Discover Community Create You

Loading publication...

Noodle always counts identifier-free feature events for service operation. With your permission, Google Analytics can also estimate audience and engagement. Search text, publication identifiers, cookies, IP addresses and browser fingerprints are never included in Noodle's first-party event counters.

Privacy details

Article

PRIMA-1(MET)/APR-246 targets mutant forms of p53 family members p63 and p73.

Oncogene - 9 Dec 2010

Rökaeus N, Shen J, Eckhardt I, Bykov V J N, Wiman K G, Wilhelm M T

Abstract excerpt

The low molecular weight compound PRIMA-1 and the structural analog PRIMA-1(MET), also named APR-246, reactivate mutant p53 through covalent binding to the core domain and induce apoptosis in tumor cells. Here, we asked whether PRIMA-1(MET)/APR-246 can rescue mutant forms of the p53 family members p63 and p73 that share high sequence homology with p53. We found that PRIMA-1(MET)/APR-246 can restore the...

Read the complete abstract on PubMed

Topics

Share this publication in a Topic to start or enrich a Post.

Share to Antineoplastic Agents
Share to Aza Compounds
Share to Bridged Bicyclo Compounds, Heterocyclic

Methodology Data sources Editorial policy Privacy About Contact Helena Bioinformatics

Share to Cyclin-Dependent Kinase Inhibitor p21

Share to Proto-Oncogene Proteins c-bcl-2

Share to Trans-Activators

Share to Tumor Protein p73

Share to Tumor Suppressor Proteins

Source

Identifiers

PMID: 20818419
DOI: 10.1038/onc.2010.382

Genes

MET

Provenance

PubMed metadata and Literature Corpus relationships. Corpus snapshot updated 7 Sept 2026. Manifest publication-graph-cohort-2026-09-07.1.

Source receipt: pubmed, retrieved 7 Sept 2026.

Related research

Semantic proximity does not establish scientific evidence.

Research trail→

Click a neighbor to travelStep 1 · 12 closest

PRIMA-1(MET)/APR-246 targets mutant forms of p53 family members p63 and p73.PMID 20818419Read ↗

Antitumor Effects of PRIMA-1 and PRIMA-1Met (APR246) in Hematological Malignancies: Still a Mutant P53-Dependent Affair?Semantic proximity Read ↗

PRIMA-1 and PRIMA-1Met (APR-246): From Mutant/Wild Type p53 Reactivation to Unexpected Mechanisms Underlying Their Potent Anti-Tumor Effect in Combinatorial TherapiesSemantic proximity Read ↗

p53 reactivating small molecule PRIMA‑1MET/APR‑246 regulates genomic instability in MDA‑MB‑231 cells.Semantic proximity Read ↗

Restoring p53-dependent tumor suppression.Semantic proximity Read ↗

Mutant p53 reactivation by PRIMA-1MET induces multiple signaling pathways converging on apoptosis.Semantic proximity Read ↗

PRIMA-1 reactivates mutant p53 by covalent binding to the core domain.Semantic proximity Read ↗

APR-246/PRIMA-1(MET) rescues epidermal differentiation in skin keratinocytes derived from EEC syndrome patients with p63 mutations.Semantic proximity Read ↗

Restoration of the tumor suppressor function to mutant p53 by a low-molecular-weight compound.Semantic proximity Read ↗

PRIMA-1met (APR-246) inhibits growth of colorectal cancer cells with different p53 status through distinct mechanismsSemantic proximity Read ↗

P63 in health and cancerSemantic proximity Read ↗

p63 and p73: Roles in Development and Tumor FormationSemantic proximity Read ↗

Variability in functional p53 reactivation by PRIMA-1(Met)/APR-246 in Ewing sarcoma.Semantic proximity Read ↗

⌁Select a neighboring publication to make it the new centre.