The last few years has seen a revolution in combinatorial chemistry, an approach that has been developed for the synthesis of chemical libraries for application within the pharmaceutical industry. Many chemical methods have been investigated, which can be utilized in all manner of strategies for library synthesis, including reactions of diazocarbonyls. This review discusses the application of diazocarbonyl functionalized molecules for the preparation of chemical libraries.
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Sci Rep
December 2024
IFOM ETS, The AIRC Institute of Molecular Oncology, Milan, Italy.
Targeting nuclear mechanics is emerging as a promising therapeutic strategy for sensitizing cancer cells to immunotherapy. Inhibition of the mechano-sensory kinase ATR leads to mechanical vulnerability of cancer cells, causing nuclear envelope softness and collapse and activation of the cGAS-STING-mediated innate immune response. Finding novel compounds that interfere with the non-canonical role of ATR in controlling nuclear mechanics presents an intriguing therapeutic opportunity.
View Article and Find Full Text PDFNat Chem Biol
January 2025
Institute of Pharmaceutical Sciences, Department of Chemistry and Applied Biosciences, ETH Zurich, Zurich, Switzerland.
ACS Synth Biol
December 2024
Division of Chemistry and Chemical Engineering, California Institute of Technology, Pasadena, California91125, United States.
Sequence-function data provides valuable information about the protein functional landscape but is rarely obtained during directed evolution campaigns. Here, we present Long-read every variant Sequencing (LevSeq), a pipeline that combines a dual barcoding strategy with nanopore sequencing to rapidly generate sequence-function data for entire protein-coding genes. LevSeq integrates into existing protein engineering workflows and comes with open-source software for data analysis and visualization.
View Article and Find Full Text PDFOrg Lett
December 2024
Department of Chemistry, Emory University, 1515 Dickey Drive, Atlanta, Georgia 30322, United States.
The synthetic utility of tetrabenzyl pyrophosphate for achieving chemoselective phosphorylation of phenols, as well as primary, secondary, and tertiary alcohols, is reported here. Additionally, we introduce a rapid, mild, and chemoselective debenzylation procedure, enabling access to phosphates in the presence of redox sensitive groups. Finally, stoichiometrically controlled monodebenzylation provides a versatile platform for late-stage divergent synthesis of phosphodiester and phosphoramidate chemical libraries.
View Article and Find Full Text PDFBiomacromolecules
December 2024
Polymer Science Group, Department of Chemical Engineering, The University of Melbourne, Melbourne 3010, Australia.
Advancements in polymer chemistry have enabled the design of macromolecular structures with tailored properties for diverse applications. Reversible addition-fragmentation chain-transfer (RAFT) polymerization is a controlled technique for precise polymer design. Automation tools further enhance polymer synthesis by enabling the rapid, reproducible preparation of polymer libraries.
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