期刊
BIOORGANIC & MEDICINAL CHEMISTRY LETTERS
卷 23, 期 13, 页码 3802-3805出版社
PERGAMON-ELSEVIER SCIENCE LTD
DOI: 10.1016/j.bmcl.2013.04.094
关键词
MDM2; MDMX; p53 Protein; HTS; Microarray technology
资金
- MEXT, Japan
- Grants-in-Aid for Scientific Research [23510287, 24659046] Funding Source: KAKEN
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. (C) 2013 Elsevier Ltd. All rights reserved.
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