An overview of kinase downregulators and recent advances in discovery approaches

doi:10.1038/s41392-021-00826-7

	An overview of kinase downregulators and recent advances in discovery approaches
	Wang, Beilei 1,2; Wu, Hong 1,2; Hu, Chen 1,2; Wang, Haizhen 3; Liu, Jing 1,2; Wang, Wenchao 1,2; Liu, Qingsong 1,2
刊名	SIGNAL TRANSDUCTION AND TARGETED THERAPY
	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.
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关键词	CHRONIC LYMPHOCYTIC-LEUKEMIA ; TYROSINE-KINASE ; SMALL-MOLECULE ; IN-VITRO ; IRREVERSIBLE INHIBITORS ; PROTEIN-DEGRADATION ; LIGAND INTERACTIONS ; TARGET ENGAGEMENT ; DRUG DISCOVERY ; CANCER MODELS
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
内容类型	期刊论文
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, Hefei Canc Hosp, Hefei 230031, Peoples R China 2.Chinese Acad Sci, Inst Hlth & Med Technol, Hefei Inst Phys Sci, Anhui Prov Key Lab Med Phys & Technol, 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).