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Updated: May 9, 2026

Yeast As a Chassis for Developing Functional Assays to Study Human P53
14:57

Yeast As a Chassis for Developing Functional Assays to Study Human P53

Published on: August 4, 2019

Disruption of focal adhesion kinase and p53 interaction with small molecule compound R2 reactivated p53 and blocked

Vita M Golubovskaya, Baotran Ho, Min Zheng

    BMC Cancer
    |July 12, 2013
    PubMed
    Abstract

    Insights

    A novel small molecule, Roslin 2 (R2), disrupts the FAK-p53 interaction, reactivating p53. This approach shows promise for targeted cancer therapy by decreasing cancer cell viability and tumor growth.

    Area of Science:

    • Oncology
    • Molecular Biology
    • Drug Discovery

    Background:

    • Focal Adhesion Kinase (FAK) is a key regulator of cancer cell survival and metastasis.
    • The interaction between FAK and p53 is crucial in cancer progression.

    Purpose of the Study:

    • To identify small molecules that disrupt the FAK-p53 interaction.
    • To evaluate the therapeutic potential of such molecules in cancer treatment.

    Main Methods:

    • Computer modeling was used to predict peptide structures and dock compounds to the FAK-p53 interaction site.
    • In vitro and in vivo assays were performed using isogenic HCT116 cell lines and xenografts.
    • Dual-luciferase assays assessed p53 transcriptional activity.

    Main Results:

    • Roslin 2 (R2) was identified as a compound that binds FAK, disrupts FAK-p53 interaction, and decreases cancer cell viability and clonogenicity in a p53-dependent manner.
    • R2 increased p53 transcriptional activity and the expression of p53 targets (p21, Mdm-2, Bax).
    • In vivo, R2 decreased tumor growth and upregulated p21 in HCT116 p53+/+ xenografts, and sensitized cells to chemotherapy.

    Conclusions:

    • Disruption of the FAK-p53 interaction with R2 reactivates p53 in cancer cells.
    • This novel small molecule strategy offers a potential new avenue for FAK-p53 targeted cancer therapy.

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