Butyrylcholinesterase (BChE) is a serine hydrolase (EC 3.1.1.8) which can be found in most animal tissues. This enzyme has a broad spectrum of efficacy against organophosphorus compounds, which makes it a prime candidate for the role of stoichiometric bioscavenger. Development of a new-age DNA-encoded bioscavenger is a vival task. Several transgenic expression systems of human BChE were develop...

A new assay has been developed for detection of butyrylcholinesterase (EC 3.1.1.8) activity based upon the change in absorbance of phenol red, caused by the r e l ease of bu ty r i c acid from the substrate. Using c o m m e r c i a l l y avai lable enzyme prepared from horse serum, linear, dose-related decreases in absorbance were obtained, generally with correlation values of 0.965 or greater....

Isosorbide-2-carbamate-5-esters are highly potent and selective butyrylcholinesterase inhibitors with potential utility in the treatment of Alzheimer's Disease (AD). They are stable in human plasma but in mouse plasma they undergo hydrolysis at the 5-ester group potentially attenuating in vivo potency. In this paper we explore the role of the 5-position in modulating potency. The focus of the s...

Recombinant proteins represent a large sector of the biopharma market. Determination of the main elimination pathways raises the opportunities to significantly increase their half-lives in vivo. However, evaluation of biodegradation of pharmaceutical biopolymers performed in the course of pre-clinical studies is frequently complicated. Noninvasive pharmacokinetic and biodistribution studies in ...

The function of the enzyme butyrylcholinesterase (BChE) both in serum and in brain is unclear. In serum, BChE has been found complexed with several biomedically relevant proteins, with which it could function in concert. Here, the existence of a similar complex formed between BChE and sero-transferrin from adult chicken serum was elucidated. In order to identify both proteins unequivocally, we ...

The title compound, C20H24N2O4, is the product of a ring-expansion reaction from a seven-membered hexa-hydro-azepine to a nine-membered azonine. The azonine ring of the mol-ecule adopts a chair-boat conformation. In the crystal, mol-ecules are linked by bifurcated N-H⋯(O,O) hydrogen bonds, generating [010] zigzag chains. The title compound shows inhibitory activity against acetyl-cholinesterase...

Highly efficient and rapid lead compound evaluation for estimation of inhibition parameters and type of inhibition is proposed. This is based on a single progress-curve measurement in the presence of each candidate compound, followed by the simultaneous analysis of all of these curves using the ENZO enzyme kinetics suite, which can be implemented as a web application. In the first step, all of ...

We studied the influence of some factors on plasma butyrylcholinesterase activity (BChE) and we assessed the health status of agricultural workers and looked for the effects of chronic exposure to pesticides, in the aim to determinate factors that must be considered for interpretation of BChE, for occupational monitoring of workers exposed to pesticides. The study was carried out in 110 workers...

The activity of every substance I inhibiting an enzymatic reaction can be approximately evaluated by the index PI50. This paper describes a simple and fast method of estimate and/ or determination of this index. The method is based on the linearity of the dependence of the ratio of reaction rates of uninhibited and inhibited reaction vs. concentration of the inhibitor at constant initial substr...