. "GA203/04/0298" . "Z\u00E1m\u011Brem projektu je p\u0159\u00EDprava, identifikace a biologick\u00E9 testov\u00E1n\u00ED stereochemicky p\u0159esn\u011B definovan\u00FDch fytoekdysteroid\u016F a jejich analog\u016F pro \u00FApln\u00E9 zmapov\u00E1n\u00ED ekdysteroidn\u00EDho receptoru reguluj\u00EDc\u00EDho hmyz\u00ED metamorf\u00F3zu . P\u016Fjde o polyhydroxylovan\u00E9 steroidy rostlinn\u00E9ho p\u016Fvodu a jejich chemicky transformovan\u00E9 deriv\u00E1ty, jako\u017E i o nesteroidn\u00ED bio-analogy fenylpropanoidn\u00EDho typu, kter\u00E9 jsou schopn\u00E9 substituovat \u00FA\u010Dinky metamorf\u00F3zn\u00EDho hormonu ekdysonu, nebo interferovat s\u00A0jeho \u00FA\u010Dinky p\u0159\u00EDmo na vazebn\u00EDm m\u00EDst\u011B receptoru. Z test\u016F budou odvozeny kvantitativn\u00ED vztahy mezi strukturou a biologick\u00FDm \u00FA\u010Dinkem, kde vazebn\u00ED afinita ligandu k\u00A0receptoru vyjad\u0159uje charakter a potenci \u00FA\u010Dinku testovan\u00E9 l\u00E1tky. Aplikac\u00ED metod CoMFA a z\u00A0n\u00ED odvozen\u00E9 komplexn\u00ED hypot\u00E9zy farmakoforu ligandu budou specifikov\u00E1ny molekul\u00E1rn\u00ED determinanty ur\u010Duj\u00EDc\u00ED charakter ligandu a v\u00FDpo\u010Dtem budou ur\u010Deny ty strukturn\u00ED \u010D\u00E1sti nebo funk\u010Dn\u00ED skupiny, kam lze beze ztr\u00E1ty aktivity zav\u00E9st fotosenzitivn\u00ED nebo jinak zna\u010Den\u00E9 substituenty pro sledov\u00E1n\u00ED" . . "2007-10-16+02:00"^^ . . . . . "0"^^ . . . "The project was focused to identify biologically active plant substances and their chemically or photochemically transformed analogues that\u00A0 can interfere with the insect moulting hormone ecdysone. We investigated their agonistic or antagonistic effect ("@en . . . . "Preparation and structural identification of steroid and non-steroid ligands efficient in interaction with the ecdysteroid receptor"@en . "P\u0159\u00EDprava a strukturn\u00ED identifikace steroidn\u00EDch a nesteroidn\u00EDch ligand\u016F schopn\u00FDch interakce s ekdysteroidn\u00EDm receptorem" . "1"^^ . . . . . "0"^^ . "7"^^ . . . . "7"^^ . "http://www.isvav.cz/projectDetail.do?rowId=GA203/04/0298"^^ . . . "The project objectives consist in preparation, identification and biological evaluation of stereochemically fully defined phytoecdysteroid analogues for a final ecdysteroid receptor mapping, responsible for the insect metamorphosis regulation. It concerns polyhydroxylated steroids of plant origin and their chemically trans-formed derivatives, as well as non-steroid (phenylpropanoid) bio-analogues efficient in substituting the moulting hormone ecdysone action, or interfering with its effect directly at the binding site of the ecdysone receptor. 3D-QSAR evaluation will be done, based on results obtained from a well-established bioassay, in which the potency reflects the affinity of the test compound for the ligand-binding site of the receptor. Application of the CoMFA calculations expressed in a complex pharmacophore hypothesis will be used to specify structure determinants reflecting agonistic or antagonistic character of the ligand. Photosensitive substituents will be introduced"@en . . "Neuvedeno."@en . "T\u011B\u017Ei\u0161t\u011Bm projektu je p\u0159\u00EDprava a identifikace bioaktivn\u00EDch rostlinn\u00FDch l\u00E1tek a jejich chemicky a fotochemicky transformovan\u00FDch analog\u016F, interferuj\u00EDc\u00EDc\u00EDch s \u00FA\u010Dinky hmyz\u00EDho metamorfozn\u00EDho hormonu ekdysonu. Zkoum\u00E1n je jejich agonistick\u00FD nebo antagonistick\u00FD ("@cs .