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.
Site-specific activation of the proton pumpinhibitor rabeprazole by tetrathiolate zinccentres https://covalentmodifiers.blogspot.com/2025/02/site-specific-activation-of-proton.html
February 22, 2025 at 2:00 AM
Site-specific activation of the proton pumpinhibitor rabeprazole by tetrathiolate zinccentres https://covalentmodifiers.blogspot.com/2025/02/site-specific-activation-of-proton.html
Total syntheses of cyclohelminthol I–IV reveal a new cysteine-selective covalent reactive group https://covalentmodifiers.blogspot.com/2025/01/total-syntheses-of-cyclohelminthol-iiv.html
January 31, 2025 at 1:00 AM
Total syntheses of cyclohelminthol I–IV reveal a new cysteine-selective covalent reactive group https://covalentmodifiers.blogspot.com/2025/01/total-syntheses-of-cyclohelminthol-iiv.html
Species Dependent Metabolism of a Covalent nsP2 Protease Inhibitor with in Vivo Anti-alphaviral Activity https://covalentmodifiers.blogspot.com/2025/01/species-dependent-metabolism-of.html
January 20, 2025 at 7:01 AM
Species Dependent Metabolism of a Covalent nsP2 Protease Inhibitor with in Vivo Anti-alphaviral Activity https://covalentmodifiers.blogspot.com/2025/01/species-dependent-metabolism-of.html
Covalent Plant Natural Product that Potentiates Antitumor Immunity https://covalentmodifiers.blogspot.com/2025/01/covalent-plant-natural-product-that.html
January 14, 2025 at 2:00 AM
Covalent Plant Natural Product that Potentiates Antitumor Immunity https://covalentmodifiers.blogspot.com/2025/01/covalent-plant-natural-product-that.html
Exploring Extended Warheads toward Developing Cysteine-Targeted Covalent Kinase Inhibitors https://covalentmodifiers.blogspot.com/2024/12/exploring-extended-warheads-toward.html
December 14, 2024 at 6:00 AM
Exploring Extended Warheads toward Developing Cysteine-Targeted Covalent Kinase Inhibitors https://covalentmodifiers.blogspot.com/2024/12/exploring-extended-warheads-toward.html
Open-source Electrophilic Fragment Screening Platform to Identify Chemical Starting Points for UCHL1 Covalent Inhibitors https://covalentmodifiers.blogspot.com/2024/12/open-source-electrophilic-fragment.html
December 3, 2024 at 8:00 PM
Open-source Electrophilic Fragment Screening Platform to Identify Chemical Starting Points for UCHL1 Covalent Inhibitors https://covalentmodifiers.blogspot.com/2024/12/open-source-electrophilic-fragment.html
Lysine-Targeted Covalent Inhibitors of PI3Kδ Synthesis and Screening by In Situ Interaction Upgradation https://covalentmodifiers.blogspot.com/2024/11/lysine-targeted-covalent-inhibitors-of.html
November 25, 2024 at 8:00 PM
Lysine-Targeted Covalent Inhibitors of PI3Kδ Synthesis and Screening by In Situ Interaction Upgradation https://covalentmodifiers.blogspot.com/2024/11/lysine-targeted-covalent-inhibitors-of.html
Potent Inhibition and Rapid Photoactivation of Endogenous Bruton’s Tyrosine Kinase Activity in Native Cells via Opto-Covalent Modulators https://covalentmodifiers.blogspot.com/2024/10/potent-inhibition-and-rapid_15.html
October 15, 2024 at 3:00 PM
Potent Inhibition and Rapid Photoactivation of Endogenous Bruton’s Tyrosine Kinase Activity in Native Cells via Opto-Covalent Modulators https://covalentmodifiers.blogspot.com/2024/10/potent-inhibition-and-rapid_15.html
Reversible covalent c-Jun N-terminal kinase inhibitors targeting a specific cysteine by precision-guided Michael-acceptor warheads https://covalentmodifiers.blogspot.com/2024/10/reversible-covalent-c-jun-n-terminal.html
