An Update on MDMX and Dual MDM2/X Inhibitors

作者: Margarida Espadinha , Valentina Barcherini , Elizabeth A. Lopes , Maria M.M. Santos

DOI: 10.2174/1568026618666180604080119

关键词: P53 statusMdm2ChemistryP53 reactivationSmall moleculeGeneSuppressorMutationMDMXCancer research

摘要: The tumor suppressor protein p53 is inactivated in all types of human cancers, either by negative regulation, mutation or deletion its gene. Specifically, tumors that retain wild-type (wt) status, interaction with regulators, such as MDM2 and MDMX. These two proteins are found to be overexpressed several different the restoration activity inhibition these now considered an important approach for cancer treatment. first studies using this strategy reactivate wt were focused on development small molecules could inhibit MDM2. In way, liberated act again a suppressor. From studies, nine have reached clinical trials. More recently, MDMX was also identified therapeutic target efficiently p53, it that, full reactivation, dual required. review we will focus most recent advances discovery novel stapled peptides selective inhibitors MDM2/X inhibitors.

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