Purīnerģiskā divpadsmitā receptora 181. pozīcijas randomizēto variantu funkcionālā aktivitātes izpēte

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Purīnerģiskā divpadsmitā receptora 181. pozīcijas randomizēto variantu funkcionālā aktivitātes izpēte

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Kopsavilkums Darba gaitā tika izvērtēta P2Y12R 181. pozīcijā esošās glutamīnskābes loma receptora mijiedarbībā ar agonistu ADP un antagonistu OSI-10110. P2Y12R varianti ar mutaģenizētu 181. pozīciju tika ekspresēti S. cerevisiae šūnās un aktivēti ar ADP, OSI-10110 un AR-C66096. Tika konstatēts, ka Glu181 aizvietošana ar pēc fizikāli ķīmiskās dabas līdzīgām aminoskābēm, var dažādi ietekmēt receptora un liganda mijiedarbību. Ar QSAR datu analīzi, tika konstatēts, ka P2Y12R Glu181 mijiedarbībā ar ADP un OSI-10110, būtiskas ir aminoskābes hidrofīlās un elektriskās īpašības. Glu181 mijiedarbību ar OSI-10110 nedaudz arī ietekmē aminoskābes fleksibilitāte. OSI-10110 uzrāda zemāku ietekmi uz ADP izraisīto P2Y12R funkcionālo aktivitāti, nekā AR-C66096. Atslēgvārdi: P2Y12R, Saccharomyces cerevisiae, funkcionālā analīze, QSAR.

year	journal	country	edition	language
2011-01-01

https://dspace.lu.lv/dspace/handle/7/20937

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