Covalent Modifiers

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A mastodon feed for the blog http://covalentmodifiers.blogspot.com. Discusses the covalent modification of proteins, particularly with regards to inhibitors.
covalentdrug
irreversibleprotein
chemistrypharmaceutical
inhibitor
An allosteric cyclin E-CDK2 site mapped by paralog hopping with covalent probes

Yuanjin Zhang, Zhonglin Liu, Marscha Hirschi, Oleg Brodsky, Eric Johnson, Sang Joon Won, Asako Nagata, Divya Bezwada, Matthew D. Petroski, J...

Selective Covalent Inhibiting JNK3 by Small Molecules for Parkinson's Diseases

Liang Ouyang, Wen Shuai, Panpan Yang, Huan Xiao, Yumeng Zhu, Faqian Bu, Aoxue Wang, Qiu Sun, Guan Wang Angewandte Chemie   2024 e202411037 ...

Development of ketalized unsaturated saccharides as multifunctional cysteine-targeting covalent warheads https://covalentmodifiers.blogspot.com/2024/09/development-of-ketalized-unsaturated.html?utm_source=dlvr.it&utm_medium=mastodon
Development of ketalized unsaturated saccharides as multifunctional cysteine-targeting covalent warheads

Dong, S., Huang, H., Li, J.  et al. Commun Chem   7 , 201 (2024).  https://doi.org/10.1038/s42004-024-01279-z Multi-functional cysteine-targ...

From Mechanism-Based Retaining Glycosidase Inhibitors to Activity-Based Glycosidase Profiling https://covalentmodifiers.blogspot.com/2024/09/from-mechanism-based-retaining.html?utm_source=dlvr.it&utm_medium=mastodon
From Mechanism-Based Retaining Glycosidase Inhibitors to Activity-Based Glycosidase Profiling

  Marta Artola, Johannes M. F. G. Aerts, Gijsbert A. van der Marel, Carme Rovira, Jeroen D. C. Codée, Gideon J. Davies, and Herman S. Overkl...

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?utm_source=dlvr.it&utm_medium=mastodon
SuFEx Chemistry Enables Covalent Assembly of a 280-kDa 18-Subunit Pore-Forming Complex

Lee Schnaider, Sophia Tan, Pratik R. Singh, Floriana Capuano, Alistair J. Scott, Richard Hambley, Lei Lu, Hyunjun Yang, E. Jayne Wallace, Hy...

Targeted Protein Localization by Covalent 14–3–3 Recruitment

 Qian Shao, Tuong Nghi Duong, Inji Park, Lauren M. Orr, and Daniel K. Nomura Journal of the American Chemical Society 2024 DOI: 10.1021/jacs...

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?utm_source=dlvr.it&utm_medium=mastodon
Aminomethyl Salicylaldehydes Lock onto a Surface Lysine by Forming an Extended Intramolecular Hydrogen Bond Network

Jacqueline Weaver, Gregory B. Craven, Linh Tram, Hao Chen, and Jack Taunton Journal of the American Chemical Society   2024 DOI: 10.1021/jac...

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?utm_source=dlvr.it&utm_medium=mastodon
Discovery of a Covalent Inhibitor of Pro-Caspase-1 Zymogen Blocking NLRP3 Inflammasome Activation and Pyroptosis

Dongyi Cao, Ruiying Xi, Hongye Li, Zhonghui Zhang, Xiaoke Shi, Shanshan Li, Yujie Jin, Wanli Liu, Guolin Zhang, Xiaohua Liu, Shunxi Dong, Xi...

Discovering Covalent Cyclic Peptide Inhibitors of 2 Peptidyl Arginine Deiminase 4 (PADI4) Using mRNA3 Display with a Genetically Encoded Electrophilic 4 Warhead https://covalentmodifiers.blogspot.com/2024/08/discovering-covalent-cyclic-peptide.html?utm_source=dlvr.it&utm_medium=mastodon
Discovering Covalent Cyclic Peptide Inhibitors of 2 Peptidyl Arginine Deiminase 4 (PADI4) Using mRNA3 Display with a Genetically Encoded Electrophilic 4 Warhead

 Isabel Mathiesen, Ewen Calder, Simone Kunzelmann, Louise Walport  ChemRxiv , 2024 https://doi.org/10.26434/chemrxiv-2024-w8nbl Covalent dru...

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?utm_source=dlvr.it&utm_medium=mastodon
Electrophilic proximity-inducing synthetic adapters enhance universal T cell function by covalently enforcing immune receptor signaling [@RulloLab]

Nickolas J. Serniuck, Eden Kapcan, Duane Moogk,Allyson E. Moore,Benjamin P.M. Lake, Galina Denisova,Joanne A. Hammill,Jonathan L. Bramson, A...