| Literature DB >> 27907876 |
Ewa Surmiak1, Constantinos G Neochoritis2, Bogdan Musielak1, Aleksandra Twarda-Clapa3, Katarzyna Kurpiewska1, Grzegorz Dubin3, Carlos Camacho4, Tad A Holak5, Alexander Dömling6.
Abstract
Using the computational pharmacophore-based ANCHOR.QUERY platform a new scaffold was discovered. Potent compounds evolved inhibiting the protein-protein interaction p53-MDM2. An extensive SAR study was performed based on our four-point pharmacophore model, yielding derivatives with affinity to MDM2 in the nanomolar range. Their binding affinity with MDM2 was evaluated using both fluorescence polarization (FP) assay and 2D-NMR-HSQC experiments.Entities:
Mesh：
Substances：
Year: 2016 PMID： 27907876 DOI： 10.1016/j.ejmech.2016.11.029
Source DB: PubMed Journal: Eur J Med Chem ISSN： 0223-5234 Impact factor: 6.514