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Small-molecule covalent bond formation at tyrosine creates a binding site and inhibits activation of Ral GTPases

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Pitfalls and Considerations in Determining the Potency and Mutant Selectivity of Covalent Epidermal Growth Factor Receptor Inhibitors

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Covalent Proteomimetic Inhibitor of the Bacterial FtsQB Divisome Complex

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Novel Electrophilic Warhead Targeting a Triple-Negative Breast Cancer Driver in Live Cells Revealed by “Inverse Drug Discovery”

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Racemases and epimerases operating through a 1,1-proton transfer mechanism: reactivity, mechanism and inhibition

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Never Gonna Give You Up – Current Developments in Covalent Protein Kinase Inhibitors

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Inverse Drug Discovery identifies weak electrophiles affording protein conjugates

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Systematic Exploration of Privileged Warheads for Covalent Kinase Drug Discovery

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A targeted covalent inhibitor of p97 with proteome-wide selectivity

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Reactive fragments targeting carboxylate residues employing direct to biology, high-throughput chemistry

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Unraveling the nexus: Genomic instability and metabolism in cancer

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Advances in UDP-N-Acetylglucosamine Enolpyruvyl Transferase (MurA) Covalent Inhibition

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Extended Applications of Small-Molecule Covalent Inhibitors toward Novel Therapeutic Targets

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Profiling and Optimizing Targeted Covalent Inhibitors through EGFR-Guided Studies

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New Cysteine Covalent Modification Strategies Enable Advancement of Proteome‐wide Selectivity of Kinase Modulators

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Global Mapping of Metalloproteomes

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Covalent fragment-based ligand screening approaches for identification of novel ubiquitin proteasome system modulators

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Discovery of a Tunable Heterocyclic Electrophile 4-Chloro-pyrazolopyridine That Defines a Unique Subset of Ligandable Cysteines

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Best Practices for Design and Characterization of Covalent Chemical Probes

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Furan warheads for covalent trapping of weak protein–protein interactions: cross-linking of thymosin β4 to actin

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On the Origin of the Different Reversible Characters of Salinosporamide A and Homosalinosporamide A in the Covalent Inhibition of the Human 20S Proteasome

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Size-Dependent Target Engagement of Covalent Probes

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Druggable Sterol Metabolizing Enzymes in Infectious Diseases: Cell Targets to Therapeutic Leads

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Theoretical Studies of the Acid–Base Equilibria in a Model Active Site of the Human 20S Proteasome

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Discovery and Characterization of a Cryptic Secondary Binding Site in the Molecular Chaperone HSP70

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High-throughput mechanistic screening of non-equilibrium inhibitors by a fully automated data analysis pipeline in early drug-discovery

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Synthesis and optimisation of P3 substituted vinyl sulfone-based inhibitors as anti-trypanosomal agents

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Electronic Structures and Reactivities of COVID-19 Drugs: A DFT Study

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Steady-state kinetic analysis of reversible enzyme inhibitors: A case study on calf intestine alkaline phosphatase

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Steroidal Antimetabolites Protect Mice against Trypanosoma brucei

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Covalent Inhibitors - An Overview of Design Process, Challenges and Future Directions

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Vanillin-grafted chitosan biopolymers via nucleophilic addition–elimination: A promising bioactive biopolymer for enhanced skin wound repair

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Detection of an enzyme isomechanism by means of the kinetics of covalent inhibition

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Recombinant protein production for structural and kinetic studies: A case study using M. tuberculosis α-methylacyl-CoA racemase (MCR)

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Rational Design of Stapled Covalent Peptide Modifiers of Oncoprotein E6 from Human Papillomavirus

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Targeting protein–protein interactions with reversible covalent modalities: Non‐cysteine chemistries

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Organoselenium with electrophilic center targeting PDGFB for selective osteosarcoma radiosensitization

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Trends in covalent drug discovery: a 2020–23 patent landscape analysis focused on select covalent reacting groups (CRGs) found in FDA-approved drugs

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Synthesis of the 4-aza cyclopentenone analogue of Δ12,14-15-deoxy-PGJ2 and S-cysteine adducts

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Programmable synthesis of alkaloidal frameworks integrating Michael acceptor generates covalent probes for targeting POLE3 in HBV replication

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Targeting Conformational Flexibility of a Reactive Intermediate to Enhance Selectivity of a GABA Aminotransferase Inactivator

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Reactivity and mechanism in chemical and synthetic biology

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Thiol modification and signaling by biological electrophiles

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Expanding the Chemistry of Acyl Diazo Electrophile as a Tunable Warhead for Covalent Targeting of KRAS (G12D) Mutant

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Inactivation of ornithine aminotransferase by (1R,4S)-4-Amino-3-(trifluoromethyl)cyclopent-2-ene-1-carboxylic acid via a stable quinonoid intermediate

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Reaction hijacking of enzymes to generate potent therapeutic modulators in situ

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Structural Principles of Covalent Flavin Modification in Oxidoreductases

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Identification of small covalent inhibitors targeting DsbA using virtual screening, covalent docking, and molecular dynamics simulations

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