Rapid mechanistic evaluation and parameter estimation of putative inhibitors in a single-step progress-curve analysis : the case of horse butyrylcholinesterase

Stojan, Jure (author)

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 the candidate ligands are tested as competitive inhibitors. Where the theoretical curves do not correspond to the experimental data, minimal additional measurements are added, with subsequent processing according to modified reaction mechanisms.

• Language: English
• Keywords: enzymic mechanism, inhibitors, reactivators, butyrylcholinestersae
• Work type: Article
• Typology: 1.01 - Original Scientific Article
• Organization: MF - Faculty of Medicine
• Publication status: Published
• Publication version: Version of Record
• Year: 2017
• Number of pages: 9 str.
• Numbering: Vol. 22, iss. 8, art. 1248
• PID: 20.500.12556/RUL-131013
• UDC: 577
• ISSN on article: 1420-3049
• DOI: 10.3390/molecules22081248
• COBISS.SI-ID: 34387929
• Publication date in RUL: 21.09.2021

Record is a part of a journal

• Title: Molecules
• Shortened title: Molecules
• Publisher: MDPI
• ISSN: 1420-3049
• COBISS.SI-ID: 18462981

Licences

• License: CC BY 4.0, Creative Commons Attribution 4.0 International
• Link: http://creativecommons.org/licenses/by/4.0/
• Description: This is the standard Creative Commons license that gives others maximum freedom to do what they want with the work as long as they credit the author.
• Licensing start date: 01.08.2017

Secondary language

• Language: Slovenian
• Keywords: encimski mehanizem, inhibitorji, reaktivatorji

Projects

• Funder: ARRS - Slovenian Research Agency
• Project number: P1-0170
• Name: Molekulski mehanizmi uravnavanja celičnih procesov v povezavi z nekaterimi boleznimi pri človeku