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The Quest for Novel Cancer Biomarkers and Drug Targets in the Alternative Splicing Landscape: Highlights of Analytical Sciences in Switzerland
No full textVisible Light Induced One-pot Synthesis of Spirocyclopropyl Oxindoles from Isatin Derivatives and Glycine Ester Hydrochloride
Full text linkAn integrated one pot protocol for the in situ generation of hazardous alkyl diazoacetates (from glycine ester hydrochloride) and their subsequent reaction with 3-alkenyl oxoindoles (generated via the in situ Wittig reaction from isatin derivatives) to afford diastereomeric mixtures of spirocyclopropyl oxoindoles in toluene at room temperature is presented. Spirocyclopropyl oxoindoles are interesting building blocks prevalent in many active pharmaceutical ingredients and in natural products. This protocol is devoid of any metal catalysts or bases
‘Chemie für dich und mich’ – A Hands-on Science Resource for Primary Schools
No full textChemistry without formulas or reaction equations, but with full relevance to a 12-year-old’s everyday life. This is “Chemie für dich und mich”: a learning resource for primary schools, combining a hands-on kit with a training course for teachers
Beyond the Canonical 20: Peptide Discovery with Non-Canonical Amino Acids
Full text linkAmino acids are central to biology as signaling molecules and as the building blocks of peptides and proteins, which represent an expanding class of drugs with vast therapeutic potential. The precise modulation of individual residues in therapeutic peptides and proteins is crucial to enhance their pharmacological properties. Expanding beyond the twenty proteinogenic amino acids to include non-canonical amino acids (ncAAs) offers powerful strategies to optimize the stability, selectivity, and potency of peptides. Including ncAAs in the early discovery phase can significantly accelerate lead development and clinical translation. This review examines how diverse platforms integrate ncAAs in early discovery and compares the capabilities and limitations of these discovery technologies. Finally, key challenges are outlined that must be addressed to drive future innovations and explore new therapeutic avenues. Together, these approaches mark a shift towards peptide drug discovery where non-canonical chemistry is not an exception but a necessity
Guided by Enzymes: Targeted Photodynamic Therapy as a Strategy for Precision Medicine
Full text linkPhotodynamic therapy (PDT) is a clinically proven, non-invasive cancer treatment that enables precise spatial and temporal control of cytotoxicity. Yet, many current photosensitisers (PSs) suffer from poor tumour specificity, limiting their effectiveness. Targeted photodynamic therapy (tPDT) addresses this by directing PSs to selectively accumulate in tumour tissue. Among the emerging strategies, enzyme targeting stands out as a powerful approach. This review explores enzyme-targeted PDT using metal-based PSs conjugated to small-molecule enzyme inhibitors — a dual-action design that enables tumour destruction while blocking key pro-tumour signalling pathways. Five distinct proteins with enzymatic activity such as carbonic anhydrase (CA), cathepsin B, cyclooxygenase (COX), epidermal growth factor receptor (EGFR), and heat shock protein 90 (Hsp90) are presented through selected conjugates. These cases underscore the versatility of tPDT in achieving precise tumour targeting. By enhancing therapeutic efficacy, minimising off-target toxicity and collateral damage, and ultimately improving patient safety, enzyme-directed tPDT bridges targeted therapy, photomedicine, and precision oncology — setting the stage for next-generation cancer treatments
New Ligands Beyond N-Heterocyclic Carbenes for Application in Homogeneous Catalysis
Full text linkBuilding on the success of N-heterocyclic carbenes, extended versions comprised of an exocyclic metal bonding site have become increasingly popular. Pyridinium amidates (PYAs) belong to these ligand systems, as they contain a N-donor site that is formally stabilized by a pyridine-derived carbene. These PYAs are characterized by a unique donor flexibility, which imparts in some settings extraordinarily high catalytic activity, and in other settings remarkable stability of (catalytic) intermediates, which allows for deciphering mechanistic pathways
Unlocking the Potential of Flow Biocatalysis with Enzyme Immobilization
Full text linkFlow biocatalysis combines the superior selectivity and sustainability of enzymes with the flexibility, automation potential, and enhanced productivity of continuous manufacturing. However, to apply a biocatalytic step in flow, some intrinsic limitations of biocatalysts must be addressed, especially their stability and reusability. Thus, enzyme immobilization is a key enabling technology and remains a critical step and one of the main bottlenecks. Immobilizing enzymes on solid supports improves their stability, reusability, and compatibility with flow conditions, but it is limited by the trial-and-error approach at the development stages. In this short perspective, we discuss recent innovations in enzyme immobilization, including in silico design, the combination with 3D printing and high-throughput screening, and present selected examples of applications in flow of immobilized enzymes, with a particular focus on process flexibility and their combination into chemoenzymatic cascades