Discovery of a novel class of highly potent inhibitors of the p53-MDM2 interaction by structure-based design starting from a conformational argument.

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作者： Pascal,Furet ^[1] ; Keiichi,Masuya ^[2] ; Joerg,Kallen ^[2] ; Thérèse,Stachyra-Valat ^[2] ; Stephan,Ruetz ^[2] ; Vito,Guagnano ^[2] ; Philipp,Holzer ^[2] ; Robert,Mah ^[2] ; Stefan,Stutz ^[2] ; Andrea,Vaupel ^[2] ; Patrick,Chène ^[2] ; Sébastien,Jeay ^[2] ; Achim,Schlapbach ^[2]

作者单位： Novartis Institutes for BioMedical Research, WKL-136.P.12, CH-4002 Basel, Switzerland. Electronic address: pascal.furet@novartis.com. ^[1] Novartis Institutes for BioMedical Research, WKL-136.P.12, CH-4002 Basel, Switzerland. ^[2]

关键词 Anticancer agents Protein–protein interaction inhibitors Structure-based design p53–MDM2 inhibitors

主题词结晶学, X线(Crystallography, X-Ray);药物发现(Drug Discovery);荧光共振能量转移(Fluorescence Resonance Energy Transfer);分子构象(Molecular Conformation);原癌基因蛋白质c-mdm2(Proto-Oncogene Proteins c-mdm2);肿瘤抑制蛋白质p53(Tumor Suppressor Protein p53)

DOI 10.1016/j.bmcl.2016.08.010

PMID 27542305

发布时间 2017-11-22

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