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An overview of kinase downregulators and recent advances in discovery approaches

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摘要 Since the dinical 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 bee n applied to solve the above problems duri ng the discovery process of kin ase down regulators.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 assessme nt.Here,we review the adva nces in drug desig n strategies,drug property evaluatio n tech no logies,and efficacy evaluatio n models and tech no logies.Finally,we discuss the challenges and perspectives in the development of kin ase down regulator drugs.
出处 《Signal Transduction and Targeted Therapy》 SCIE CSCD 2022年第1期112-130,共19页 信号转导与靶向治疗(英文)
基金 This work was supported by the National Natural Science Foundation of China(Grant No.81903650) the Natural Science Foundation of Anhui Province(Grant Nos.1808085MH274 and 2008085MH274) the China Postdoctoral Science Foundation(Grant Nos.2020M671916 and 2019M652057) the Postdoctoral Science Foundation of Anhui Province(Grant Nos.2019B326 and 2019B300) the Frontier Science Key Research Program of CAS(Grant No.QYZDB-SSW-SLH037) the CASHIPS Directors Found(Grant Nos.BJPY2019A03 and YZJJZX202011).
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