An overview of kinase downregulators and recent advances in discovery approaches
文献类型：期刊论文
| 作者 | Wang, Beilei1,2; Wu, Hong1,2 ; Hu, Chen1,2; Wang, Haizhen3; Liu, Jing1,2; Wang, Wenchao1,2; Liu, Qingsong1,2
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| 刊名 | SIGNAL TRANSDUCTION AND TARGETED THERAPY
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| 出版日期 | 2021-12-20 |
| 卷号 | 6 |
| ISSN号 | 2095-9907 |
| DOI | 10.1038/s41392-021-00826-7 |
| 通讯作者 | Liu, Qingsong(qsliu97@hmfl.ac.cn) |
| 英文摘要 | Since the clinical approval of imatinib, the discovery of protein kinase downregulators entered a prosperous age. However, challenges still exist in the discovery of kinase downregulator drugs, such as the high failure rate during development, side effects, and drug-resistance problems. With the progress made through multidisciplinary efforts, an increasing number of new approaches have been applied to solve the above problems during the discovery process of kinase downregulators. In terms of in vitro and in vivo drug evaluation, progress was also made in cellular and animal model platforms for better and more clinically relevant drug assessment. Here, we review the advances in drug design strategies, drug property evaluation technologies, and efficacy evaluation models and technologies. Finally, we discuss the challenges and perspectives in the development of kinase downregulator drugs. |
| WOS关键词 | CHRONIC LYMPHOCYTIC-LEUKEMIA ; TYROSINE-KINASE ; SMALL-MOLECULE ; IN-VITRO ; IRREVERSIBLE INHIBITORS ; PROTEIN-DEGRADATION ; LIGAND INTERACTIONS ; TARGET ENGAGEMENT ; DRUG DISCOVERY ; CANCER MODELS |
| 资助项目 | National Natural Science Foundation of China[81903650] ; Natural Science Foundation of Anhui Province[1808085MH274] ; Natural Science Foundation of Anhui Province[2008085MH274] ; China Postdoctoral Science Foundation[2020M671916] ; China Postdoctoral Science Foundation[2019M652057] ; Postdoctoral Science Foundation of Anhui Province[2019B326] ; Postdoctoral Science Foundation of Anhui Province[2019B300] ; Frontier Science Key Research Program of CAS[QYZDB-SSW-SLH037] ; CASHIPS Director's Found[BJPY2019A03] ; CASHIPS Director's Found[YZJJZX202011] |
| WOS研究方向 | Biochemistry & Molecular Biology ; Cell Biology |
| 语种 | 英语 |
| 出版者 | SPRINGERNATURE |
| WOS记录号 | WOS:000731514300002 |
| 资助机构 | National Natural Science Foundation of China ; Natural Science Foundation of Anhui Province ; China Postdoctoral Science Foundation ; Postdoctoral Science Foundation of Anhui Province ; Frontier Science Key Research Program of CAS ; CASHIPS Director's Found |
| 源URL | [http://ir.hfcas.ac.cn:8080/handle/334002/126976]  |
| 专题 | 中国科学院合肥物质科学研究院 |
| 通讯作者 | Liu, Qingsong |
| 作者单位 | 1.Chinese Acad Sci, Inst Hlth & Med Technol, Hefei Inst Phys Sci, Anhui Prov Key Lab Med Phys & Technol, Hefei 230031, Peoples R China 2.Chinese Acad Sci, Hefei Canc Hosp, Hefei 230031, Peoples R China 3.Hefei PreceDo Pharmaceut Co Ltd, Hefei 230088, Anhui, Peoples R China |
| 推荐引用方式 GB/T 7714 | Wang, Beilei,Wu, Hong,Hu, Chen,et al. An overview of kinase downregulators and recent advances in discovery approaches[J]. SIGNAL TRANSDUCTION AND TARGETED THERAPY,2021,6. |
| APA | Wang, Beilei.,Wu, Hong.,Hu, Chen.,Wang, Haizhen.,Liu, Jing.,...&Liu, Qingsong.(2021).An overview of kinase downregulators and recent advances in discovery approaches.SIGNAL TRANSDUCTION AND TARGETED THERAPY,6. |
| MLA | Wang, Beilei,et al."An overview of kinase downregulators and recent advances in discovery approaches".SIGNAL TRANSDUCTION AND TARGETED THERAPY 6(2021). |
入库方式： OAI收割
来源：合肥物质科学研究院
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