Allosteric inhibition of antiapoptotic MCL-1

Identification of an allosteric mechanism disrupting the antiapoptotic BH3 binding activity of MCL-1 offers a new approach for targeting the apoptotic resistance of human cancers. MCL-1 is an antiapoptotic BCL-2 family protein that has emerged as a major pathogenic factor in human cancer. Like BCL-2...

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Veröffentlicht in:	Nature structural & molecular biology 2016-06, Vol.23 (6), p.600-607
Hauptverfasser:	Lee, Susan, Wales, Thomas E, Escudero, Silvia, Cohen, Daniel T, Luccarelli, James, Gallagher, Catherine G, Cohen, Nicole A, Huhn, Annissa J, Bird, Gregory H, Engen, John R, Walensky, Loren D
Format:	Artikel
Sprache:	eng
Schlagworte:	13/1 13/2 13/95 631/45/612/1243 631/80/82/23 82/58 82/80 82/83 96/47 Allosteric Regulation - drug effects Animals Apoptosis Apoptosis - drug effects bcl-2-Associated X Protein - chemistry bcl-2-Associated X Protein - metabolism Biochemistry Biological Microscopy Cancer Carcinogenesis Cell Line Gene expression Genetic aspects Health aspects Humans Life Sciences Membrane Biology Mice Molecular biology Molecular Dynamics Simulation Mutagenesis Myeloid Cell Leukemia Sequence 1 Protein - chemistry Myeloid Cell Leukemia Sequence 1 Protein - genetics Myeloid Cell Leukemia Sequence 1 Protein - metabolism Neoplasms - genetics Neoplasms - metabolism Point Mutation Properties Protein binding Protein Binding - drug effects Protein Conformation - drug effects Protein Domains Protein Structure Proteins Proto-Oncogene Proteins c-bcl-2 - chemistry Proto-Oncogene Proteins c-bcl-2 - metabolism Small Molecule Libraries - pharmacology Tumor proteins
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