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Protein kinases as targets for developing anticancer agents from marine organisms
Biochimica et Biophysica Acta (BBA) - General Subjects ( IF 2.8 ) Pub Date : 2020-10-08 , DOI: 10.1016/j.bbagen.2020.129759
Gan Qiao , Kangping Bi , Junhong Liu , Shousong Cao , Minghua Liu , Milica Pešić , Xiukun Lin

Protein kinases play a fundamental role in the intracellular transduction because of their ability to phosphorylate plethora of proteins. Over the past three decades, numerous protein kinase inhibitors have been identified and are being used clinically successfully. The biodiversity of marine organisms provides a rich source for the discovery and development of novel anticancer agents in the treatment of human malignancies and a lot of bioactive ingredients from marine organisms display anticancer effects by affecting the protein kinases-mediated pathways. In the present mini-review, anticancer compounds from marine source were reviewed and discussed in context of their targeted pathways associated with protein kinases and the progress of these compounds as anticancer agents in recent five years were emphasized. The molecular entities and their modes of actions were presented. We focused on protein kinases-mediated signaling pathways including PI3K/Akt/mTOR, p38 MAPK, and EGFR. The marine compounds targeting special pathways of protein kinases were highlighted. We have also discussed the existing challenges and prospects related to design and development of novel protein kinase inhibitors from marine sources.



中文翻译:

蛋白激酶作为开发海洋生物抗癌剂的靶标

蛋白激酶由于其使过多的蛋白磷酸化的能力而在细胞内转导中起基本作用。在过去的三十年中,已经发现了许多蛋白激酶抑制剂,并已在临床上成功使用。海洋生物的生物多样性为治疗人类恶性肿瘤的新型抗癌药的发现和开发提供了丰富的资源,并且海洋生物的许多生物活性成分通过影响蛋白激酶介导的途径显示出抗癌作用。在本小型综述中,对海洋来源的抗癌化合物与蛋白激酶相关的靶向途径进行了综述和讨论,并着重强调了这些化合物作为抗癌剂在最近五年中的进展。介绍了分子实体及其作用方式。我们专注于蛋白激酶介导的信号通路,包括PI3K / Akt / mTOR,p38 MAPK和EGFR。强调了针对蛋白质激酶特殊途径的海洋化合物。我们还讨论了与来自海洋的新型蛋白激酶抑制剂的设计和开发有关的现有挑战和前景。

更新日期:2020-10-13
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