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Discovery, X-ray structure and CPP-conjugation enabled uptake of p53/MDM2 macrocyclic peptide inhibitors

Mouse double minute 2 homolog (MDM2, Hdm2) is an important negative regulator of the tumor suppressor p53. Using a mRNA based display technique to screen a library of >10(12)in vitro-translated cyclic peptides, we have identified a macrocyclic ligand that shows picomolar potency on MDM2. X-Ray cr...

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Detalles Bibliográficos
Autores principales: Schneider, Anselm F. L., Kallen, Joerg, Ottl, Johannes, Reid, Patrick C., Ripoche, Sebastien, Ruetz, Stephan, Stachyra, Therese-Marie, Hintermann, Samuel, Dumelin, Christoph E., Hackenberger, Christian P. R., Marzinzik, Andreas L.
Formato: Online Artículo Texto
Lenguaje:English
Publicado: RSC 2021
Materias:
Acceso en línea:https://www.ncbi.nlm.nih.gov/pmc/articles/PMC8637822/
https://www.ncbi.nlm.nih.gov/pubmed/34977581
http://dx.doi.org/10.1039/d1cb00056j