Phenotype-first covalent fragment screening identifies a synthetic lethal TYMS inhibitor in ATRX-deficient cells

Abstract excerpt

Chemoproteomic mapping of covalent fragment libraries is expanding the ligandable human proteome with direct evidence of cellular target engagement. However, understanding the functional consequences of specific covalent modifications typically requires extensive downstream biological characterisation. Here we present a ‘phenotype-first’ approach that integrates covalent fragment screening with chemoproteomics and...

Topics

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• Biosensing Techniques
• Chemical Synthesis and Analysis
• Click Chemistry and Applications
• DNA Repair Enzymes
• HEK293 Cells
• High-Throughput Screening Assays
• Peptidase Inhibition and Analysis
• Poly (ADP-Ribose) Polymerase-1

Identifiers and source

Literature Corpus work

21b99a2e-3df9-5bee-8a1f-a0e845010463

DOI

10.64898/2026.06.10.731339