Conformational control and regulation of the pseudokinase KSR via small molecule binding interactions.

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作者： Arthur,Chow ^[1] ; Zaigham M,Khan ^[1] ; William M,Marsiglia ^[1] ; Arvin C,Dar ^[2]

作者单位： Department of Oncological Sciences, Department of Pharmacological Sciences, The Tisch Cancer Institute, Mount Sinai Centre for Therapeutic Discovery, Icahn School of Medicine at Mount Sinai, New York, NY, United States. ^[1] Department of Oncological Sciences, Department of Pharmacological Sciences, The Tisch Cancer Institute, Mount Sinai Centre for Therapeutic Discovery, Icahn School of Medicine at Mount Sinai, New York, NY, United States. Electronic address: arvin.dar@mssm.edu. ^[2]

关键词 Activity-based probes Crystallization Interfacial sites KSR MEK Molecular glues Orthosteric site RAF SBDD Target engagement

主题词结合部位(Binding Sites);分子构象(Molecular Conformation);磷酰化(Phosphorylation);蛋白激酶类(Protein Kinases);原癌基因蛋白质c-raf(Proto-Oncogene Proteins c-raf);信号传导(Signal Transduction)

DOI 10.1016/bs.mie.2022.03.039

PMID 35525547

发布时间 2024-09-23

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