Associated Papers
Targeting the p53 cancer mutants Y220C, Y220N, and Y220S with the small-molecule stabilizer rezatapopt.
Mavridi D et al.
Cell Death & Disease, 2026
TP53 mutation heterogeneity reveals distinct prognoses in mantle cell lymphoma.
Liu S et al.
Annals of Hematology, 2026
Neoantigenic properties of TP53 variants influence cancer risk in individuals with Li-Fraumeni syndrome.
Montellier E et al.
Ebiomedicine, 2026
Mechanistic Insights into the Allosteric Regulation of P53 Y220C by Small-Molecule Stabilizers.
Wen Y et al.
Journal of Chemical Information and Modeling, 2025
Discovery of novel covalent stabilizers for p53 Y220C using structure-based drug discovery methods.
Wen Y et al.
Molecular Diversity, 2025
Cellular activity upregulation of the thermolabile p53 cancer mutant Y220C by small molecule indazole derivatives.
Khadiullina R et al.
Cell Death Discovery, 2025
A quantitative, Bayesian-informed approach to gene-specific variant classification: Updated Expert Panel recommendations improve classification of TP53 germline variants for Li-Fraumeni syndrome.
Fortuno C et al.
Genome Medicine, 2025
Restoration of the Tumor Suppressor Function of Y220C-Mutant p53 by Rezatapopt, a Small-Molecule Reactivator.
Puzio-Kuter AM et al.
Cancer Discovery, 2025
In Silico Screening, Molecular Dynamics Simulation and Binding Free Energy Identify Single-Point Mutations That Destabilize p53 and Reduce Binding to DNA.
Islam SM et al.
Proteins, 2025
Discovery of Rezatapopt (PC14586), a First-in-Class, Small-Molecule Reactivator of p53 Y220C Mutant in Development.
Vu BT et al.
Acs Medicinal Chemistry Letters, 2025
Deep CRISPR mutagenesis characterizes the functional diversity of TP53 mutations.
Funk JS et al.
Nature Genetics, 2025
SNAr Reactive Pyrazine Derivatives as p53-Y220C Cleft Binders with Diverse Binding Modes.
Klett T et al.
Drug Design, Development and Therapy, 2025
Clustering of TP53 variants into functional classes correlates with cancer risk and identifies different phenotypes of Li-Fraumeni syndrome.
Montellier E et al.
Iscience, 2024
Interaction of p53 with the Δ133p53α and Δ160p53α isoforms regulates p53 conformation and transcriptional activity.
Tomas F et al.
Cell Death & Disease, 2024
Comprehensive classification of TP53 somatic missense variants based on their impact on p53 structural stability.
Tam B et al.
Briefings in Bioinformatics, 2024
Structural basis of p53 inactivation by cavity-creating cancer mutations and its implications for the development of mutant p53 reactivators.
Balourdas DI et al.
Cell Death & Disease, 2024
Biomolecular Condensation of the Human Papillomavirus E2 Master Regulator with p53: Implications in Viral Replication.
Borkosky SS et al.
Journal of Molecular Biology, 2023
Multifunctional metallochaperone modifications for targeting subsite cavities in mutant p53-Y220C.
Miller JJ et al.
Journal of Inorganic Biochemistry, 2023
Different impacts of TP53 mutations on cell cycle-related gene expression among cancer types.
Sasaki K et al.
Scientific Reports, 2023
OPUS-Mut: Studying the Effect of Protein Mutation through Side-Chain Modeling.
Xu G et al.
Journal of Chemical Theory and Computation, 2023
Targeting p53 pathways: mechanisms, structures, and advances in therapy.
Wang H et al.
Signal Transduction and Targeted Therapy, 2023
A Comprehensive Analysis of Cutaneous Melanoma Patients in Greece Based on Multi-Omic Data.
Kontogianni G et al.
Cancers, 2023
A Small Molecule Reacts with the p53 Somatic Mutant Y220C to Rescue Wild-type Thermal Stability.
Guiley KZ et al.
Cancer Discovery, 2023
Water Leakage Pathway Leads to Internal Hydration of the p53 Core Domain.
Lima IDM et al.
Biochemistry, 2023
AI-powered discovery of a novel p53-Y220C reactivator.
Zhou S et al.
Frontiers in Oncology, 2023
Mapping Interactions of the Intrinsically Disordered C-Terminal Regions of Tetrameric p53 by Segmental Isotope Labeling and NMR.
Krois AS et al.
Biochemistry, 2022
Evolutionary history of the p53 family DNA-binding domain: insights from an Alvinella pompejana homolog.
Zhang Q et al.
Cell Death & Disease, 2022
Analysis and Interpretation of the Impact of Missense Variants in Cancer.
Petrosino M et al.
International Journal of Molecular Sciences, 2021
Phosphorylation Control of p53 DNA-Binding Cooperativity Balances Tumorigenesis and Aging.
Timofeev O et al.
Cancer Research, 2020
Tumorigenic p53 mutants undergo common structural disruptions including conversion to α-sheet structure.
Bromley D et al.
Protein Science : a Publication of the Protein Society, 2020
Targeting Cavity-Creating p53 Cancer Mutations with Small-Molecule Stabilizers: the Y220X Paradigm.
Bauer MR et al.
Acs Chemical Biology, 2020
Bifunctional ligand design for modulating mutant p53 aggregation in cancer.
Miller JJ et al.
Chemical Science, 2019
Structural insights into the critical DNA damage sensors DNA-PKcs, ATM and ATR.
Baretic D et al.
Progress in Biophysics and Molecular Biology, 2019
A structure-guided molecular chaperone approach for restoring the transcriptional activity of the p53 cancer mutant Y220C.
Bauer MR et al.
Future Medicinal Chemistry, 2019
From uncertainty to pathogenicity: clinical and functional interrogation of a rare TP53 in-frame deletion.
Quinn EA et al.
Cold Spring Harbor Molecular Case Studies, 2019
Virtual screening of p53 mutants reveals Y220S as an additional rescue drug target for PhiKan083 with higher binding characteristics.
Raghavan V et al.
Computational Biology and Chemistry, 2019
Finding driver mutations in cancer: Elucidating the role of background mutational processes.
Brown AL et al.
Plos Computational Biology, 2019
Modulation of interaction of mutant TP53 and wild type BRCA1 by alkaloids: a computational approach towards targeting protein-protein interaction as a futuristic therapeutic intervention strategy for breast cancer impediment.
Tiwari S et al.
Journal of Biomolecular Structure & Dynamics, 2018
Effects of Y361-auto-phosphorylation on structural plasticity of the HIPK2 kinase domain.
Scaglione A et al.
Protein Science : a Publication of the Protein Society, 2018