Covalent Modifiers

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Zongertinib (BI 1810631), an Irreversible HER2 TKI, Spares EGFR Signaling and Improves Therapeutic Response in Preclinical Models and Patients with HER2-Driven Cancers covalentmodifiers.blogspot.com/2025/05/zonger…

Design, synthesis and biological evaluation of the activity-based probes for FGFR covalent inhibitor covalentmodifiers.blogspot.com/2025/05/design…

Discovery of a Novel Serine-Targeting Covalent Inhibitor against HCES2A for Treating Drug-induced Diarrhea and Ulcerative Colitis covalentmodifiers.blogspot.com/2025/05/discov…

Chimeric deubiquitinase engineering reveals structural basis for specific inhibition of the mitophagy regulator USP30 covalentmodifiers.blogspot.com/2025/05/chimer…

Blocking C-terminal processing of KRAS4b via a direct covalent attack on the CaaX-box cysteine covalentmodifiers.blogspot.com/2025/05/blocki…

Discovery of Carbodiimide Warheads to Selectively and Covalently Target Aspartic Acid in KRASG12D covalentmodifiers.blogspot.com/2025/05/discov…

Residue-Selective Inhibitors Discovery via Covalent DNA-Encoded Chemical Libraries with Diverse Warheads covalentmodifiers.blogspot.com/2025/05/residu…

Glecirasib, a potent and selective covalent KRAS G12C inhibitor exhibiting synergism 2 with cetuximab or SHP2 inhibitor JAB-3312 covalentmodifiers.blogspot.com/2025/05/glecir…

Clinical update for zoldonrasib - Ras(on)G12D selective covalent inhibitor - dosed at 1200 mg qd po (MTD previously not reached). Generally well tolerated, 89% disease control rate for NSCLC patients, two promising case studies shared, but still very early days. #AACR25 @AACR

Discovery and Optimization of a Covalent AKR1C3 Inhibitor covalentmodifiers.blogspot.com/2025/04/discov…

DCAF16-Based Covalent Degradative Handles for the Modular Design of Degraders covalentmodifiers.blogspot.com/2025/04/dcaf16…

Proteomic Ligandability Maps of Phosphorus(V) Stereoprobes Identify Covalent TLCD1 Inhibitors covalentmodifiers.blogspot.com/2025/04/proteo…

Discovery and Optimization of a Covalent AKR1C3 Inhibitor covalentmodifiers.blogspot.com/2025/04/discov…

Discovery of RNA-Reactive Small Molecules Guides Design of Electrophilic Modules for RNA-Specific Covalent Binders covalentmodifiers.blogspot.com/2025/04/discov…

Identification of a phenyl ester covalent inhibitor of caseinolytic protease and analysis of the ClpP1P2 inhibition in mycobacteria covalentmodifiers.blogspot.com/2025/04/identi…

Substrate Trapping in Polyketide Synthase Thioesterase Domains: Structural Basis for Macrolactone Formation covalentmodifiers.blogspot.com/2025/04/substr…

Covalent Modification of Glutamic Acid Inspired by HaloTag Technology covalentmodifiers.blogspot.com/2025/04/covale…

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A predictive model for thiol reactivity of N-heteroaryl α-methylene–γ-lactams—a medicinally relevant covalent reactive group covalentmodifiers.blogspot.com/2025/04/a-pred…