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Covalent Modifiers

@covalentmod.bsky.social
890 followers 64 following 551 posts

A BlueSky feed for the blog covalentmodifiers.blogspot.com. Discusses the covalent modification of proteins, particularly with regards to inhibitors.

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Covalent Modifiers @covalentmod.bsky.social · 04/10/2026
β-d-Arabinofuranose-configured Cyclitol Aziridines as Selective, Brain-penetrant Covalent GBA2 Inhibitors covalentmodifiers.blogspot.com/2026…
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Covalent Modifiers @covalentmod.bsky.social · 02/10/2026
Structure-Guided Design of a Brain-Penetrant Covalent Inhibitor of Human Butyrylcholinesterase with In Vivo Procognitive Efficacy covalentmodifiers.blogspot.com/2026…
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Covalent Modifiers @covalentmod.bsky.social · 22/09/2026
Fragment-Based Covalent Targeting of Lysines at the Allosteric Latch Site of SHP2. covalentmodifiers.blogspot.com/2026…
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Covalent Modifiers @covalentmod.bsky.social · 14/09/2026
Dual-Site Covalent Targeting Enables BD2-Selective BET Inhibition With Potent Antitumor Activity in Mice covalentmodifiers.blogspot.com/2026…
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Covalent Modifiers @covalentmod.bsky.social · 14/09/2026
Isoform-Selective Targeting of Akt Through Covalent Allosteric Inhibition covalentmodifiers.blogspot.com/2026…
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Covalent Modifiers @covalentmod.bsky.social · 31/08/2026
An enantioselective covalent inhibitor of BAX confers cytoprotection in vivo covalentmodifiers.blogspot.com/2026…
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Covalent Modifiers @covalentmod.bsky.social · 31/08/2026
Enhancing De Novo Designed Peptides and Proteins via Irreversible Covalent Isoquinolinium Capture covalentmodifiers.blogspot.com/2026…
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Covalent Modifiers @covalentmod.bsky.social · 30/08/2026
Sulfonyl-Imidazopyridines Decouple Reactivity from Stability for Ligandability Mapping and Covalent Inhibitor Discovery covalentmodifiers.blogspot.com/2026…
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Covalent Modifiers @covalentmod.bsky.social · 26/08/2026
Development of Covalent Inhibitors of Chikungunya Virus nsP2 Cysteine Protease Enabled by Direct-to-Biology Synthesis and Screening D covalentmodifiers.blogspot.com/2026…
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Covalent Modifiers @covalentmod.bsky.social · 24/08/2026
Covalent allosteric inhibition of AARS1 lactyltransferase covalentmodifiers.blogspot.com/2026…
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Covalent Modifiers @covalentmod.bsky.social · 22/08/2026
Sulfonyl-Imidazopyridines Decouple Reactivity from Stability for Ligandability Mapping and Covalent Inhibitor Discovery covalentmodifiers.blogspot.com/2026…
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Covalent Modifiers @covalentmod.bsky.social · 16/08/2026
Late-stage functionalization with strain-release warheads enables tunable covalent inhibition. covalentmodifiers.blogspot.com/2026…
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Covalent Modifiers @covalentmod.bsky.social · 13/08/2026
Discovery and Optimization of a WRN Helicase Inhibitor Series through Structure-Guided Drug Design from a Covalent Fragment Binding Insight covalentmodifiers.blogspot.com/2026…
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Covalent Modifiers @covalentmod.bsky.social · 10/08/2026
Discovery of a covalent FGFR2-selective inhibitor overcoming clinically-acquired resistance mutations covalentmodifiers.blogspot.com/2026…
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Covalent Modifiers @covalentmod.bsky.social · 06/08/2026
A covalent PFKL activator suppresses tumor growth covalentmodifiers.blogspot.com/2026…
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Covalent Modifiers @covalentmod.bsky.social · 28/07/2026
Late-stage functionalization with strain-release warheads enables tunable covalent inhibition covalentmodifiers.blogspot.com/2026…
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Covalent Modifiers @covalentmod.bsky.social · 24/07/2026
