Detailed Information on Publication Record
2017
Development and comprehensive comparison of two on-line capillary electrophoretic methods for beta-secretase inhibitor screening
ŘEMÍNEK, Roman, Lucie SLEZÁČKOVÁ, Jan SCHEJBAL and Zdeněk GLATZBasic information
Original name
Development and comprehensive comparison of two on-line capillary electrophoretic methods for beta-secretase inhibitor screening
Name in Czech
Vývoj a srovnání dvou on-line kapilárně elektroforetických metod pro screening inhibitorů beta-sekretasy
Authors
ŘEMÍNEK, Roman (203 Czech Republic, belonging to the institution), Lucie SLEZÁČKOVÁ (203 Czech Republic, belonging to the institution), Jan SCHEJBAL (203 Czech Republic, belonging to the institution) and Zdeněk GLATZ (203 Czech Republic, guarantor, belonging to the institution)
Edition
Journal of Chromatography A, Amsterdam, ELSEVIER SCIENCE BV, 2017, 0021-9673
Other information
Language
English
Type of outcome
Článek v odborném periodiku
Field of Study
10600 1.6 Biological sciences
Country of publisher
Czech Republic
Confidentiality degree
není předmětem státního či obchodního tajemství
References:
Impact factor
Impact factor: 3.716
RIV identification code
RIV/00216224:14310/17:00095133
Organization unit
Faculty of Science
UT WoS
000412621200010
Keywords (in Czech)
kapilární elektroforéza; Alzheimerova choroba; beta-sekretasa; kinetika; inhibice
Keywords in English
capillary electrophoresis; Alzheimer's disease; beta-secretase; kinetics; inhibition
Tags
Tags
International impact, Reviewed
Změněno: 6/2/2019 11:46, prof. RNDr. Zdeněk Glatz, CSc.
V originále
Alzheimer’s disease is the most common cause of dementia, afflicting over 34 million patients worldwide. Since beta-secretase is a rate-limiting enzyme of the production of neurotoxic beta-amyloid peptide oligomers abnormally accumulated in the affected brain tissue, its specific inhibition appears to be a promising approach to slowing down or even stopping the progression of the disease. Hence two on-line capillary electrophoretic methods for studies of beta-secretase activity based on the principles of transverse diffusion of laminar flow profiles and electrophoretically mediated microanalysis were developed, both using a simple unlabeled peptide substrate and UV detection. The optimized procedures were thoroughly validated and applied for determining the enzyme’s kinetic parameters and the inhibition characteristics of two potent probe inhibitors. The resulting values were found to be comparable to literature data obtained with other analytical techniques. The suitability of the employed methodologies for different experimental designs is discussed on the basis of a statistical evaluation of the experimental data. The presented methods constitute a miniaturized and fully automated tool, which should be suitable for kinetic and inhibition studies of beta-secretase as a target for Alzheimer’s disease drug discovery in the early stages of the development of a new drug.
In Czech
Byly zavedeny dvě on-line metody pro kinetické a inhibiční studie beta-sekretasy, založené na principu techniky příčné difuze laminárního toku a elektroforeticky zprostředkované mikroanalýzy. Praktické aspekty zavedených metod byly posléze srovnány na základě dat získaných pomocí jednotlivých metod.
Links
| GA16-06106S, research and development project |
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| MUNI/A/1278/2016, interní kód MU |
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