October 10, 2024 at 9:00 PM
Reversible covalent c-Jun N-terminal kinase inhibitors targeting a specific cysteine by precision-guided Michael-acceptor warheads https://covalentmodifiers.blogspot.com/2024/10/reversible-covalent-c-jun-n-terminal.html
Multi-tiered chemical proteomic maps of tryptoline acrylamide–protein interactions in cancer cells https://covalentmodifiers.blogspot.com/2024/10/multi-tiered-chemical-proteomic-maps-of.html
October 1, 2024 at 6:00 PM
Multi-tiered chemical proteomic maps of tryptoline acrylamide–protein interactions in cancer cells https://covalentmodifiers.blogspot.com/2024/10/multi-tiered-chemical-proteomic-maps-of.html
Activity-Based Acylome Profiling with N-(Cyanomethyl)-N-(phenylsulfonyl)amides for Targeted Lysine Acylation and Post-Translational Control of Protein Function in Cells https://covalentmodifiers.blogspot.com/2024/09/activity-based-acylome-profiling-with-n.html
October 1, 2024 at 4:00 AM
Activity-Based Acylome Profiling with N-(Cyanomethyl)-N-(phenylsulfonyl)amides for Targeted Lysine Acylation and Post-Translational Control of Protein Function in Cells https://covalentmodifiers.blogspot.com/2024/09/activity-based-acylome-profiling-with-n.html
Isocyanides inhibit bacterial pathogens by covalent targeting of essential metabolic enzymes https://covalentmodifiers.blogspot.com/2024/09/isocyanides-inhibit-bacterial-pathogens.html
September 30, 2024 at 8:00 PM
Isocyanides inhibit bacterial pathogens by covalent targeting of essential metabolic enzymes https://covalentmodifiers.blogspot.com/2024/09/isocyanides-inhibit-bacterial-pathogens.html
Peptide and Protein Cysteine Modification Enabled by Hydrosulfuration of Ynamide https://covalentmodifiers.blogspot.com/2024/09/peptide-and-protein-cysteine.html
September 26, 2024 at 3:00 PM
Peptide and Protein Cysteine Modification Enabled by Hydrosulfuration of Ynamide https://covalentmodifiers.blogspot.com/2024/09/peptide-and-protein-cysteine.html
An allosteric cyclin E-CDK2 site mapped by paralog hopping with covalent probes https://covalentmodifiers.blogspot.com/2024/09/an-allosteric-cyclin-e-cdk2-site-mapped.html
September 24, 2024 at 3:00 PM
An allosteric cyclin E-CDK2 site mapped by paralog hopping with covalent probes https://covalentmodifiers.blogspot.com/2024/09/an-allosteric-cyclin-e-cdk2-site-mapped.html
Selective Covalent Inhibiting JNK3 by Small Molecules for Parkinson's Diseases https://covalentmodifiers.blogspot.com/2024/09/selective-covalent-inhibiting-jnk3-by.html
September 19, 2024 at 5:00 AM
Selective Covalent Inhibiting JNK3 by Small Molecules for Parkinson's Diseases https://covalentmodifiers.blogspot.com/2024/09/selective-covalent-inhibiting-jnk3-by.html
Development of ketalized unsaturated saccharides as multifunctional cysteine-targeting covalent warheads https://covalentmodifiers.blogspot.com/2024/09/development-of-ketalized-unsaturated.html
September 14, 2024 at 2:00 PM
Development of ketalized unsaturated saccharides as multifunctional cysteine-targeting covalent warheads https://covalentmodifiers.blogspot.com/2024/09/development-of-ketalized-unsaturated.html
From Mechanism-Based Retaining Glycosidase Inhibitors to Activity-Based Glycosidase Profiling https://covalentmodifiers.blogspot.com/2024/09/from-mechanism-based-retaining.html
September 4, 2024 at 1:00 PM
