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Targeted covalent inhibitors of MDM2 using electrophile-bearing stapled peptides.
- Source :
-
Chemical communications (Cambridge, England) [Chem Commun (Camb)] 2019 Jul 14; Vol. 55 (55), pp. 7914-7917. Date of Electronic Publication: 2019 Jun 21. - Publication Year :
- 2019
-
Abstract
- Herein, we describe the development of a novel staple with an electrophilic warhead to enable the generation of stapled peptide covalent inhibitors of the p53-MDM2 protein-protein interaction (PPI). The peptide developed showed complete and selective covalent binding resulting in potent inhibition of p53-MDM2 PPI.
- Subjects :
- Binding Sites drug effects
Enzyme Inhibitors chemical synthesis
Humans
Lysine chemistry
Molecular Dynamics Simulation
Muramidase chemistry
Peptides, Cyclic chemical synthesis
Proto-Oncogene Proteins c-mdm2 chemistry
Saccharomyces cerevisiae chemistry
Sulfones chemical synthesis
Enzyme Inhibitors chemistry
Peptides, Cyclic chemistry
Proto-Oncogene Proteins c-mdm2 antagonists & inhibitors
Sulfones chemistry
Subjects
Details
- Language :
- English
- ISSN :
- 1364-548X
- Volume :
- 55
- Issue :
- 55
- Database :
- MEDLINE
- Journal :
- Chemical communications (Cambridge, England)
- Publication Type :
- Academic Journal
- Accession number :
- 31225847
- Full Text :
- https://doi.org/10.1039/c9cc04022f