Glycosyltranferases are enzymes responsible for the formation of the glycosidic bond in living system. They transfer the sugar unit from a nucleoside diphosphate sugar (NDP-sugar e.g. UDP-glucose) to a specific hydroxyl- or amino- group of the acceptor substrate which is usually other sugar but nucleic acids, proteins, lipids and other small molecules are also encountered [1]. Modification of many structures through addition of sugars unit can have a significant impact on their physical, chemical or biological properties. Current research confirms that cell surface glycoconjugates have pivotal functions in various cellular recognition systems involving cell differentiation, development, inflammation, immune response, bacterial/viral infections, and many other intercellular communications [2]. In recent years increased attention toward GTs inhibitors has emerged due to key role of these enzymes in biological synthesis of glycoconjugates and polysaccharides. Development of new selective inhibitors is of great importance in dealing with bacterial [3] and fungal diseases [4].  Analogues of NDP-sugar can have an important role as new drug candidates. Our recent research led to analogues of GTs natural substrates in which diphosphate moiety was replaced with amide unit connecting carbohydrate to cyclic or acyclic nucleoside part. Alternative route includes 1,2,3-triazole linkage installed by dipolar cycloaddition.

Research studies part-financed by the European Union within the European Regional Development Fund (POIG.01.01.02-14-102/09). Roman Komor received a scholarship under the project DoktoRIS - Scholarship Program for Innovative Silesia.

References:

[1] L. L. Lairson, B. Henrissat, G. J. Davies, S. G. Withers, Annu. Rev. Biochem., 2008, 77, 521-555.

[2] K. Hosoguchi, T. Maeda, J. Furukawa, Y. Shinohara, H. Hinou, M. Sekiguchi, H. Togame, H. Takemoto, H. Kondo, S.-I. Nishimura, J. Med. Chem., 2010, 53, 5607-5619.

[3] S. Berg, D. Kaur, M. Jackson, P. J. Brennan, Glycobiology,  2007, 17, 35-56.

[4] J. B. Behr, A. Gainvors-Claisse, A. Belarbi, Nat. Prod. Res., 2007, 21, 76-82.

• Legal notice:
  

  Copyright (c) Pielaszek Research, all rights reserved.
  The above materials, including auxiliary resources, are subject to Publisher's copyright and the Author(s) intellectual rights. Without limiting Author(s) rights under respective Copyright Transfer Agreement, no part of the above documents may be reproduced without the express written permission of Pielaszek Research, the Publisher. Express permission from the Author(s) is required to use the above materials for academic purposes, such as lectures or scientific presentations.
  In every case, proper references including Author(s) name(s) and URL of this webpage: https://science24.com/paper/31045 must be provided.

1. Synthesis and potential spectrum of biological activities of glycoconjugates derivatives of hydroxy-2-methylquinoline carboxylic acids
2. Fucosyl derivatives in the synthesis of uridine glycoconjugates - potential glycosyltransferase inhibitors
3. Synthesis and biological activity of synthetic β-D-glucose and β-D-galactose conjugates with various acyclic nucleosides
4. Synthesis of glycosyltransferases natural substrate analogues from 1,6-anhydrosugars and acyclic uridine derivatives
5. Evaluation of cytoxicity of glycosyl uridine derivatives
6. Application of different α-1-thioglycosides preparation methods in synthesis of 5-nitro-pyridyl 1-thioglycosides - substrates in construction of conjugates with uridine moiety
7. The biological activity of sugar derivatives based on quinoline scaffold
8. The role of a sugar moiety in new genitein derivatives affecting proliferation and apoptosis of cancer cells
9. Synthesis of galactothiophosphoesters of uridine and preliminary tests to evaluate their activity against selected glycosyltransferases
10. The immunochemical studies of the glycinated glycoconjugates based on synthetic thioglycosides as mimic factors of bacterial endotoxins using in the polysaccharide vaccines preparation
11. (5-Nitro-2-pyridyl) 1-thioglycosides: application in synthesis of analogues of glycosyltransferases natural substrates
12. Glycoconjugates, products of uridine derivatives phosphitylation and oxidation as glycosyltransferases potential inhibitors
13. Uridine derivatives of 1-thioglycosides as analogs of glycosyltransferases natural substrates
14. Uridine derivatives of heteroaryl 1-thioglycosides: synthesis and biological activity against CSFV glycoproteins
15. 1-THIOSUGARS: SYNTHESIS AND BIOLOGICAL ACTIVITY AGAINST CSFV GLYCOPROTEINS.