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

Restoration of the Tumor Suppressor Function of Y220C-Mutant p53 by Rezatapopt, a Small-Molecule Reactivator

13 Feb 2025

Abstract excerpt

Restoration of the tumor suppressor function of tumor-associated p53 mutants, including the Y220C substitution, has posed a significant challenge for therapeutic discovery. In this study, we describe rezatapopt (PC14586), part of a series of compounds designed to reactivate the p53 Y220C mutant. These compounds restore p53 tumor suppressor function by correcting its conformation and enabling it to bind DNA and...

Read the complete abstract on PubMed

Topics

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

Share to Cancer-related Molecular Pathways
Share to Microtubule and mitosis dynamics
Share to PI3K/AKT/mTOR signaling in cancer

Methodology Data sources Editorial policy Privacy About Contact Helena Bioinformatics

Source

Identifiers

PMID: 39945593
DOI: 10.1158/2159-8290.cd-24-1421

Provenance

PubMed metadata and Literature Corpus relationships. Corpus snapshot updated 2 Sept 2026.

Related research

Semantic proximity does not establish scientific evidence.

Research trail→

Click a neighbor to travelStep 1 · 12 closest

Restoration of the Tumor Suppressor Function of Y220C-Mutant p53 by Rezatapopt, a Small-Molecule ReactivatorPMID 39945593Read ↗

Discovery of Rezatapopt (PC14586), a First-in-Class, Small-Molecule Reactivator of p53 Y220C Mutant in DevelopmentSemantic proximity Read ↗

Targeting the p53 cancer mutants Y220C, Y220N, and Y220S with the small-molecule stabilizer rezatapopt.Semantic proximity Read ↗

Acquired On-Target Alterations Drive Clinical Resistance to p53-Y220C Reactivators.Semantic proximity Read ↗

Phase 1 Study of Rezatapopt, a p53 Reactivator, in TP53 Y220C-Mutated Tumors.Semantic proximity Read ↗

Discovery of Nanomolar-Affinity Pharmacological Chaperones Stabilizing the Oncogenic p53 Mutant Y220CSemantic proximity Read ↗

Restoring p53 wild-type conformation in TP53 -Y220C–mutant acute myeloid leukemiaSemantic proximity Read ↗

Pharmacological reactivation of mutant p53: from protein structure to the cancer patient.Semantic proximity Read ↗

A Small Molecule Reacts with the p53 Somatic Mutant Y220C to Rescue Wild-type Thermal Stability.Semantic proximity Read ↗

Discovery of compounds that reactivate p53 mutants in vitro and in vivo.Semantic proximity Read ↗

Anticancer therapeutic strategies for targeting mutant p53-Y220CSemantic proximity Read ↗

Targeting Oncogenic Mutant p53 for Cancer TherapySemantic proximity Read ↗

Activating p53Y220C with a mutant-specific small molecule.Semantic proximity Read ↗

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