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Research advances in kinase enzymes and inhibitors for cardiovascular disease treatment

机译:激酶酶和抑制剂在心血管疾病治疗中的研究进展

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摘要

The targeting of protein kinases has great future potential for the design of new drugs against cardiovascular diseases (CVDs). Enormous efforts have been made toward achieving this aim. Unfortunately, kinase inhibitors designed to treat CVDs have suffered from numerous limitations such as poor selectivity, bad permeability and toxicity. So, where are we now in terms of discovering effective kinase targeting drugs to treat CVDs? Various drug design techniques have been approached for this purpose since the discovery of the inhibitory activity of Staurosporine against protein kinase C in 1986. This review aims to provide context for the status of several emerging classes of direct kinase modulators to treat CVDs and discuss challenges that are preventing scientists from finding new kinase drugs to treat heart disease.
机译:靶向蛋白激酶在设计针对心血管疾病(CVD)的新药物方面具有巨大的未来潜力。为了实现这个目标,已经做出了巨大的努力。不幸的是,设计用于治疗CVD的激酶抑制剂具有许多局限性,例如选择性差,通透性差和毒性小。那么,就发现有效的针对CVD的激酶靶向药物而言,我们现在在哪里呢?自从1986年发现Staurosporine对蛋白激酶C的抑制活性以来,已经采用了多种药物设计技术。该综述旨在为几种新兴的直接激酶调节剂治疗CVD的现状提供背景信息,并讨论一些挑战。正在阻止科学家找到治疗心脏病的新激酶药物。

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