Open AccessDiscovery of Potent and Selective p53-MDM2 Protein–Protein Interaction Inhibitors as Anticancer Drugs
Author(s) -
Philipp Holzer
Publication year - 2017
Publication title -
chimia
Language(s) - English
Resource type - Journals
SCImago Journal Rank - 0.387
H-Index - 55
eISSN - 2673-2424
pISSN - 0009-4293
DOI - 10.2533/chimia.2017.716
Subject(s) - pharmacophore , mdm2 , in vivo , drug discovery , computational biology , in vitro , pharmacology , chemistry , medicine , bioinformatics , biology , biochemistry , gene , genetics
As a result of our persistent efforts to discover novel inhibitors of the p53-MDM2 protein–protein interaction useful for the treatment of cancer, the potent and selective MDM2 inhibitors NVP-CGM097 and NVP-HDM201 with excellent in vitro and in vivo profile were selected as clinical candidates and are currently in phase 1 clinical development. This short review article provides a summary of the program history, the applied pharmacophore model and the discovery story of these novel p53-MDM2 inhibitor investigational drugs.