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
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
Discovery of Novel RASGRF2 Fusions as a Therapeutic Target in Lung Adenocarcinoma of Never or Light Smokers.
Terashima Y et al.
Cancer Science, 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
Mechanisms of p53 core tetramer stability mediated by multi-interface interactions: A molecular dynamics study.
Zhou H et al.
Archives of Biochemistry and Biophysics, 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
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
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 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
Sequence Properties of An Intramolecular Interaction That Inhibits p53 DNA Binding.
Gregory E et al.
Biomolecules, 2022
Insights into Allosteric Mechanisms of the Lung-Enriched p53 Mutants V157F and R158L.
Lei J et al.
International Journal of Molecular Sciences, 2022
Mechanistic insights into global suppressors of protein folding defects.
Chattopadhyay G et al.
Plos Genetics, 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
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
Simulations of mutant p53 DNA binding domains reveal a novel druggable pocket.
Pradhan MR et al.
Nucleic Acids Research, 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
Targeting mutant p53 for efficient cancer therapy.
Bykov VJN et al.
Nature Reviews. Cancer, 2018
Insights into the Effect of the G245S Single Point Mutation on the Structure of p53 and the Binding of the Protein to DNA.
Lepre MG et al.
Molecules (basel, Switzerland), 2017
Reactivation of mutant p53: Constraints on mechanism highlighted by principal component analysis of the DNA binding domain.
Ouaray Z et al.
Proteins, 2016
Aggregation tendencies in the p53 family are modulated by backbone hydrogen bonds.
Cino EA et al.
Scientific Reports, 2016
An in silico algorithm for identifying stabilizing pockets in proteins: test case, the Y220C mutant of the p53 tumor suppressor protein.
Bromley D et al.
Protein Engineering, Design & Selection : Peds, 2016
Structural and sequential context of p53: A review of experimental and theoretical evidence.
Saha T et al.
Progress in Biophysics and Molecular Biology, 2015
Oxidation of p53 through DNA charge transport involves a network of disulfides within the DNA-binding domain.
Schaefer KN et al.
Biochemistry, 2015