Developing Covalent Protein Drugs via Proximity-Enabled Reactive Therapeutics
Sign Up to like & getrecommendations! Published in 2020 at "Cell"
DOI: 10.1016/j.cell.2020.05.028
Abstract: Small molecule covalent drugs provide desirable therapeutic properties over noncovalent ones for treating challenging diseases. The potential of covalent protein drugs, however, remains unexplored due to protein's inability to bind targets covalently. We report a… read more here.
Keywords: protein; covalent protein; protein drugs; proximity enabled ... See more keywords
Covalent Protein Labeling at Glutamic Acids.
Sign Up to like & getrecommendations! Published in 2017 at "Cell chemical biology"
DOI: 10.1016/j.chembiol.2017.03.015
Abstract: Covalent labeling of amino acids in proteins by reactive small molecules, in particular at cysteine SH and lysine NH groups, is a powerful approach to identify and characterize proteins and their functions. However, for the… read more here.
Keywords: covalent protein; protein labeling; covalent; biology ... See more keywords
Cov_DOX: A Method for Structure Prediction of Covalent Protein-Ligand Bindings.
Sign Up to like & getrecommendations! Published in 2022 at "Journal of medicinal chemistry"
DOI: 10.1021/acs.jmedchem.1c02007
Abstract: A handful of molecular docking tools have been extended to enable a covalent docking. However, all of them face the challenge brought by the covalent bond between proteins and ligands. Many covalent drug design scenarios… read more here.
Keywords: chemistry; covalent; method; covalent protein ... See more keywords
Involvement of Reactive Metabolites of Diclofenac in Cytotoxicity in Sandwich-Cultured Rat Hepatocytes
Sign Up to like & getrecommendations! Published in 2017 at "International Journal of Toxicology"
DOI: 10.1177/1091581817700584
Abstract: Background and Objectives: Diclofenac (DIC) is metabolized to reactive metabolites such as diclofenac acyl-β-d-glucuronide (DIC-AG). It is possible that such reactive metabolites could cause tissue damage by formation of covalent protein adducts and other modification… read more here.
Keywords: covalent protein; dic dic; metabolites diclofenac; sandwich cultured ... See more keywords
Technologies for Direct Detection of Covalent Protein–Drug Adducts
Sign Up to like & getrecommendations! Published in 2023 at "Pharmaceuticals"
DOI: 10.3390/ph16040547
Abstract: In the past two decades, drug candidates with a covalent binding mode have gained the interest of medicinal chemists, as several covalent anticancer drugs have successfully reached the clinic. As a covalent binding mode changes… read more here.
Keywords: direct detection; technologies direct; covalent protein; covalent ... See more keywords