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
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
Dominant-Negative Effects of p53 R337 Variants in Li-Fraumeni Syndrome: Impact on Tetramer Formation and Transcriptional Activity.
Kamada R et al.
Chembiochem : a European Journal of Chemical Biology, 2025
Cellular activity upregulation of the thermolabile p53 cancer mutant Y220C by small molecule indazole derivatives.
Khadiullina R et al.
Cell Death Discovery, 2025
p53 isoforms have a high aggregation propensity, interact with chaperones and lack binding to p53 interaction partners.
Brdar A et al.
Elife, 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
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
Molecular Divergence upon EGFR-TKI Resistance Could Be Dependent on the Exon Location of the Original EGFR-Sensitizing Mutation.
Serna-Blasco R et al.
Cancers, 2022
TP53_PROF: a machine learning model to predict impact of missense mutations in TP53.
Ben-Cohen G et al.
Briefings in Bioinformatics, 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
The disordered DNA-binding domain of p53 is indispensable for forming an encounter complex to and jumping along DNA.
Graha Subekti DR et al.
Biochemical and Biophysical Research Communications, 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
Thermodynamic and Evolutionary Coupling between the Native and Amyloid State of Globular Proteins.
Langenberg T et al.
Cell Reports, 2020
Targeting Cavity-Creating p53 Cancer Mutations with Small-Molecule Stabilizers: the Y220X Paradigm.
Bauer MR et al.
Acs Chemical Biology, 2020
Liquid-like droplet formation by tumor suppressor p53 induced by multivalent electrostatic interactions between two disordered domains.
Kamagata K et al.
Scientific Reports, 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
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
The Disordered Linker in p53 Participates in Nonspecific Binding to and One-Dimensional Sliding along DNA Revealed by Single-Molecule Fluorescence Measurements.
Subekti DRG et al.
Biochemistry, 2017