| 引用本文: | 牟杰,李龙宝,孟思寒,裴冬生.Ⅱ型p21激活激酶在肿瘤中的调节作用及其抑制剂研究进展[J].中国现代应用药学,2021,38(20):2608-2615. |
| MOU Jie,LI Longbao,MENG Sihan,PEI Dongsheng.Research Progress of Regulatory role of Group Ⅱ p21-activated kinases in cancer and the development of the inhibitors[J].Chin J Mod Appl Pharm(中国现代应用药学),2021,38(20):2608-2615. |
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| Ⅱ型p21激活激酶在肿瘤中的调节作用及其抑制剂研究进展 |
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牟杰1,2, 李龙宝1, 孟思寒2, 裴冬生3
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1.徐州医科大学, 药学院, 江苏 徐州 221004;2.徐州医科大学, 江苏省新药研究与临床药学重点实验室, 江苏 徐州 221004;3.徐州医科大学, 病理学教研室, 江苏 徐州 221004
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| 摘要: |
| p21激活激酶（p21-activated kinases，PAKs）是小GTP酶Rho家族的成员Rac和Cdc42的下游靶蛋白，参与调节细胞骨架重构和细胞运动等多种生物功能。PAKs家族分为I型PAKs（PAK1~3）和Ⅱ型PAKs（PAK4~6），其中Ⅱ型PAKs在多种肿瘤中高表达，并与肿瘤的发生和预后密切相关。Ⅱ型PAKs对肿瘤的增殖、凋亡、侵袭和转移起到重要的调控作用，成为有研发前途的抗肿瘤靶点。本文从Ⅱ型PAKs在肿瘤领域的研究进展及其抑制剂在肿瘤中的作用进行综述，期望为开发选择性Ⅱ型PAKs抑制剂提供参考。 |
| 关键词: Ⅱ型p21激活激酶 肿瘤 抑制剂 亚型选择性 |
| DOI：10.13748/j.cnki.issn1007-7693.2021.20.024 |
| 分类号:R966 |
| 基金项目:国家自然科学基金项目（81872080，81572349）；江苏省自然科学基金项目（BK20181148）；徐州市推动科技创新项目（KC20245）；江苏省研究生科研创新计划（KYCX20_2510）；江苏省高等学校大学生实践创新训练计划（201910313073Y，201910313098H） |
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| Research Progress of Regulatory role of Group Ⅱ p21-activated kinases in cancer and the development of the inhibitors |
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MOU Jie1,2, LI Longbao1, MENG Sihan2, PEI Dongsheng3
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1.Xuzhou Medical University, School of Pharmacy, Xuzhou 221004, China;2.Xuzhou Medical University, Jiangsu Key Laboratory of New drug and Clinical Pharmacy, Xuzhou 221004, China;3.Xuzhou Medical University, Department of Pathology, Xuzhou 221004, China
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| Abstract: |
| p21-activated kinases(PAKs) are important downstream effector molecules of the small G protein Rho family Rac and Cdc42 which involved in regulating various biological functions such as cytoskeletal remodeling and cell movement. The human PAKs family can be divided into two types:type I PAKs(PAK1-3) and type Ⅱ PAKs(PAK4-6), in which type Ⅱ PAKs are highly expressed in various tumors and are closely related to the occurrence and prognosis of tumors. Type Ⅱ PAKs play the vital role in the regulation of tumor proliferation, apoptosis, invasion and metastasis, and become a promising anti-tumor target. Herein, the research progress of type Ⅱ PAKs in oncology and the roles of their inhibitors in cancer were reviewed, expecting to develop selective type Ⅱ PAKs inhibitors. |
| Key words: group Ⅱ p21-activated kinase tumor inhibitor subtype selectivity |
