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Leveraging the multivalent p53 peptide-MdmX interaction to guide the improvement of small molecule inhibitors

Overexpressed Mdm2 and its 7homolog MdmX impair p53 activity in many cancers. Small molecules mimicking a p53 peptide can effectively inhibit Mdm2 but not MdmX. Here, we show a strategy for improving lead compounds for Mdm2 and MdmX inhibition based on the multivalency of the p53 peptide. Crystal st...

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Detalles Bibliográficos
Autores principales: Cheng, Xiyao, Chen, Rong, Zhou, Ting, Zhang, Bailing, Li, Zichun, Gao, Meng, Huang, Yongqi, Liu, Huili, Su, Zhengding
Formato: Online Artículo Texto
Lenguaje:English
Publicado: Nature Publishing Group UK 2022
Materias:
Acceso en línea:https://www.ncbi.nlm.nih.gov/pmc/articles/PMC8885691/
https://www.ncbi.nlm.nih.gov/pubmed/35228542
http://dx.doi.org/10.1038/s41467-022-28721-x