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p53, the Guardian of the Genome

p53, often referred to as the "guardian of the genome," is a crucial tumor suppressor protein that regulates cell cycle progression, apoptosis, and DNA repair. Its role in maintaining genomic stability is paramount, as it activates DNA Damage Response (DDR) pathways upon detecting DNA damage. The DDR involves a series of signaling cascades that halt cell cycle progression, allowing time for DNA repair or triggering apoptosis if the damage is irreparable. 

Drug discovery efforts targeting p53 focus on restoring its tumor-suppressive functions, given that TP53 mutations are common in cancers. Key strategies include reactivating mutant p53 (e.g., APR-246), inhibiting the MDM2-p53 interaction to stabilize p53, and activating alternative pathways in p53-deficient cells. Additionally, mutant-specific small molecules and gene or immunotherapy approaches are being explored to counteract the effects of dysfunctional p53 in tumors. These approaches aim to harness or mimic p53’s role as a "guardian of the genome" in cancer therapy.

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The table below outlines our comprehensive assays for p53.  

Protein Assay Table

CategoryItem
Protein Productsp53 WT
p53 Y220C
p53 R175H
p53 R248W
p53 R273H
Biochemicalp53 Y220C/DNA HTRF Binding Assay
Biophysicalp53 Y220C/R175H/R248W TSA Assay
p53 WT/Y220C NanoDSF Assay
p53 WT/Y220C SPR Assay
p53 Y220C MS-based Covalent Binding Assay
Cell-basedNUGC-3 P21RE Reporter Assay
NUGC-3 TP53 KO P21RE Reporter Assay
NUGC-3 p53RE Reporter Assay
GSH/GSSG assay using TNB
SKOV3 TP53 P21RE Reporter Assay
Cell Viability Assay
CETSA Assay
P21/MDM2 qPCR Assay
Cell PanelCell lines with endogenous p53 mutations
TP53 KO Cell Lines
In VivoNUGC3 BALB/c nude mice CDX modeling

Our capabilities extend to systematically supporting the integrated drug discovery process, particularly for challenging-to-drug targets in oncology and immunology. Feel free to connect with our experts to explore how we can assist with your projects.


Learn more from our poster presented at the 7th Annual DDR Inhibitor Summit

A Comprehensive p53 Drug Discovery Platform: From Target-Base Assays to In Vivo Models 

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