Activators and Inhibitors of Protein Kinase C (PKC): Their Applications in Clinical Trials.

Activators and Inhibitors of Protein Kinase C (PKC): Their Applications in Clinical Trials.
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DOI:
10.3390/pharmaceutics13111748
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发表时间:
2021-10-20
期刊:
影响因子:
5.4
通讯作者:
Kang JH
Kang JH
中科院分区:
医学2区
文献类型:
--
作者:
Kawano T;Inokuchi J;Eto M;Murata M;Kang JH

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蛋白激酶C(PKC)是磷脂依赖性丝氨酸/苏氨酸激酶的一个家族,根据其结构和活化特征可分为三个亚家族:常规或经典PKC同工酶(cPKC; α、βI、βII和γ)、新型或非经典PKC同工酶(nPKC; δ、ε、η和θ)和非典型PKC同工酶(aPKC; α、β I和λ)。PKC抑制剂和激活剂用于了解PKC介导的细胞内信号传导途径,并用于诊断和治疗各种PKC相关疾病,如癌症,神经系统疾病,心血管疾病和感染。许多PKC抑制剂在癌症中的临床试验显示没有显著的临床益处,这意味着设计单独靶向PKC的癌症治疗策略存在局限性。本文就蛋白激酶C的激活剂和抑制剂及其临床应用作一综述。
Protein kinase C (PKC), a family of phospholipid-dependent serine/threonine kinase, is classed into three subfamilies based on their structural and activation characteristics: conventional or classic PKC isozymes (cPKCs; α, βI, βII, and γ), novel or non-classic PKC isozymes (nPKCs; δ, ε, η, and θ), and atypical PKC isozymes (aPKCs; ζ, ι, and λ). PKC inhibitors and activators are used to understand PKC-mediated intracellular signaling pathways and for the diagnosis and treatment of various PKC-associated diseases, such as cancers, neurological diseases, cardiovascular diseases, and infections. Many clinical trials of PKC inhibitors in cancers showed no significant clinical benefits, meaning that there is a limitation to design a cancer therapeutic strategy targeting PKC alone. This review will focus on the activators and inhibitors of PKC and their applications in clinical trials.
DOI: 10.1002/ajh.21449
发表时间: 2009-08
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