Deka Suman J, Trivedi Vishal
Department of Biosciences and Bioengineering, Indian Institute of Technology-Guwahati, Guwahati-781039, Assam, India.
Curr Drug Discov Technol. 2019;16(2):135-147. doi: 10.2174/1570163815666180219113614.
PKC is a family of serine-threonine kinases which play crucial roles in the regulation of important signal transduction pathways in mammalian cell-biology. These enzymes are themselves regulated by various molecules that can serve as ligands to the regulatory domains and translocate PKC to membrane for activity. The role of PKC in the modulation of both proliferative and apoptotic signaling in cancer has become a subject of immense interest after it was discovered that PKC regulates a myriad of enzymes and transcription factors involved in carcinogenic signaling. Therefore, PKC has served as an attractive target for the development of newer generation of anti-cancer drugs. The following review discusses the potential of PKC to be regarded as a target for anti-cancer therapy. We also review all the molecules that have been discovered so far to be regulators/activators/inhibitors of PKC and also how far these molecules can be considered as potential candidates for anti-cancer drug development based on PKC.
蛋白激酶C（PKC）是丝氨酸 - 苏氨酸激酶家族，在哺乳动物细胞生物学中重要信号转导通路的调节中发挥关键作用。这些酶本身受各种分子调节，这些分子可作为调节域的配体，并使PKC转位至细胞膜以发挥活性。自从发现PKC调节众多参与致癌信号传导的酶和转录因子后，PKC在癌症增殖和凋亡信号调节中的作用已成为一个备受关注的课题。因此，PKC已成为新一代抗癌药物开发的有吸引力的靶点。以下综述讨论了PKC作为抗癌治疗靶点的潜力。我们还综述了迄今为止发现的所有作为PKC调节剂/激活剂/抑制剂的分子，以及基于PKC这些分子在多大程度上可被视为抗癌药物开发的潜在候选物。
