Abstract
In this section, a novel approach for identifying MDM2-p53 and MDMX-p53 protein–protein interactions (PPIs) inhibitors by using chemically synthesized MDM2 and MDMX proteins has been established. MDM2 and MDMX are oncoproteins that negatively regulate the activity and stability of the tumor suppressor protein p53. The inhibitors of PPIs of MDM2-p53 and MDMX-p53 represent potential anticancer agents. Affinity-based chemical array screening is one of the efficient methods for identification of binding agents toward various pockets of proteins. To establish chemistry-based screening platform for identification of MDM2 and MDMX inhibitors, synthetic strategy of MDM2 and MDMX proteins and application of these proteins for chemical array screening were performed. MDM2 and MDMX proteins were prepared by Fmoc-based solid-phase peptide synthesis (SPPS), and binding candidates for them were identified from an in-house compound library by chemical array screening. The subsequent fluorescence polarization (FP) assay identified peptidic compounds that inhibited MDM2-p53 and MDMX-p53 interactions.
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