Author/Authors :
Kristi Leonard، نويسنده , , Juan Jose Marugan، نويسنده , , Pierre Raboisson، نويسنده , , Raul Calvo، نويسنده , , Joan M. Gushue، نويسنده , , Holly K. Koblish، نويسنده , , Jennifer Lattanze، نويسنده , , Shuyuan Zhao، نويسنده , , Maxwell D. Cummings، نويسنده , , Mark R. Player، نويسنده , , Anna C. Maroney، نويسنده , , Tianbao Lu، نويسنده ,
Abstract :
The disruption of the p53-Hdm2 protein–protein interaction induces cell growth arrest and apoptosis. We have identified the 1,4-benzodiazepine-2,5-dione scaffold as a suitable template for inhibiting this interaction by binding to the Hdm2 protein. Several compounds have been made with improved potency, solubility, and cell-based activities.