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PKC isozymes in chronic cardiac disease: possible therapeutic targets?
Annual Review of Pharmacology and Toxicology ( IF 12.5 ) Pub Date : 2007-10-09 , DOI: 10.1146/annurev.pharmtox.48.121806.154902
Eric Churchill 1 , Grant Budas , Alice Vallentin , Tomoyoshi Koyanagi , Daria Mochly-Rosen
Affiliation  

Cardiovascular disease is the leading cause of death in the United States. Therefore, identifying therapeutic targets is a major focus of current research. Protein kinase C (PKC), a family of serine/threonine kinases, has been identified as playing a role in many of the pathologies of heart disease. However, the lack of specific PKC regulators and the ubiquitous expression and normal physiological functions of the 11 PKC isozymes has made drug development a challenge. Here we discuss the validity of therapeutically targeting PKC, an intracellular signaling enzyme. We describe PKC structure, function, and distribution in the healthy and diseased heart, as well as the development of rationally designed isozyme-selective regulators of PKC functions. The review focuses on the roles of specific PKC isozymes in atherosclerosis, fibrosis, and cardiac hypertrophy, and examines principles of pharmacology as they pertain to regulators of signaling cascades associated with these diseases.

中文翻译:

慢性心脏病中的PKC同工酶:可能的治疗靶点?

在美国,心血管疾病是主要的死亡原因。因此,确定治疗目标是当前研究的主要重点。蛋白激酶C(PKC)是丝氨酸/苏氨酸激酶的一个家族,已被确定在许多心脏病病理中均起着作用。但是,缺乏特定的PKC调节剂以及11种PKC同工酶的普遍表达和正常的生理功能使药物开发面临挑战。在这里,我们讨论治疗性靶向PKC(一种细胞内信号转导酶)的有效性。我们描述了PKC的结构,功能和在健康和患病心脏中的分布,以及合理设计的PKC功能的同工酶选择性调节剂的发展。这篇综述着重于特定的PKC同工酶在动脉粥样硬化,纤维化,
更新日期:2019-11-01
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