the growth arrested cultures of bovine carotid smooth muscle, K252a (10 - 100 ng/ml), a protein kinase inhibitor with wide spectrum suppressed the cell proliferation induced by TPA and increase of serum. K252a was more potent in the antiproliferative activity than H7, a C-kinase-specific inhibitor, but less than staurosporine, another wide-spectrum protein kinase inhibitor. Since C-kinase plays an important role in the signal transduction leading to the cell proliferation and K252a inhibits C-kinase in vitro, the antiproliferative effect of K252a to carotid smooth muscle cells is likely to be exerted through c-kinase dependent pathway.
在生长停滞的牛颈动脉平滑肌培养物中，K252a（10 - 100纳克/毫升），一种具有广谱性的蛋白激酶抑制剂，可抑制由佛波酯（TPA）和血清增加所诱导的细胞增殖。K252a在抗增殖活性方面比H7（一种C激酶特异性抑制剂）更强，但比另一种广谱蛋白激酶抑制剂星形孢菌素弱。由于C激酶在导致细胞增殖的信号转导中起重要作用，且K252a在体外可抑制C激酶，因此K252a对颈动脉平滑肌细胞的抗增殖作用可能是通过依赖C激酶的途径发挥的。
