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.
Protein tyrosine phosphatase inactivation by electrophilic tyrosine modification https://covalentmodifiers.blogspot.com/2026/01/protein-tyrosine-phosphatase.html
January 20, 2026 at 4:00 PM
Protein tyrosine phosphatase inactivation by electrophilic tyrosine modification https://covalentmodifiers.blogspot.com/2026/01/protein-tyrosine-phosphatase.html
Covalent Peptide-Encoded Libraries Enable Discovery of Inhibitors of Epidermal Growth Factor Receptor (EGFR) https://covalentmodifiers.blogspot.com/2026/01/covalent-peptide-encoded-libraries.html
January 19, 2026 at 3:00 AM
Covalent Peptide-Encoded Libraries Enable Discovery of Inhibitors of Epidermal Growth Factor Receptor (EGFR) https://covalentmodifiers.blogspot.com/2026/01/covalent-peptide-encoded-libraries.html
Structure-Guided Optimization of 4-Chloro-Pyrazolopyridine Analogs for Covalent PREP Inhibition https://covalentmodifiers.blogspot.com/2026/01/structure-guided-optimization-of-4.html
January 12, 2026 at 2:00 PM
Structure-Guided Optimization of 4-Chloro-Pyrazolopyridine Analogs for Covalent PREP Inhibition https://covalentmodifiers.blogspot.com/2026/01/structure-guided-optimization-of-4.html
Ninhydrin as a covalent warhead for chemical proteomic-enabled discovery and selective engagement of reactive arginines https://covalentmodifiers.blogspot.com/2026/01/ninhydrin-as-covalent-warhead-for.html
January 6, 2026 at 7:00 PM
Ninhydrin as a covalent warhead for chemical proteomic-enabled discovery and selective engagement of reactive arginines https://covalentmodifiers.blogspot.com/2026/01/ninhydrin-as-covalent-warhead-for.html
Peptide-based covalent inhibitor of tubulin detyrosination promotes mesenchymal-to-epithelial transition in lung cancer cells https://covalentmodifiers.blogspot.com/2026/01/peptide-based-covalent-inhibitor-of.html
January 4, 2026 at 6:00 AM
Peptide-based covalent inhibitor of tubulin detyrosination promotes mesenchymal-to-epithelial transition in lung cancer cells https://covalentmodifiers.blogspot.com/2026/01/peptide-based-covalent-inhibitor-of.html
Discovery of a First-in-Class Covalent Allosteric SHP1 Inhibitor with Immunotherapeutic Activity https://covalentmodifiers.blogspot.com/2025/12/discovery-of-first-in-class-covalent.html
December 29, 2025 at 7:00 PM
Discovery of a First-in-Class Covalent Allosteric SHP1 Inhibitor with Immunotherapeutic Activity https://covalentmodifiers.blogspot.com/2025/12/discovery-of-first-in-class-covalent.html
Covalent Drug Binding in Live Cells Monitored by Mid-Infrared Quantum Cascade Laser Spectroscopy: Photoactive Yellow Protein as a Model System https://covalentmodifiers.blogspot.com/2025/12/covalent-drug-binding-in-live-cells.html
December 23, 2025 at 8:00 AM
Covalent Drug Binding in Live Cells Monitored by Mid-Infrared Quantum Cascade Laser Spectroscopy: Photoactive Yellow Protein as a Model System https://covalentmodifiers.blogspot.com/2025/12/covalent-drug-binding-in-live-cells.html
A practical method for determining the rate of covalent modification of fragments and leads https://covalentmodifiers.blogspot.com/2025/12/a-practical-method-for-determining-rate.html
December 20, 2025 at 3:00 AM
A practical method for determining the rate of covalent modification of fragments and leads https://covalentmodifiers.blogspot.com/2025/12/a-practical-method-for-determining-rate.html
Stereoselective Degradation of Diacylglycerol Kinases Potentiate T cell Activation and Tumor Cell Cytotoxicity https://covalentmodifiers.blogspot.com/2025/12/stereoselective-degradation-of.html
December 13, 2025 at 6:00 AM
Stereoselective Degradation of Diacylglycerol Kinases Potentiate T cell Activation and Tumor Cell Cytotoxicity https://covalentmodifiers.blogspot.com/2025/12/stereoselective-degradation-of.html
Identification of VVD-214/RO7589831, a Clinical-Stage, Covalent Allosteric Inhibitor of WRN Helicase for the Treatment of MSI-High Cancers https://covalentmodifiers.blogspot.com/2025/12/identification-of-vvd-214ro7589831.html
December 11, 2025 at 3:00 AM
Identification of VVD-214/RO7589831, a Clinical-Stage, Covalent Allosteric Inhibitor of WRN Helicase for the Treatment of MSI-High Cancers https://covalentmodifiers.blogspot.com/2025/12/identification-of-vvd-214ro7589831.html
The Development of UM-203, A Reversible Covalent STING Antagonis https://covalentmodifiers.blogspot.com/2025/12/the-development-of-um-203-reversible.html
December 10, 2025 at 10:00 PM
The Development of UM-203, A Reversible Covalent STING Antagonis https://covalentmodifiers.blogspot.com/2025/12/the-development-of-um-203-reversible.html
A Highly Reactive Cysteine-Targeted Acrylophenone Chemical Probe That Enables Peptide/Protein Bioconjugation and Chemoproteomics Analysis https://covalentmodifiers.blogspot.com/2025/12/a-highly-reactive-cysteine-targeted.html
December 7, 2025 at 5:00 AM
A Highly Reactive Cysteine-Targeted Acrylophenone Chemical Probe That Enables Peptide/Protein Bioconjugation and Chemoproteomics Analysis https://covalentmodifiers.blogspot.com/2025/12/a-highly-reactive-cysteine-targeted.html
Preclinical characterization of EGT710, an oral non-peptidomimetic reversible covalent SARS-CoV-2 main protease inhibitor https://covalentmodifiers.blogspot.com/2025/11/preclinical-characterization-of-egt710.html
December 1, 2025 at 2:00 AM
Preclinical characterization of EGT710, an oral non-peptidomimetic reversible covalent SARS-CoV-2 main protease inhibitor https://covalentmodifiers.blogspot.com/2025/11/preclinical-characterization-of-egt710.html
Fast and Site-Specific Covalent Targeting of Proteins by Arylfluorosulfate-Modified Aptamers https://covalentmodifiers.blogspot.com/2025/11/fast-and-site-specific-covalent.html
November 25, 2025 at 4:00 PM
Fast and Site-Specific Covalent Targeting of Proteins by Arylfluorosulfate-Modified Aptamers https://covalentmodifiers.blogspot.com/2025/11/fast-and-site-specific-covalent.html
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