166959-67-7Relevant articles and documents
Terphenyl-based helical mimetics that disrupt the p53/HDM2 interaction
Yin, Hang,Lee, Gui-In,Hyung, Soon Park,Payne, Gregory A.,Rodriguez, Johanna M.,Sebti, Said M.,Hamilton, Andrew D.
, p. 2704 - 2707 (2007/10/03)
(Chemical Equation Presented) HDM2 regulates p53 by binding to its transactivation domain and promoting its ubiquitin-dependent degradation. Crystallographic analysis of the HDM2/p53 complex revealed that three hydrophobic residues (F19, W23, L26) along one face of the p53 helical peptide are essential for binding (see picture). Terphenyl-based antagonists mimic the α-helical region of p53 and disrupt HDM2/p53 complexation.