"2010-06-08+02:00"^^ . . . . "2009-12-31+01:00"^^ . "L\u00E9\u010Diva na b\u00E1zi sacharid\u016F a calixaren\u016F - design, struktura, protin\u00E1dorov\u00E1 a protivirov\u00E1 aktivita" . . "3"^^ . . "0"^^ . "IAA400200503" . . "saccharides" . "Navrhujeme strukturu nov\u00FDch, ve vod\u011B rozpustn\u00FDch ligand\u016F s biomolekulami, um\u00EDst\u011Bn\u00FDmi na molekul\u00E1rn\u00EDm le\u0161en\u00ED v \u0159iditeln\u00E9 prostorov\u00E9 orientaci. Jako molekul\u00E1rn\u00ED le\u0161en\u00ED bude vyu\u017Eit kalix[4]aren v jedn\u00E9 ze sv\u00FDch zn\u00E1m\u00FDch koformac\u00ED. Biomolekuly budou vybr\u00E1ny ze skupiny sacharid\u016F, glykopeptid\u016F a glykosaminokyselin a glykodendron\u016F. V\u00FDpo\u010Detn\u00ED metody zalo\u017Een\u00E9 na kvantov\u00E9 chemii a molekul\u00E1rn\u00ED dynamice budou vyv\u00EDjeny a vyu\u017E\u00EDv\u00E1ny k racion\u00E1ln\u00EDmu n\u00E1vrhu struktury shora charakterizovan\u00FDch ligand\u016F. Krom\u011B organick\u00E9 synt\u00E9zy bude vyu\u017Eito enzymov\u00FDch reakc\u00ED pro p\u0159ipojen\u00ED biomolekul ke kalixarenov\u00E9mu skeletu. D\u00E1le bude provedeno studium komplexa\u010Dn\u00EDch schopnost\u00ED z\u00EDskan\u00FDch ligand\u016F. Jeho vyu\u017Eit\u00ED povede jednak k systematick\u00E9mu studiu vzajemn\u00FDch interakc\u00ED pou\u017Eit\u00FDch biomolekul, jednak k tvorb\u011B (nekovalentn\u00EDch) komplex\u016F s jin\u00FDmi, biologicky zaj\u00EDmav\u00FDmi biomolekulami (nap\u0159. NO, kys. sialov\u00E1). Jako biologick\u00E9 syst\u00E9my pro testov\u00E1n\u00ED budou vyu\u017Eity aktiva\u010Dn\u00ED receptory NK bun\u011Bk, b-N-acetylhexosaminidasa a pertussis toxin." . "saccharides; glykosaminoacids; saccharide recognition; glycomimetics; calix[n]arenes"@en . "2005-01-01+01:00"^^ . "1"^^ . . . . "2009-04-28+02:00"^^ . . "Byly p\u0159ipraveny a otestov\u00E1ny zcela nov\u00E9 imunostimul\u00E1tory na b\u00E1zi thiacalixaren\u016F a cyklopeptidick\u00FDch glykoneokonjug\u00E1t\u016F pro aktivaci leukocyt\u016F (NK) s velmi vysokou aktivitou, bez negativn\u00EDch vedlej\u0161\u00EDch \u00FA\u010Dink\u016F, vhodn\u00E9 pro hum\u00E1nn\u00ED protin\u00E1dorovou terapii."@cs . . " glycomimetics" . . . . " saccharide recognition" . . "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."@en . "Entirely new immunostimulants based on thiacalixarenes and cyclopeptidic neoglycoconjugates were prepared and tested for NK cell (leukocyte) activation. They are void of negative side effect and are well applicable in the terapy of human cancers."@en . . "21"^^ . " glykosaminoacids" . "21"^^ . . "Calixarene-based multivalent glyco-druge - design, structure, biological (antitumor and antiviral) activity"@en . . . . "http://www.isvav.cz/projectDetail.do?rowId=IAA400200503"^^ .