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Novi derivati cimetne kisline kot inhibitorji 17ß-hidroksisteroid-dehidrogenaz = New cinnamic acid derivatives as inhibitors of 17ß-hydroxysteroid dehidrogenases : diplomsko deloStarčević, Štefan17 -hidroksisteroid-dehidrogenaze (17 -HSD) katalizirajo zadnjo stopnjo biosinteze spolnih hormonov. Ker so lahko vpletene v razvoj stevilnih hormonsko odvisnih bolezni, predstavljajo zanimivo tarèno ... mesto za uravnavanjekoncentracije estrogenov in androgenov v organizmu. Na osnovi estrov cimetne kisline, ki so se v preteklih raziskavah izkazali kot dobri inhibitorji encima 17Ž-HSD iz glive Cochliobolus lunatus (17Ž-HSDcl), smo v okviru diplomske naloge sintetizirali serijo novih spojin in ugotavljali njihovo delovanje. Inhibitorno aktivnost sintetiziranih spojin smo testirali na rekombinantni 17Ž-HSDcl, modelnem encimu proteinske naddruzine kratkoveriznih dehidrogenazžreduktaz. Encim smo izolirali iz bakterije Escherichia coli z vstavljenim plazmidom pGEX-17 -hsdcl, ki nosi genski zapis za 17 -HSDcl. Rezultati meritev so pokazali, da je za inhibitorno delovanje sintetiziranih spojin nujno potrebna esterska oz. amidna skupina, pri èemer soestri cimetne kisline boljsi inhibitorji modelne 17 -HSD kot amidi, ter da imajo derivati 3,4,5-trimetoksicimetne kisline slabso inhibitorno aktivnost kot derivati nesubstituirane cimetne kisline. Z optimizacijo sintetiziranih spojin bi lahko v prihodnosti razvili bolj uèinkovite inhibitorje èloveskih 17-hidroksisteroid-dehidrogenaz, ki bi jih uporabljali za prepreèevanje in zdravljenje razliènih hormonsko odvisnih bolezni, kot so nekatere oblike raka,osteoporoza, Alzheimerjeva bolezen in druga patoloska stanja.Type of material - undergraduate thesisPublication and manufacture - Ljubljana : [Starčević, Š.], 2006Language - slovenianCOBISS.SI-ID - 1888625
Author
Starčević, Štefan
Other authors
Gobec, Stanislav, 1970- |
Lanišnik-Rižner, Tea
Topics
hidroksisteroid-dehidrogenaze |
fitoestrogeni |
inhibitorji |
spolni hormoni |
metode |
sinteza derivatov cimetne kisline
Library | Call number – location, accession no. ... | Copy status |
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Faculty of Pharmacy, Lj. | Knjižnica dp 542 STARČEVIĆ ŠTEFAN Novi derivati IN: 0008806 |
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DRS, in which the journal is indexed
Database name | Field | Year |
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Links to authors' personal bibliographies | Links to information on researchers in the SICRIS system |
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Starčević, Štefan | 28776 |
Gobec, Stanislav, 1970- | 15284 |
Lanišnik-Rižner, Tea | 11699 |
Source: Personal bibliographies
and: SICRIS
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