Covalent Modifiers
@covalentmod.bsky.social
A BlueSky feed for the blog http://covalentmodifiers.blogspot.com. Discusses the covalent modification of proteins, particularly with regards to inhibitors.
Reimagining Druggability using Chemoproteomic Platforms
YouTube video by Drug Hunter
youtu.be
November 4, 2025 at 2:48 AM
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
October 20, 2025 at 6:00 PM
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
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
October 20, 2025 at 4:00 PM
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
Discovery of an Internal Alkyne Warhead Scaffold for Irreversible hTG2 Inhibition https://covalentmodifiers.blogspot.com/2025/10/discovery-of-internal-alkyne-warhead.html
October 12, 2025 at 5:00 PM
Discovery of an Internal Alkyne Warhead Scaffold for Irreversible hTG2 Inhibition https://covalentmodifiers.blogspot.com/2025/10/discovery-of-internal-alkyne-warhead.html
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
October 10, 2025 at 4:00 PM
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
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
October 5, 2025 at 1:00 AM
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
Sulfinyl Aziridines as Stereoselective Covalent Destabilizing Degraders of the Oncogenic Transcription Factor MYC https://covalentmodifiers.blogspot.com/2025/09/sulfinyl-aziridines-as-stereoselective.html
September 27, 2025 at 6:00 PM
Sulfinyl Aziridines as Stereoselective Covalent Destabilizing Degraders of the Oncogenic Transcription Factor MYC https://covalentmodifiers.blogspot.com/2025/09/sulfinyl-aziridines-as-stereoselective.html
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
September 13, 2025 at 3:00 PM
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
A covalent inhibitor targeting Cys16 on RhoA in colorectal cancer https://covalentmodifiers.blogspot.com/2025/09/a-covalent-inhibitor-targeting-cys16-on.html
September 9, 2025 at 3:00 PM
A covalent inhibitor targeting Cys16 on RhoA in colorectal cancer https://covalentmodifiers.blogspot.com/2025/09/a-covalent-inhibitor-targeting-cys16-on.html
Covalent Irreversible Inhibitors of Tetracycline Destructases https://covalentmodifiers.blogspot.com/2025/09/covalent-irreversible-inhibitors-of.html
September 4, 2025 at 2:00 PM
Covalent Irreversible Inhibitors of Tetracycline Destructases https://covalentmodifiers.blogspot.com/2025/09/covalent-irreversible-inhibitors-of.html
Covalent chemical probes https://covalentmodifiers.blogspot.com/2025/09/covalent-chemical-probes.html
September 2, 2025 at 4:00 PM
Covalent chemical probes https://covalentmodifiers.blogspot.com/2025/09/covalent-chemical-probes.html
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
September 1, 2025 at 11:00 PM
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
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
September 1, 2025 at 2:00 AM
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
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
August 30, 2025 at 10:00 PM
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
Structure-based rational design of covalent probes https://covalentmodifiers.blogspot.com/2025/08/structure-based-rational-design-of.html
August 29, 2025 at 3:00 AM
Structure-based rational design of covalent probes https://covalentmodifiers.blogspot.com/2025/08/structure-based-rational-design-of.html
Potent Inducers of Paraptosis through Electronic Tuning of Hemicyanine Electrophiles https://covalentmodifiers.blogspot.com/2025/08/potent-inducers-of-paraptosis-through.html
August 27, 2025 at 6:00 AM
Potent Inducers of Paraptosis through Electronic Tuning of Hemicyanine Electrophiles https://covalentmodifiers.blogspot.com/2025/08/potent-inducers-of-paraptosis-through.html
Profiling the proteome-wide selectivity of diverse electrophiles https://covalentmodifiers.blogspot.com/2025/08/profiling-proteome-wide-selectivity-of.html
August 13, 2025 at 4:00 PM
Profiling the proteome-wide selectivity of diverse electrophiles https://covalentmodifiers.blogspot.com/2025/08/profiling-proteome-wide-selectivity-of.html
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
August 9, 2025 at 8:00 PM
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
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
August 8, 2025 at 5:00 PM
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
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
August 2, 2025 at 9:00 PM
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
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
August 1, 2025 at 4:00 PM
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
Research progress on covalent inhibitors targeting alkaline amino acids https://covalentmodifiers.blogspot.com/2025/07/research-progress-on-covalent.html
July 29, 2025 at 2:00 AM
Research progress on covalent inhibitors targeting alkaline amino acids https://covalentmodifiers.blogspot.com/2025/07/research-progress-on-covalent.html
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
July 25, 2025 at 4:00 PM
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
State-of-the-art covalent virtual screening with AlphaFold3 https://covalentmodifiers.blogspot.com/2025/07/state-of-art-covalent-virtual-screening.html
July 24, 2025 at 5:00 PM
State-of-the-art covalent virtual screening with AlphaFold3 https://covalentmodifiers.blogspot.com/2025/07/state-of-art-covalent-virtual-screening.html
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
July 23, 2025 at 10:00 PM
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