Peptidic Phosphonates as Irreversible Covalent Inhibitors of Plasmodium falciparum Serine Protease PfSUB1. covalentmodifiers.blogspot.com/2026…
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Covalent Modifiers @covalentmod.bsky.social · 23/07/2026
CHARMM-GUI Covalent Ligand Docker as a Web-based Molecular Docking Platform for Covalent Ligands covalentmodifiers.blogspot.com/2026…
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Covalent Modifiers @covalentmod.bsky.social · 22/07/2026
Covalent remodeling of CRBN creates a non-canonical neosubstrate interface with NTAQ1 covalentmodifiers.blogspot.com/2026…
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Covalent Modifiers @covalentmod.bsky.social · 20/07/2026
A covalent irreversible inhibitor binds in two mutually exclusive conformations to the active-site cysteine residue of human aldehyde dehydrogenase 1A3 covalentmodifiers.blogspot.com/2026…
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Covalent Modifiers @covalentmod.bsky.social · 17/07/2026
A covalent inhibitor targeting Cys-349 of LIMK1 confers selectivity over LIMK2 covalentmodifiers.blogspot.com/2026…
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Covalent Modifiers @covalentmod.bsky.social · 15/07/2026
Machine learning-guided discovery of covalent sortase A inhibitors targeting MRSA virulence covalentmodifiers.blogspot.com/2026…
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Covalent Modifiers @covalentmod.bsky.social · 08/06/2026
A chemoproteomic atlas of the human purine interactome for regioselective ligand discovery covalentmodifiers.blogspot.com/2026…
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Covalent Modifiers @covalentmod.bsky.social · 24/05/2026
Characterization of the Second-Generation Covalent Fragment Library (CovLib Gen2): Thiol Reactivity Profiling and p53-Y220C Rescue covalentmodifiers.blogspot.com/2026…
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Covalent Modifiers @covalentmod.bsky.social · 21/05/2026
Accelerating SuFEx Reactions via Aryl Fluorosulfate Structural Engineering for Enhanced Covalent Targeted Cancer Therapy covalentmodifiers.blogspot.com/2026…
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Covalent Modifiers @covalentmod.bsky.social · 10/05/2026
Covalent Inhibitors of Monoacylglycerol Lipase Induce Conformational Changes and Proteasomal Degradation covalentmodifiers.blogspot.com/2026…
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Covalent Modifiers @covalentmod.bsky.social · 08/05/2026
Development and Structural Characterization of UTE-156, a Covalent Inhibitor of the VCP/p97 AAA+ ATPase covalentmodifiers.blogspot.com/2026…
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Covalent Modifiers @covalentmod.bsky.social · 08/05/2026
Nitro-Diphenyl Ethers as Emerging Cysteine-Targeting Covalent Warheads Enable Identification of Novel Target LDLRAP1 for Anticoronaviral Activity covalentmodifiers.blogspot.com/2026…
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Covalent Modifiers @covalentmod.bsky.social · 07/05/2026
Shifting the PPARγ conformational ensemble toward a transcriptionally repressive state improves covalent inhibitor efficacy covalentmodifiers.blogspot.com/2026…
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Covalent Modifiers @covalentmod.bsky.social · 06/05/2026
Don’t Lose Your (War)head: Structure–Activity Relationships of Covalent Warheads as Substrates for GST-Catalyzed Glutathione Conjugation covalentmodifiers.blogspot.com/2026…
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Covalent Modifiers @covalentmod.bsky.social · 06/05/2026
Deciphering covalent kinase inhibitor binding landscape through structural kinome profiling covalentmodifiers.blogspot.com/2026…
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Covalent Modifiers @covalentmod.bsky.social · 06/05/2026
Data-driven design of chiral covalent fragments using highthroughput chemoproteomics and machine learning covalentmodifiers.blogspot.com/2026…
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Covalent Modifiers @covalentmod.bsky.social · 06/05/2026
Electrophilic compound screening identifies GPX4-dependent ferroptosis as a senescence vulnerability covalentmodifiers.blogspot.com/2026…
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Covalent Modifiers @covalentmod.bsky.social · 06/05/2026
