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Covalent Modifiers @covalentmod.bsky.social · 3d

youtu.be/4dC23U9S2Vc?... @dannomura.bsky.social @drug-hunter.bsky.social

Reimagining Druggability using Chemoproteomic Platforms

YouTube video by Drug Hunter

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Covalent Modifiers @covalentmod.bsky.social · 17d

A multicenter, open-label, first-in-human study of TYRA-200 in advanced intrahepatic cholangiocarcinoma and other solid tumors with activating FGFR2 gene alterations (SURF201). https://covalentmodifiers.blogspot.com/2025/10/a-multicenter-open-label-first-in-human.html

Covalent Modifiers @covalentmod.bsky.social · 17d

Discovery of Fulzerasib (GFH925) for the Treatment of KRAS G12C-Mutated Solid Tumors https://covalentmodifiers.blogspot.com/2025/10/discovery-of-fulzerasib-gfh925-for.html

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Covalent Modifiers @covalentmod.bsky.social · 25d

Discovery of an Internal Alkyne Warhead Scaffold for Irreversible hTG2 Inhibition https://covalentmodifiers.blogspot.com/2025/10/discovery-of-internal-alkyne-warhead.html

Covalent Modifiers @covalentmod.bsky.social · 27d

Covalent Probes Reveal Small-Molecule Binding Pockets in Structured RNA and Enable Bioactive Compound Design https://covalentmodifiers.blogspot.com/2025/10/covalent-probes-reveal-small-molecule.html

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Covalent Modifiers @covalentmod.bsky.social · Oct 5

AI-assisted delivery of novel covalent WRN inhibitors from a non-covalent fragment screen https://covalentmodifiers.blogspot.com/2025/10/ai-assisted-delivery-of-novel-covalent.html

Covalent Modifiers @covalentmod.bsky.social · Sep 27

Sulfinyl Aziridines as Stereoselective Covalent Destabilizing Degraders of the Oncogenic Transcription Factor MYC https://covalentmodifiers.blogspot.com/2025/09/sulfinyl-aziridines-as-stereoselective.html

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Covalent Modifiers @covalentmod.bsky.social · Sep 13

Covalent Ligand Electrophiles Are Differentially Activated by Proximity Effects Which Govern Latent Protein Reactivit https://covalentmodifiers.blogspot.com/2025/09/covalent-ligand-electrophiles-are.html

Covalent Modifiers @covalentmod.bsky.social · Sep 9

A covalent inhibitor targeting Cys16 on RhoA in colorectal cancer https://covalentmodifiers.blogspot.com/2025/09/a-covalent-inhibitor-targeting-cys16-on.html

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Covalent Modifiers @covalentmod.bsky.social · Sep 4

Covalent Irreversible Inhibitors of Tetracycline Destructases https://covalentmodifiers.blogspot.com/2025/09/covalent-irreversible-inhibitors-of.html

Covalent Modifiers @covalentmod.bsky.social · Sep 2

Covalent chemical probes https://covalentmodifiers.blogspot.com/2025/09/covalent-chemical-probes.html

Covalent Modifiers @covalentmod.bsky.social · Sep 1

Cell-Active, Irreversible Covalent Inhibitors Targeting a Surface-Exposed Non-Catalytic Lysine on Aurora a Kinase by Using Squarate Chemistry https://covalentmodifiers.blogspot.com/2025/09/cell-active-irreversible-covalent.html

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Covalent Modifiers @covalentmod.bsky.social · Sep 1

Small-Molecule Covalent Stabilization and Inhibition of the TEAD·YAP1 Transcription Factor in Cancer Cells https://covalentmodifiers.blogspot.com/2025/08/small-molecule-covalent-stabilization.html

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Covalent Modifiers @covalentmod.bsky.social · Aug 30

Chemoselective Installation of Electrophilic Warheads onto C-Terminal Peptide Hydrazides for Covalent Protease Inhibitor Synthesis https://covalentmodifiers.blogspot.com/2025/08/chemoselective-installation-of.html

Covalent Modifiers @covalentmod.bsky.social · Aug 29

Structure-based rational design of covalent probes https://covalentmodifiers.blogspot.com/2025/08/structure-based-rational-design-of.html

Covalent Modifiers @covalentmod.bsky.social · Aug 27

Potent Inducers of Paraptosis through Electronic Tuning of Hemicyanine Electrophiles https://covalentmodifiers.blogspot.com/2025/08/potent-inducers-of-paraptosis-through.html

Covalent Modifiers @covalentmod.bsky.social · Aug 13

Profiling the proteome-wide selectivity of diverse electrophiles https://covalentmodifiers.blogspot.com/2025/08/profiling-proteome-wide-selectivity-of.html

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Covalent Modifiers @covalentmod.bsky.social · Aug 9

Discovery of an Orally Bioavailable Reversible Covalent SARS-CoV-2 Mpro Inhibitor with Pan-Coronavirus Activity https://covalentmodifiers.blogspot.com/2025/08/discovery-of-orally-bioavailable.html

Covalent Modifiers @covalentmod.bsky.social · Aug 8

A twist in the tale: shifting from covalent targeting of a tyrosine in JAK3 to a lysine in MK2 https://covalentmodifiers.blogspot.com/2025/08/a-twist-in-tale-shifting-from-covalent.html

Covalent Modifiers @covalentmod.bsky.social · Aug 2

AGPAT4 targeted covalent inhibitor potentiates targeted therapy to overcome cancer cell plasticity in hepatocellular carcinoma mouse models https://covalentmodifiers.blogspot.com/2025/08/agpat4-targeted-covalent-inhibitor.html

Covalent Modifiers @covalentmod.bsky.social · Aug 1

A Covalent Self-Reporting Peptide Degrader Enables Real-Time Monitoring of Targeted Protein Degradation In Vivo https://covalentmodifiers.blogspot.com/2025/08/a-covalent-self-reporting-peptide.html

Covalent Modifiers @covalentmod.bsky.social · Jul 29

Research progress on covalent inhibitors targeting alkaline amino acids https://covalentmodifiers.blogspot.com/2025/07/research-progress-on-covalent.html

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Covalent Modifiers @covalentmod.bsky.social · Jul 25

Orelabrutinib, an irreversible inhibitor of Bruton’s tyrosine kinase, for the treatment of systemic lupus erythematosus: a randomised, double-blind, placebo-controlled, phase Ib/IIa study https://covalentmodifiers.blogspot.com/2025/07/orelabrutinib-irreversible-inhibitor-of.html

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Covalent Modifiers @covalentmod.bsky.social · Jul 24

State-of-the-art covalent virtual screening with AlphaFold3 https://covalentmodifiers.blogspot.com/2025/07/state-of-art-covalent-virtual-screening.html

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Covalent Modifiers @covalentmod.bsky.social · Jul 23

The structure of KRASG12C bound to divarasib highlights features of potent switch-II pocket engagement https://covalentmodifiers.blogspot.com/2025/07/the-structure-of-krasg12c-bound-to.html

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