ChemMedChem, EarlyView.Two PROTAC‐based degraders targeting the cancer‐associated transcriptional co‐activators CBP/p300 weredeveloped. These degraders, combining the CBP/p300 inhibitor C646 with the CRBN ligand thalidomide, reduced CBP/p300 levels in lymphoma cells at low‐micromolar concentration.
Francesco Fiorentino +9 more
wiley +1 more source
Studies on the functional role of UFMylation in cells (Review). [PDF]
Mol Med RepQin R +7 more
europepmc +1 more source
Beyond Docking: A Multi‐Tier Computational Pipeline for USP7 Inhibitor Optimization
ChemMedChem, Accepted Article.Ubiquitin‐specific protease 7 (USP7) is a key deubiquitinating enzyme involved in tumor suppression, DNA repair, and epigenetic regulation. Given its critical role in cancer progression, USP7 has emerged as an attractive therapeutic target. In this study, we employed a multi‐tier computational approach, integrating ligand‐based virtual screening ...
Serdar Durdagi +3 more
wiley +1 more source
TRIM52 maintains cellular fitness and is under tight proteolytic control by multiple giant E3 ligases. [PDF]
Nat CommunShulkina A +10 more
europepmc +1 more source
Advances in Isotope Labeling for Solution Nucleic Acid Nuclear Magnetic Resonance Spectroscopy
ChemPlusChem, EarlyView.Recent advances in the field of nucleic acid nuclear magnetic resonance (NMR) are presented. Stable isotope labeling protocols and new approaches to segmentally label nucleic acid with NMR‐active residues are summarized. The novel methods will have a strong impact on the future of nucleic acid NMR and the characterization of structure and dynamics of ...
Stefan Hilber +3 more
wiley +1 more source
High-Throughput Discovery of Substrate Peptide Sequences for E3 Ubiquitin Ligases Using a cDNA Display Method. [PDF]
ChembiochemTamagawa K, Campbell RE, Terai T.
europepmc +1 more source
Developmental Dynamics, EarlyView.Abstract Background Mutations in cohesins cause cohesinopathies such as Cornelia de Lange Syndrome (CdLS) and Roberts Syndrome (RBS). Prior findings demonstrate that Esco2 (a cohesin activator) and Smc3 (a core cohesin subunit) regulate the CRL4 E3 ubiquitin ligase. SMC3 mutations, however, account for a small percentage of CdLS.
Annie C. Sanchez +4 more
wiley +1 more source
During recombinase-mediated homology recognition RecQ helicases inhibit formation of toxic long-lived D-loops that could promote genomic instability. [PDF]
Nucleic Acids ResDanilowicz C, Meron A, Prentiss M.
europepmc +1 more source
European Journal of Heart Failure, EarlyView.The analysis workflow, findings and potential clinical consequences of iron deficiency in heart failure (HF). From 881 patients with worsening HF, whole blood transcriptome was analysed using the Affymetrix Human Transcriptome Array (HTA) 2.0. Subjects were stratified according to their transferrin saturation (TSAT) levels as iron‐deficient (TSAT <20%)
Niels Grote Beverborg +17 more
wiley +1 more source
A Commentary on Mitochondrial Dysfunction and Compromised DNA Repair in Neurodegeneration: The Emerging Role of FUS in ALS. [PDF]
Neurosci InsightsKodavati M, Hegde ML.
europepmc +1 more source