From Mechanism-Based Retaining Glycosidase Inhibitors to Activity-Based Glycosidase Profiling https://covalentmodifiers.blogspot.com/2024/09/from-mechanism-based-retaining.html
SuFEx Chemistry Enables Covalent Assembly of a 280-kDa 18-Subunit Pore-Forming Complex https://covalentmodifiers.blogspot.com/2024/09/sufex-chemistry-enables-covalent.html
September 1, 2024 at 10:00 PM
SuFEx Chemistry Enables Covalent Assembly of a 280-kDa 18-Subunit Pore-Forming Complex https://covalentmodifiers.blogspot.com/2024/09/sufex-chemistry-enables-covalent.html
Targeted Protein Localization by Covalent 14–3–3 Recruitment https://covalentmodifiers.blogspot.com/2024/08/targeted-protein-localization-by.html
August 28, 2024 at 10:00 PM
Targeted Protein Localization by Covalent 14–3–3 Recruitment https://covalentmodifiers.blogspot.com/2024/08/targeted-protein-localization-by.html
Aminomethyl Salicylaldehydes Lock onto a Surface Lysine by Forming an Extended Intramolecular Hydrogen Bond Network https://covalentmodifiers.blogspot.com/2024/08/aminomethyl-salicylaldehydes-lock-onto.html
August 27, 2024 at 6:00 PM
Aminomethyl Salicylaldehydes Lock onto a Surface Lysine by Forming an Extended Intramolecular Hydrogen Bond Network https://covalentmodifiers.blogspot.com/2024/08/aminomethyl-salicylaldehydes-lock-onto.html
Discovery of a Covalent Inhibitor of Pro-Caspase-1 Zymogen Blocking NLRP3 Inflammasome Activation and Pyroptosis https://covalentmodifiers.blogspot.com/2024/08/discovery-of-covalent-inhibitor-of-pro.html
August 21, 2024 at 10:00 PM
Discovery of a Covalent Inhibitor of Pro-Caspase-1 Zymogen Blocking NLRP3 Inflammasome Activation and Pyroptosis https://covalentmodifiers.blogspot.com/2024/08/discovery-of-covalent-inhibitor-of-pro.html
Electrophilic proximity-inducing synthetic adapters enhance universal T cell function by covalently enforcing immune receptor signaling [@RulloLab] https://covalentmodifiers.blogspot.com/2024/08/electrophilic-proximity-inducing.html
August 14, 2024 at 4:00 PM
Electrophilic proximity-inducing synthetic adapters enhance universal T cell function by covalently enforcing immune receptor signaling [@RulloLab] https://covalentmodifiers.blogspot.com/2024/08/electrophilic-proximity-inducing.html
Multi-tiered chemical proteomic maps of tryptoline acrylamide–protein interactions in cancer cells [@EvertNjomen] https://covalentmodifiers.blogspot.com/2024/08/multi-tiered-chemical-proteomic-maps-of.html
August 13, 2024 at 11:00 PM
Multi-tiered chemical proteomic maps of tryptoline acrylamide–protein interactions in cancer cells [@EvertNjomen] https://covalentmodifiers.blogspot.com/2024/08/multi-tiered-chemical-proteomic-maps-of.html
Discovery of Thioether-Cyclized Macrocyclic Covalent Inhibitors by mRNA Display https://covalentmodifiers.blogspot.com/2024/08/tong-lan-cheng-peng-xiyuan-yao-rachel.html
August 13, 2024 at 4:00 PM
Discovery of Thioether-Cyclized Macrocyclic Covalent Inhibitors by mRNA Display https://covalentmodifiers.blogspot.com/2024/08/tong-lan-cheng-peng-xiyuan-yao-rachel.html
Predicting the Intravenous Pharmacokinetics of Covalent Drugs in Animals and Humans https://covalentmodifiers.blogspot.com/2024/08/predicting-intravenous-pharmacokinetics.html
August 5, 2024 at 12:00 AM
Predicting the Intravenous Pharmacokinetics of Covalent Drugs in Animals and Humans https://covalentmodifiers.blogspot.com/2024/08/predicting-intravenous-pharmacokinetics.html