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Click Chemistry Methodology: The Novel Paintbrush of Drug Design.
ACS Chem Biol
December 2024
Biomedical Science Research Complex, Schools of Biology and Chemistry, University of Saint Andrews, North Haugh, St Andrews KY16 9ST, United Kingdom of Great Britain and Northern Ireland.
Click chemistry is an immensely powerful technique for the synthesis of reliable and efficient covalent linkages. When undertaken in living cells, the concept is thereby coined bioorthogonal chemistry. Used in conjunction with the photo-cross-linking methodology, it serves as a sound strategy in the exploration of biological processes and beyond.
View Article and Find Full Text PDFGuanidinium-Stapled Helical Peptides for Targeting Protein-Protein Interactions.
Angew Chem Int Ed Engl
December 2024
Université de Bordeaux, CBMN UMR5248, IECB, 2, rue Robert Escarpit, 33607, PESSAC, FRANCE.
Peptide stapling has emerged as a versatile approach in drug discovery to reinforce secondary structure elements especially α-helices and improve properties of linear bioactive peptides. Inspired by the prevalence of arginine in protein-protein and protein-DNA interfaces, we investigated guanidinium-stapling as a means to constrain helical peptides. Guanidinium stapling was readily achieved on solid support, utilizing two orthogonally protected lysine or unatural α-amino acid residues with an amino function.
View Article and Find Full Text PDFTumour purity assessment with deep learning in colorectal cancer and impact on molecular analysis.
J Pathol
December 2024
Department of Pathology and Molecular Pathology, University Hospital and University of Zurich, Zurich, Switzerland.
Tumour content plays a pivotal role in directing the bioinformatic analysis of molecular profiles such as copy number variation (CNV). In clinical application, tumour purity estimation (TPE) is achieved either through visual pathological review [conventional pathology (CP)] or the deconvolution of molecular data. While CP provides a direct measurement, it demonstrates modest reproducibility and lacks standardisation.
View Article and Find Full Text PDFDraft genomes of two contemporary strains of .
Microbiol Resour Announc
December 2024
Vector Borne Diseases, Virology Department, Animal Plant and Health Agency, Addlestone, Surrey, United Kingdom.
, major cause of bovine babesiosis with zoonotic potential, was analyzed through genomes Bdiv23B and Bdiv24B following Illumina sequencing of DNA extracted from PCR-positive cattle blood. The genomes comprised 3888 and 4032 predicted coding sequences, respectively, comparable to the reference genome, Rouen 1987, highlighting genomic consistency across isolates.
View Article and Find Full Text PDFLINE-1 hypomethylation characterizes the inflammatory response in coeliac disease associated-intestinal mucosa and small bowel adenocarcinomas.
J Pathol
January 2025
Unit of Pathology, Department of Medicine and Technological Innovation, University of Insubria, Varese, Italy.
Long interspersed nuclear elements 1 (LINE-1) are the most abundant and the only autonomous mobile elements in the human genome. When their epigenetic repression is removed, it can lead to disease, such as autoimmune diseases and cancer. Coeliac disease (CeD) is an immune-mediated disease triggered by an abnormal T-cell response to dietary gluten and a predisposing condition of small bowel adenocarcinoma (SBA), frequently characterized by epigenetic alterations.
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