Dept. of Pharmacology, Univ. of California at San Diego, La Jolla, 92093, USA.
Am J Physiol Endocrinol Metab. 2010 Mar;298(3):E395-402. doi: 10.1152/ajpendo.00477.2009. Epub 2009 Nov 24.
Nestled at the tip of a branch of the kinome, protein kinase C (PKC) family members are poised to transduce signals emanating from the cell surface. Cell membranes provide the platform for PKC function, supporting the maturation of PKC through phosphorylation, its allosteric activation by binding specific lipids, and, ultimately, promoting the downregulation of the enzyme. These regulatory mechanisms precisely control the level of signaling-competent PKC in the cell. Disruption of this regulation results in pathophysiological states, most notably cancer, where PKC levels are often grossly altered. This review introduces the PKC family and then focuses on recent advances in understanding the cellular regulation of its diacylglycerol-regulated members.
PKC 家族成员位于激酶组的一个分支的尖端,随时准备转导来自细胞膜表面的信号。细胞膜为 PKC 功能提供了平台,通过磷酸化支持 PKC 的成熟,通过结合特定脂质的变构激活,最终促进酶的下调。这些调节机制精确地控制了细胞中具有信号转导能力的 PKC 的水平。这种调节的破坏导致了病理生理状态,最明显的是癌症,其中 PKC 的水平经常发生明显改变。本综述介绍了 PKC 家族,然后重点介绍了最近在理解其甘油二酯调节成员的细胞调节方面的进展。