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首页> 外文期刊>Proceedings of the National Academy of Sciences of the United States of America >Structural basis for selectivity of the isoquinoline sulfonamide family of protein kinase inhibitors
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Structural basis for selectivity of the isoquinoline sulfonamide family of protein kinase inhibitors

机译:蛋白质激酶抑制剂异喹啉磺酰胺家族选择性的结构基础

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摘要

A large family of isoquinoline sulfonamide compounds inhibits protein kinases by competing with aden- osine triphosphates (ATP), yet interferes little with the activ- ity of other ATP-using enzymes such as ATPases and adenyl- ate cyclases. One such compound, N-(2-aminoethyl)-5- chloroisoquinoline-8-sulfonamide (CKI7), is selective for casein kinase-1 isolated from a variety of sources.
机译:一大批异喹啉磺酰胺化合物通过与腺苷三磷酸(ATP)竞争来抑制蛋白激酶,而对其他使用ATP的酶(例如ATPase和腺苷酸环化酶)的活性影响很小。一种这样的化合物,N-(2-氨基乙基)-5-氯异喹啉-8-磺酰胺(CKI7),对于从多种来源分离的酪蛋白激酶-1具有选择性。

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