Schatzman R C, Raynor R L, Kuo J F
Biochim Biophys Acta. 1983 Jan 4;755(1):144-7. doi: 10.1016/0304-4165(83)90284-2.
N-(6-Aminohexyl)-5-chloro-1-naphthalenesulfonamide(W-7), commonly regarded as a calmodulin antagonist, inhibited phospholipid-sensitive Ca2+ -dependent protein kinase and to a lesser extent cyclic GMP- and cyclic AMP-dependent protein kinases. Kinetic studies of the inhibition of the homogeneous spleen phospholipid-sensitive Ca2+ -dependent protein kinase indicated that W-7 inhibited the enzyme activity competitively with respect to phospholipid (Ki = 60 microM). N-(6-Aminohexyl)-1-naphthalenesulfonamide (W-5) was found to be much less potent than W-7. The findings indicate that W-7 was able to inhibit a variety of protein kinases, in addition to those requiring calmodulin previously reported.
N-(6-氨基己基)-5-氯-1-萘磺酰胺(W-7),通常被视为一种钙调蛋白拮抗剂,它能抑制磷脂敏感性钙依赖性蛋白激酶,对环鸟苷酸依赖性蛋白激酶和环腺苷酸依赖性蛋白激酶的抑制作用较弱。对纯质脾脏磷脂敏感性钙依赖性蛋白激酶抑制作用的动力学研究表明,W-7对该酶活性的抑制作用相对于磷脂具有竞争性(抑制常数Ki = 60微摩尔)。研究发现N-(6-氨基己基)-1-萘磺酰胺(W-5)的效力远低于W-7。这些研究结果表明,W-7除了能抑制先前报道的那些需要钙调蛋白的蛋白激酶外,还能够抑制多种蛋白激酶。