A5087574340- Click Chemistry and Applications
- Chemical Synthesis and Analysis
- Epigenetics and DNA Methylation
- Microbial Natural Products and Biosynthesis
- Supramolecular Chemistry and Complexes
- Cancer-related gene regulation
- Carbohydrate Chemistry and Synthesis
- Protein Degradation and Inhibitors
- Antimicrobial Peptides and Activities
- Molecular Sensors and Ion Detection
École Polytechnique Fédérale de Lausanne
2022-2024
HUN-REN Research Centre for Natural Sciences
2021
Abstract Macrocycles have excellent potential as therapeutics due to their ability bind challenging targets. However, generating macrocycles against new targets is hindered by a lack of large macrocycle libraries for high-throughput screening. To overcome this, we herein established combinatorial approach tethering myriad chemical fragments peripheral groups structurally diverse macrocyclic scaffolds in fashion, all at picomole scale nanoliter volumes using acoustic droplet ejection...
Macrocycles offer an attractive format for drug development due to their good binding properties and potential cross cell membranes. To efficiently identify macrocyclic ligands new targets, methods the synthesis screening of large combinatorial libraries small cyclic peptides were developed, many them using thiol groups efficient peptide macrocyclization. However, a weakness these is that invariant thiol-containing building blocks such as cysteine are used, resulting in region does not...
Synthesis of peptides on a disulfide linker resin and release by the volatile reducing agent 1,4-butanedithiol offer efficient access to thiol-functionalized needed for peptide labeling, immobilization cyclization.
Histone methyltransferases (HMTs) have attracted considerable attention as potential targets for pharmaceutical intervention in various malignant diseases. These enzymes are known introducing methyl marks at specific locations of histone proteins, creating a complex system that regulates epigenetic control gene expression and cell differentiation. Here, we describe the identification first-generation cell-permeable non-nucleoside type inhibitors SETD2, only mammalian HMT is able to...
Abstract Macrocycles offer an attractive format for drug development due to their good binding properties and potential cross cell membranes. To efficiently identify macrocyclic ligands new targets, methods the synthesis screening of large combinatorial libraries small cyclic peptides were developed, many them using thiol groups efficient peptide macrocyclization. However, a weakness these is that invariant thiol‐containing building blocks such as cysteine are used, resulting in region does...