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Prof. Brian J. Smith, Dr. Erinna F. Lee, James W. Checco, Marco Evangelista, Prof. Samuel H. Gellman and Dr. W. Douglas Fairlie Structure-Guided Rational Design of α/β-Peptide Foldamers with High Affinity for BCL-2 Family Prosurvival Proteins ChemBioChem 14

Version of Record online: 8 AUG 2013 | DOI: 10.1002/cbic.201300351

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Killer design: A BH3-mimetic oligomer composed of α- and β-amino acids was used as a starting point for computational design approaches to improve binding affinity for antiapoptotic targets. A 250-fold gain in affinity for Mcl-1 was achieved through simple modification of side chains and configuration of α residues.

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