Covalent Modifiers

A feed for the blog Discusses the covalent modification of proteins. Available on bsky and mass std don

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[Covalent Modifiers @CovalentMod]

Zongertinib (BI 1810631), an Irreversible HER2 TKI, Spares EGFR Signaling and Improves Therapeutic Response in Preclinical Models and Patients with HER2-Driven Cancers https://t.co/KsiyO1Izh9

[Covalent Modifiers @CovalentMod]

Design, synthesis and biological evaluation of the activity-based probes for FGFR covalent inhibitor https://t.co/1Wdyhn0JXZ

[Covalent Modifiers @CovalentMod]

Discovery of a Novel Serine-Targeting Covalent Inhibitor against HCES2A for Treating Drug-induced Diarrhea and Ulcerative Colitis https://t.co/kp6NBEqeOQ

[Covalent Modifiers @CovalentMod]

Chimeric deubiquitinase engineering reveals structural basis for specific inhibition of the mitophagy regulator USP30 https://t.co/xrGdcfSQaC

[Covalent Modifiers @CovalentMod]

Blocking C-terminal processing of KRAS4b via a direct covalent attack on the CaaX-box cysteine https://t.co/tNkPKIQ8Ud

[Covalent Modifiers @CovalentMod]

Discovery of Carbodiimide Warheads to Selectively and Covalently Target Aspartic Acid in KRASG12D https://t.co/8srUH6ulYB

[Covalent Modifiers @CovalentMod]

Residue-Selective Inhibitors Discovery via Covalent DNA-Encoded Chemical Libraries with Diverse Warheads https://t.co/ax0TWqn483

[Covalent Modifiers @CovalentMod]

Glecirasib, a potent and selective covalent KRAS G12C inhibitor exhibiting synergism 2 with cetuximab or SHP2 inhibitor JAB-3312 https://t.co/h99wbdjfvN

[Ingo Hartung @HartungIngo]

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

[Covalent Modifiers @CovalentMod]

Discovery and Optimization of a Covalent AKR1C3 Inhibitor https://t.co/OxuSYNIUFb

[Covalent Modifiers @CovalentMod]

DCAF16-Based Covalent Degradative Handles for the Modular Design of Degraders https://t.co/4Ec2z4HFHB

[Covalent Modifiers @CovalentMod]

Proteomic Ligandability Maps of Phosphorus(V) Stereoprobes Identify Covalent TLCD1 Inhibitors https://t.co/ZIvn851XLY

[Covalent Modifiers @CovalentMod]

Discovery and Optimization of a Covalent AKR1C3 Inhibitor https://t.co/nw9O02hiR3

[Covalent Modifiers @CovalentMod]

Discovery of RNA-Reactive Small Molecules Guides Design of Electrophilic Modules for RNA-Specific Covalent Binders https://t.co/0bCRYsn9HO

[Covalent Modifiers @CovalentMod]

Identification of a phenyl ester covalent inhibitor of caseinolytic protease and analysis of the ClpP1P2 inhibition in mycobacteria https://t.co/GkN8BRZQsg

[Covalent Modifiers @CovalentMod]

Substrate Trapping in Polyketide Synthase Thioesterase Domains: Structural Basis for Macrolactone Formation https://t.co/Ctm5gVuAUh

[Covalent Modifiers @CovalentMod]

Covalent Modification of Glutamic Acid Inspired by HaloTag Technology https://t.co/z99ls2AtZB

[Covalent Modifiers @CovalentMod]

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A predictive model for thiol reactivity of N-heteroaryl α-methylene–γ-lactams—a medicinally relevant covalent reactive group https://t.co/8U7S1QqXBf