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In vitro characterization of novel potential modulators of cholinesterases
Táborská, Lenka ; Šorf, Aleš (advisor) ; Ťupová, Lenka (referee)
Charles University Faculty of Pharmacy in Hradec Králové Department of Social and Clinical Pharmacy Candidate: Lenka Táborská Supervisor: PharmDr. Aleš Šorf, Ph.D. Consultant: RNDr. Ľubica Múčková, Ph.D. Title of diploma thesis: In vitro characterization of novel potential modulators of cholinesterases This thesis focuses on investigating the interaction of newly synthesized potential drugs with human cholinesterases (ChE), particularly acetylcholinesterase (AChE) and butyrylcholinesterase (BChE). The main objective is to assess the inhibitory potential of these molecules against recombinant human forms of AChE and BChE. Furthermore, the cytotoxicity of selected compounds is examined using a colorimetric method on the SH-SY5Y cell line employing MTT tetrazolium salt. The theoretical part of the thesis delves into the structure and functions of cholinesterases, especially AChE and BChE, as well as the cognitive aspects of neurodegenerative diseases such as Alzheimer disease (AD), Parkinson's disease (PD), amyotrophic lateral sclerosis (ALS), and multiple system atrophy (MSA). Additionally, it addresses the toxic effects of organophosphates, which can inhibit the AChE enzyme, along with methods for determining cholinesterase activity. The practical part focuses on experimentally determining the...
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