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靶向蛋白激酶D的小分子抑制剂:一种潜在的治疗策略。

Small-Molecule Inhibitor Targeting Protein Kinase D: A Potential Therapeutic Strategy.

作者信息

Lv Die, Chen Hongli, Feng Yun, Cui Bomiao, Kang Yingzhu, Zhang Ping, Luo Min, Chen Jiao

机构信息

State Key Laboratory of Oral Diseases, National Clinical Research Center for Oral Diseases, West China Hospital of Stomatology, Sichuan University, Chengdu, China.

出版信息

Front Oncol. 2021 Jun 24;11:680221. doi: 10.3389/fonc.2021.680221. eCollection 2021.

Abstract

The protein kinase D (PKD) family is a family of serine-threonine kinases that are members of the calcium/calmodulin-dependent kinase (CaMK) superfamily. PKDs have been increasingly implicated in multiple pivotal cellular processes and pathological conditions. PKD dysregulation is associated with several diseases, including cancer, inflammation, and obesity. Over the past few years, small-molecule inhibitors have emerged as alternative targeted therapy with fewer adverse side effects than currently available chemotherapy, and these specifically targeted inhibitors limit non-specific toxicities. The successful development of PKD inhibitors would significantly suppress the growth and proliferation of various cancers and inhibit the progression of other diseases. Various PKD inhibitors have been studied in the preclinical setting. In this context, we summarize the PKD inhibitors under investigation and their application for different kinds of diseases.

摘要

蛋白激酶D(PKD)家族是丝氨酸 - 苏氨酸激酶家族,属于钙/钙调蛋白依赖性激酶(CaMK)超家族成员。PKD越来越多地参与多种关键细胞过程和病理状况。PKD失调与多种疾病相关,包括癌症、炎症和肥胖症。在过去几年中,小分子抑制剂已成为一种替代靶向疗法,其副作用比目前可用的化疗更少,并且这些特异性靶向抑制剂限制了非特异性毒性。PKD抑制剂的成功开发将显著抑制各种癌症的生长和增殖,并抑制其他疾病的进展。各种PKD抑制剂已在临床前环境中进行了研究。在此背景下,我们总结了正在研究的PKD抑制剂及其在不同疾病中的应用。

https://cdn.ncbi.nlm.nih.gov/pmc/blobs/98fc/8263921/39635ce7c72e/fonc-11-680221-g001.jpg

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