Martiny-Baron Georg, Fabbro Doriano
Novartis Institutes for Biomedical Research, Expertise Platform Kinases, Klybeckstr. 142, CH 4002 Basel, Switzerland.
Pharmacol Res. 2007 Jun;55(6):477-86. doi: 10.1016/j.phrs.2007.04.001. Epub 2007 Apr 21.
Protein kinases C (PKCs) are a family of serine/threonine kinases which are involved in tumor formation and progression. Although PKC over-expression has been shown to contribute to cell transformation, PKCs are not considered to be classical oncogenes which are activated by mutations, but considered as tumor promoters that enhance multiple cellular signaling pathways. Over the last two decades a lot of evidence has emerged demonstrating a role for various PKC isoforms in cancer. Small molecular weight inhibitors and antisense molecules have been developed, specifically targeting the calcium dependent classical isoforms of PKC. This review focuses on the role of classical PKCs in cancer and the results obtained by attempting to inhibit these enzymes to achieve a therapeutic benefit.
蛋白激酶C（PKCs）是一类丝氨酸/苏氨酸激酶家族，参与肿瘤的形成和进展。虽然已表明PKC的过表达有助于细胞转化，但PKCs不被认为是通过突变激活的经典癌基因，而是被视为增强多种细胞信号通路的肿瘤促进剂。在过去二十年中，大量证据表明各种PKC亚型在癌症中发挥作用。已经开发出小分子抑制剂和反义分子，专门针对PKC的钙依赖性经典亚型。本综述重点关注经典PKCs在癌症中的作用，以及试图抑制这些酶以获得治疗益处所取得的结果。
