Publication detail

Preparing of potencional proteasome and kinasis inhibitors based on salicylamides with acrylamide moiety

Authors: Pilařová Eliška | Imramovský Aleš | Pauk Karel | Jorda Radek | Kryštof Vladimír

Year: 2019

Type of publication: ostatní - přednáška nebo poster

Page from-to: nestránkováno

Titles:

Language	Name	Abstract	Keywords
eng	Preparing of potencional proteasome and kinasis inhibitors based on salicylamides with acrylamide moiety	Proteasome inhibitors (PI) are substances that stop proteosynthesis, which occurs in a part of cell called proteasome. Proteasome is protein complex in which occurs intracellular degradation of proteins with an error in their structure. In contrast, protein kinase inhibitors inhibit the binding of the phosphate group to amino acid residues in proteins. These substances are used to treat various type of a cancer. The various peptidic and non-peptidic inhibitors have been structurally designed to best interact with the catalytic units in the proteasome nucleus. Our research group focused on pseudo-peptide inhibitors, specifically salicylamide derivatives. PI is consisted from peptidic and reactive pharmacophore moiety. One of this pharmacophore is acrylamide pharmacophore on which is our research focused and which interact with cysteine via Michael addition. In this case the reactive center suitable for Michael addition with cysteine is SH group.	Proteasome Inhibitors; Salicylamides; Acrylamide;

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