LaValle Courtney R, George Kara M, Sharlow Elizabeth R, Lazo John S, Wipf Peter, Wang Q Jane
Department of Pharmacology and Chemical Biology, University of Pittsburgh, Pittsburgh, PA 15261, USA.
Biochim Biophys Acta. 2010 Dec;1806(2):183-92. doi: 10.1016/j.bbcan.2010.05.003. Epub 2010 May 24.
Protein kinase D is a novel family of serine/threonine kinases and diacylglycerol receptors that belongs to the calcium/calmodulin-dependent kinase superfamily. Evidence has established that specific PKD isoforms are dysregulated in several cancer types, and PKD involvement has been documented in a variety of cellular processes important to cancer development, including cell growth, apoptosis, motility, and angiogenesis. In light of this, there has been a recent surge in the development of novel chemical inhibitors of PKD. This review focuses on the potential of PKD as a chemotherapeutic target in cancer treatment and highlights important recent advances in the development of PKD inhibitors.
蛋白激酶D是丝氨酸/苏氨酸激酶和二酰基甘油受体的一个新家族,属于钙/钙调蛋白依赖性激酶超家族。有证据表明,特定的蛋白激酶D亚型在几种癌症类型中表达失调,并且在对癌症发展至关重要的各种细胞过程中,包括细胞生长、凋亡、迁移和血管生成,都有蛋白激酶D参与的记录。鉴于此,最近新型蛋白激酶D化学抑制剂的研发激增。本综述重点关注蛋白激酶D作为癌症治疗中化疗靶点的潜力,并突出了蛋白激酶D抑制剂研发方面的重要最新进展。