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Project information
Calixarenes based glycodrugs - design, structure, antitumor and antiviral activity

Project Identification
IAA400200503
Project Period
1/2005 - 12/2009
Investor / Pogramme / Project type
Academy of Sciences of the Czech Republic
  • Grants of distinctly investigative character focused on the sphere of research pursued at present particularly in the ASCR
MU Faculty or unit
Faculty of Science
  • prof. RNDr. Jaroslav Koča, DrSc.
  • prof. Ing. Vladimír Křen, DrSc.
  • prof. Ing. Ivan Stibor, CSc.
Keywords
saccharides; glycosaminoacids, saccharide recognition, glycomimetics, calix[n]arenes

New water soluble ligands will be designed. The calix[n]arene scaffold in different (semi)rigid conformations, and saccharides, glycopeptides, glykosaminoacids and glycodendrons will be used as biomolecules. Computation methods (mol. dynamics) will support rational design. Synthetic methods, supramolecular chemistry - (weak interactions in complexes) and enzymatic synthesis will be used. Ligands will be tested as follows: 1. Qualitative and quantitative study of interactions of ligands (in water) attached to scaffold as a function of their spatial orientation(s). No data of this kind are available. 2. Complexation towards external guests; co-operative binding by several units with respect to their spatial orientation. Complexes of carboxylates (sialic acids) and nitric oxides donors (carbohydrate-based) will be studied. 3. Biological activity of all compounds and complexes will be screened using e.g.: activation protein NKR-P1 of the NK-cells; pertussis toxin; N-acetylhexosaminidases.

Publications

Total number of publications: 5

2008

2007

2006

2005

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