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A Highly Potent and Cellularly Active β‐Peptidic Inhibitor of the p53/hDM2 Interaction
Author(s) -
Hintersteiner Martin,
Kimmerlin Thierry,
Garavel Geraldine,
Schindler Thorsten,
Bauer Roman,
Meisner NicoleClaudia,
Seifert JanMarcus,
Uhl Volker,
Auer Manfred
Publication year - 2009
Publication title -
chembiochem
Language(s) - English
Resource type - Journals
SCImago Journal Rank - 1.05
H-Index - 126
eISSN - 1439-7633
pISSN - 1439-4227
DOI - 10.1002/cbic.200800803
Subject(s) - chemistry , stereochemistry , combinatorial chemistry
New and improved : The incorporation of a 6‐chlorotryptophan (6‐Cl‐Trp) into a β‐peptide (M)‐3 14 helix leads to a high‐affinity hDM2 inhibitor, as demonstrated by fluorescence fluctuation analysis at single molecule resolution. When conjugated to penetratin, the newly derived hDM2 binder specifically inhibits tumour cell growth in vitro.