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The anti-angiogenic agent fumagillin covalently binds and inhibits the methionine aminopeptidase, MetAP-2

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Discovery of PF-04457845: A Highly Potent, Orally Bioavailable, and Selective Urea FAAH Inhibitor

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Rational Targeting of Active-Site Tyrosine Residues Using Sulfonyl Fluoride Probes

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Expanding the Armory: Predicting and Tuning Covalent Warhead Reactivity

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Aromatic Sulfonyl Fluorides Covalently Kinetically Stabilize Transthyretin to Prevent Amyloidogenesis while Affording a Fluorescent Conjugate

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Covalent Enzyme Inhibition through Fluorosulfate Modification of a Noncatalytic Serine Residue

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Selectively Targeting the Kinome-Conserved Lysine of PI3Kδ as a General Approach to Covalent Kinase Inhibition

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β-Lactams as Selective Chemical Probes for the in Vivo Labeling of Bacterial Enzymes Involved in Cell Wall Biosynthesis, Antibiotic Resistance, and Virulence

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Tetrazole‐Based Probes for Integrated Phenotypic Screening, Affinity‐Based Proteome Profiling, and Sensitive Detection of a Cancer Biomarker

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Molecular Mechanism of Avibactam-Mediated β-Lactamase Inhibition

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A Fluorogenic Aryl Fluorosulfate for Intraorganellar Transthyretin Imaging in Living Cells and in Caenorhabditis elegans

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Covalent Protein Labeling at Glutamic Acids

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Diazo compounds for the bioreversible esterification of proteins

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Expanding the scope of electrophiles capable of targeting K-Ras oncogenes

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Optimized Diazo Scaffold for Protein Esterification

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Chemoselective small molecules that covalently modify one lysine in a non-enzyme protein in plasma

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An Irreversible Inhibitor of HSP72 that Unexpectedly Targets Lysine‐56

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Novel inhibitors targeted to methionine aminopeptidase 2 (MetAP2) strongly inhibit the growth of cancers in xenografted nude model

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Recent Advances in Selective and Irreversible Covalent Ligand Development and Validation

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Fragment-based covalent ligand discovery

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New Electrophiles and Strategies for Mechanism-Based and Targeted Covalent Inhibitor Design

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