Protein kinase C, an elusive therapeutic target?
Protein kinase C, an elusive therapeutic target?
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DOI：
10.1038/nrd3871
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发表时间：
2012-12
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蛋白激酶C （PKC）自1982年首次被确定为肿瘤启动子磷酯的受体以来，一直是药物发现的一个诱人的靶点。虽然最初的治疗重点是癌症，但随着研究人员对PKC的八种传统和新型同工酶在健康和疾病中的作用有了更好的了解，其他疾病，包括糖尿病并发症、心力衰竭、心肌梗死、疼痛和双相情感障碍也成为了治疗目标。不幸的是，学术和制药方面的努力还没有导致一种专门针对PKC的新药获得批准。为什么PKC仍然是一个难以捉摸的药物靶点？这篇综述将简要介绍在开发PKC调节剂以解决未满足的临床需求方面的一些努力、挑战和机遇。
Protein kinase C (PKC) has been a tantalizing target for drug discovery ever since it was first identified as the receptor for the tumor promoter phorbol ester in 1982. Although initial therapeutic efforts focused on cancer, additional diseases, including diabetic complications, heart failure, myocardial infarction, pain and bipolar disease were targeted as researchers developed a better understanding of the roles that PKC’s eight conventional and novel isozymes play in health and disease. Unfortunately, both academic and pharmaceutical efforts have yet to result in the approval of a single new drug that specifically targets PKC. Why does PKC remain an elusive drug target? This review will provide a short account of some of the efforts, challenges and opportunities in developing PKC modulators to address unmet clinical needs.