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Sinteza in vrednotenje zaviralcev indolamin 2,3-dioksigenaze 1 z izoksazolo[5,4-d]pirimidin-4(5H)-onskim osnovnim skeletom = Synthesis and evaluation of indoleamine 2,3-dioxygenase 1 inhibitors with isoxazolo[5,4-d]pyrimidin-4(5H)-one scaffold : Uniform Master's Study Programme PharmacyPoljanšek Bitenc, EvaIndolamin 2,3-dioksigenaza 1 (IDO1) je citoplazemski encim, ki igra pomembno vlogo pri rakotvornosti in njenem napredovanju. Sodeluje v katabolizmu esencialne aminokisline triptofan. Imunomodulatorno ... delovanje IDO1 je predvsem posledica pomanjkanja triptofana v tumorskem mikrookolju in povečanja presnovkov, ki izvirajo iz triptofana. Aktivirani encim IDO1 namreč zniža raven triptofana v okolici tumorja, zmanjšanje pa povzroči imunosupresivne učinke. Zaviralci IDO1 predstavljajo enega izmed potencialnih terapevtskih pristopov za zaviranje rasti tumorja. V sklopu magistrske naloge smo sintetizirali enajst končnih spojin, čistost in strukturo vmesnih ter končnih spojin smo preverili z različnimi analitskimi tehnikami. Pri načrtovanju spojin smo izhajali iz strukture že znanega zaviralca IDO1, 3-(4-fluorofenil)izoksazolo[5,4-d]pirimidin-4(5H)-ona, ki je bil odkrit z virtualnim rešetanjem. Z biokemijskim testiranjem smo na osnovi merjenja fluorescence ovrednotili zaviralno delovanje vseh končnih spojin, aktivnim spojinam z močnejšim zaviralnim delovanjem pa določili in izračunali še vrednost IC50. Glede na dobljene rezultate smo ugotovili, da najmočnejše zaviralno delovanje kaže spojina N-(4-aminofenil)-2-(3-(4-fluorofenil)-4-oksoizoksazolo[5,4-d]pirimidin-5(4H)-il)acetamid (21) z IC50 = 26,3 %M. Z namenom napovedi potencialnih interakcij z vezavnim mestom IDO1 smo izvedli še sidranje spojine 21 v aktivno mesto encima. Izmed vseh sintetiziranih končnih spojin ima pet spojin pri koncentraciji 100 %M rezidualno aktivnost nižjo od 60 %, zato smo jim lahko določili in izračunali še vrednost IC50. Od teh tri spojine (15, 19 in 21) močneje zavirajo encim, dve spojini (20 in 24) pa šibkeje. Zaključimo lahko, da spojina 21 predstavlja pomembno izhodišče za nadaljnje raziskovanje zaviralcev IDO1, kot eno izmed obetavnih terapevtskih možnosti za zaviranje rasti tumorja.Type of material - master's thesis ; adult, seriousPublication and manufacture - Ljubljana : [E. Poljanšek Bitenc], 2020Language - slovenianCOBISS.SI-ID - 30849283
Author
Poljanšek Bitenc, Eva
Other authors
Sova, Matej, 1979-
Topics
Imunomodulatorji |
Tumorji |
indolamin 2, 3-dioksigenaza |
imunomodulacija |
terapevtske možnosti |
zaviralci |
sinteza spojin
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Library/institution |
City | Acronym | For loan | Other holdings |
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Faculty of Pharmacy, Ljubljana | Ljubljana | FFALJ |
reading room 1 cop.
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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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Poljanšek Bitenc, Eva | ![]() |
Sova, Matej, 1979- | 25490 |
Source: Personal bibliographies
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