A Novel Covalent Inhibitor Fragment for the SARS-CoV-2 Main Protease Identified by Target-Specific Deep Learning covalentmodifiers.blogspot.com/2026…
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Covalent Modifiers @covalentmod.bsky.social · 06/05/2026
Efficacy and safety of branebrutinib (BMS-986195), an irreversible Bruton's tyrosine kinase inhibitor, for the treatment of rheumatoid arthritis: a phase 2a, randomised, double-blind, placebo-controlled study covalentmodifiers.blogspot.com/2026…
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Covalent Modifiers @covalentmod.bsky.social · 26/03/2026
A Fragment Screen Identifies Acrylamide Covalent Inhibitors of the TEAD•YAP Protein-Protein Interaction covalentmodifiers.blogspot.com/2026…
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Covalent Modifiers @covalentmod.bsky.social · 24/03/2026
Discovery of Covalent Ligands with AlphaFold3 covalentmodifiers.blogspot.com/2026…
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Covalent Modifiers @covalentmod.bsky.social · 23/03/2026
Acrylamide Bioisosterism: Alkenyl Aromatic Heterocycles as Reactivity-Tunable Warheads for Covalent BTK Inhibitors covalentmodifiers.blogspot.com/2026…
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Covalent Modifiers @covalentmod.bsky.social · 22/03/2026
Covalent JAK3 inhibitors based on 2-arylamino and 7H-pyrrolo[2,3-d]pyrimidine scaffold: design, synthesis, and biological evaluation for the potential treatment of Bortezomib-resistant multiple myeloma covalentmodifiers.blogspot.com/2026…
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Covalent Modifiers @covalentmod.bsky.social · 12/03/2026
A Global Ligandability Map of Tryptoline Butynamide Stereoprobes Identifies Covalent Inhibitors of the Actin Maturation Protease ACTMAP covalentmodifiers.blogspot.com/2026…
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Covalent Modifiers @covalentmod.bsky.social · 12/03/2026
Development and Structural Characterization of UTE-156, a Covalent Inhibitor of the VCP/p97 AAA+ ATPase covalentmodifiers.blogspot.com/2026…
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Covalent Modifiers @covalentmod.bsky.social · 04/03/2026
Discovery and Characterization of Divarasib (GDC-6036), a Potent Covalent Inhibitor of KRAS G12C covalentmodifiers.blogspot.com/2026…
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Covalent Modifiers @covalentmod.bsky.social · 20/02/2026
A Tandem Bioorthogonal Retro-Cope and Cope Elimination for the Activation of Covalent Inhibitors with an Acrylamide or Vinylsulfonamide Warhead in Live Cells covalentmodifiers.blogspot.com/2026…
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Covalent Modifiers @covalentmod.bsky.social · 19/02/2026
Discovery of a Potent, Selective, and In Vivo Efficacious Covalent Inhibitor for Lysine Methyltransferase SETD8 covalentmodifiers.blogspot.com/2026…
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Covalent Modifiers @covalentmod.bsky.social · 16/02/2026
Exploiting human fucosyltransferase 8 allostery with a covalent inhibitor for core fucosylation suppression covalentmodifiers.blogspot.com/2026…
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Covalent Modifiers @covalentmod.bsky.social · 06/02/2026
Covalent inhibitor design confers activity against both GDP- and GTP-bound forms of KRAS G12C covalentmodifiers.blogspot.com/2026…
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Covalent Modifiers @covalentmod.bsky.social · 05/02/2026
Development of a Lysine-Reactive Targeted Covalent Inhibitor (TCI) for the P300/CBP-Associated Factor (PCAF) Bromodomain Through Structure-Based Design covalentmodifiers.blogspot.com/2026…
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Covalent Modifiers @covalentmod.bsky.social · 03/02/2026
Covalent Protein Inhibitors via Tyrosine and Tryptophan Conjugation with Cyclic Imine Mannich Electrophiles covalentmodifiers.blogspot.com/2026…
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Covalent Modifiers @covalentmod.bsky.social · 02/02/2026
Chemoproteomics discovery of a CNS-penetrant covalent inhibitor of PIKfyve covalentmodifiers.blogspot.com/2026…
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Covalent Modifiers @covalentmod.bsky.social · 26/01/2026
Group Competition Strategy for Covalent Ligand Discovery covalentmodifiers.blogspot.com/2026…
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