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Affinity-based screening of MDM2/MDMX-p53 interaction inhibitors by chemical array: identification of novel peptidic inhibitors.

Abstract：

:MDM2 and MDMX are oncoproteins that negatively regulate the activity and stability of the tumor suppressor protein p53. The inhibitors of protein-protein interactions (PPIs) of MDM2-p53 and MDMX-p53 represent potential anticancer agents. In this study, a novel approach for identifying MDM2-p53 and MDMX-p53 PPI inhibitor candidates by affinity-based screening using a chemical array has been established. A number of compounds from an in-house compound library, which were immobilized onto a chemical array, were screened for interaction with fluorescence-labeled MDM2 and MDMX proteins. The subsequent fluorescent polarization assay identified several compounds that inhibited MDM2-p53 and MDMX-p53 interactions.

journal_name

Bioorg Med Chem Lett

journal_title

Bioorganic & medicinal chemistry letters

authors

Noguchi T,Oishi S,Honda K,Kondoh Y,Saito T,Kubo T,Kaneda M,Ohno H,Osada H,Fujii N

doi

10.1016/j.bmcl.2013.04.094

subject

Has Abstract

pub_date

2013-07-01 00:00:00

pages

3802-5

issue

13

eissn

0960-894X

issn

1464-3405

pii

S0960-894X(13)00595-7

journal_volume

23

pub_type

杂志文章

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