Repurposing of 8‐Hydroxyquinoline‐Based Butyrylcholinesterase and Cathepsin B Ligands as Potent Nonpeptidic Deoxyribonuclease I Inhibitors
Sign Up to like & getrecommendations! Published in 2022 at "ChemMedChem"
DOI: 10.1002/cmdc.202100694
Abstract: A library of 31 butyrylcholinesterase (BChE) and cathepsin B (CatB) inhibitors was screened in vitro for inhibition of deoxyribonuclease I (DNase I). Compounds 22, 8 and 7 are among the most potent synthetic non‐peptide DNase I… read more here.
Keywords: deoxyribonuclease; dnase; cathepsin; repurposing hydroxyquinoline ... See more keywords
Piperazine derivatives with potent drug moiety as efficient acetylcholinesterase, butyrylcholinesterase, and glutathione S‐transferase inhibitors
Sign Up to like & getrecommendations! Published in 2022 at "Journal of Biochemical and Molecular Toxicology"
DOI: 10.1002/jbt.23259
Abstract: Cholinesterases catalyze the breakdown of the neurotransmitter acetylcholine (ACh), a naturally occurring neurotransmitter, into choline and acetic acid, allowing the nervous system to function properly. In the human body, cholinesterases come in two types, including… read more here.
Keywords: piperazine derivatives; ache bche; bche; butyrylcholinesterase ... See more keywords
Interactions of human butyrylcholinesterase with phenylvalerate and acetylthiocholine as substrates and inhibitors: kinetic and molecular modeling approaches
Sign Up to like & getrecommendations! Published in 2019 at "Archives of Toxicology"
DOI: 10.1007/s00204-019-02423-8
Abstract: Phenyl valerate (PV) is a substrate for measuring the PVase activity of neuropathy target esterase (NTE), a key molecular event of organophosphorus-induced delayed neuropathy. A protein with PVase activity in chicken (model for delayed neurotoxicity)… read more here.
Keywords: human butyrylcholinesterase; butyrylcholinesterase; inhibition; site ... See more keywords
Targeting organophosphorus compounds poisoning by novel quinuclidine-3 oximes: development of butyrylcholinesterase-based bioscavengers
Sign Up to like & getrecommendations! Published in 2020 at "Archives of Toxicology"
DOI: 10.1007/s00204-020-02811-5
Abstract: A library of 14 mono-oxime quinuclidinium-based compounds with alkyl or benzyl substituent were synthesized and characterized in vitro as potential antidotes for organophosphorus compounds (OP) poisoning treatment. We evaluated their potency for reversible inhibition and… read more here.
Keywords: butyrylcholinesterase; organophosphorus compounds; based bioscavengers; quinuclidinium ... See more keywords
Alterations in acetylcholinesterase and butyrylcholinesterase activities in chronic obstructive pulmonary disease: relationships with oxidative and inflammatory markers
Sign Up to like & getrecommendations! Published in 2017 at "Molecular and Cellular Biochemistry"
DOI: 10.1007/s11010-017-3246-z
Abstract: This work focused on finding a relationship between acetylcholinesterase (AChE) and butyrylcholinesterase (BChE) activities and the development and severity of COPD. The possible link of these enzymes to oxidative and inflammatory processes was also investigated.… read more here.
Keywords: ache; butyrylcholinesterase; bche activities; bche ... See more keywords
Characterization of butyrylcholinesterase from porcine milk.
Sign Up to like & getrecommendations! Published in 2018 at "Archives of biochemistry and biophysics"
DOI: 10.1016/j.abb.2018.06.006
Abstract: Human butyrylcholinesterase (HuBChE) is under development for use as a pretreatment antidote against nerve agent toxicity. Animals are used to evaluate the efficacy of HuBChE for protection against organophosphorus nerve agents. Pharmacokinetic studies of HuBChE… read more here.
Keywords: pobche; porcine milk; butyrylcholinesterase; hubche ... See more keywords
Butyrylcholinesterase, a stereospecific in vivo bioscavenger against nerve agent intoxication.
Sign Up to like & getrecommendations! Published in 2019 at "Biochemical pharmacology"
DOI: 10.1016/j.bcp.2019.113670
Abstract: Human butyrylcholinesterase (E.C. 3.1.1.8) purified from blood plasma has previously been shown to provide protection against up to five and a half times the median lethal dose of an organophosphorus nerve agent in several animal… read more here.
Keywords: agent; human butyrylcholinesterase; butyrylcholinesterase; median lethal ... See more keywords
Purification and site-specific N-glycosylation analysis of human recombinant butyrylcholinesterase from Nicotiana benthamiana
Sign Up to like & getrecommendations! Published in 2019 at "Biochemical Engineering Journal"
DOI: 10.1016/j.bej.2018.11.004
Abstract: Abstract Butyrylcholinesterase (BChE) is a glycosylated serine hydrolase found in human serum that has been shown to protect against various cholinesterase-inhibiting organophosphate nerve agents. The supply of plasma-derived butyrylcholinesterase (hBChE) is constrained by the availability… read more here.
Keywords: purification; specific glycosylation; nicotiana benthamiana; butyrylcholinesterase ... See more keywords
Design, synthesis and biological evaluation of bambuterol analogues as novel inhibitors of butyrylcholinesterase.
Sign Up to like & getrecommendations! Published in 2017 at "European journal of medicinal chemistry"
DOI: 10.1016/j.ejmech.2016.08.061
Abstract: An increase activity of butyrylcholinesterase is believed to contribute to Alzheimer's disease. Bambuterol is a known potent inhibitor of butyrylcholinesterase, but it has undesired cardiac effects and less lipophilicity. Thirteen bambuterol analogues were synthesized using… read more here.
Keywords: design synthesis; butyrylcholinesterase; bambuterol analogues; biological evaluation ... See more keywords
The development of a butyrylcholinesterase porous pellet for innovative detection of cholinesterase inhibitors
Sign Up to like & getrecommendations! Published in 2017 at "European Journal of Pharmaceutical Sciences"
DOI: 10.1016/j.ejps.2017.09.015
Abstract: &NA; The aim of the presented research was the preparation of an innovative carrier with significantly improved properties for the fast and sensitive detection of cholinesterase inhibitors such as nerve agents. This innovative carrier was… read more here.
Keywords: cholinesterase inhibitors; butyrylcholinesterase; detection cholinesterase; activity ... See more keywords
Easy-Preparable Butyrylcholinesterase/Microgel Construct for Facilitated Organophosphate Biosensing.
Sign Up to like & getrecommendations! Published in 2017 at "Analytical chemistry"
DOI: 10.1021/acs.analchem.7b00732
Abstract: A versatile guest matrix was fabricated from a temperature- and pH-sensitive poly(N-isopropylacrylamide)-co-(3-(N,N-dimethylamino)propylmethacrylamide) microgel (poly(NIPAM-co-DMAPMA), MG) for the gentle incorporation of butyrylcholinesterase (BChE). The microgel/BChE films were built up on a surface of graphite-based screen-printed electrodes… read more here.
Keywords: butyrylcholinesterase; microgel; construct; spe mno2 ... See more keywords