Inotora basa rakakosha mumatanho ehupenyu, phosphorylating Tyrr, Ser, Thr, iri pamapeptides.Iyo phosphorylated amino acid inowanzoshandiswa mukugadzira phosphoric acid peptide, parizvino inoshandiswa mune imwechete phenyl phosphorylated amino acids.HBTU/phosphorylated amino acids inowanzo shandiswa kubatanidza iyo phosphorylated amino acids HOBt/DIEA nzira, asi iyo phosphoric acid peptide iri kusarudza nzira iyi kukanganisa, kunyanya mune inogadzirwa yakareba peptide peptide kana amino acid phosphate, kubatanidza kushanda kwakaderera, kwakaderera. kuchena kwechigadzirwa chekupedzisira.Kune iyi phosphopeptide, takafunga nzira yekusarudza post-phosphorylation.Iyo chizvarwa maitiro ndeye kusarudzwa kubviswa kweamino acid parutivi-cheni ekudzivirira mapoka anoda kunyorwa mushure mepeptide synthesis.Kune Tyr, Thr inogona kuita zvakananga ichishandisa amino acids ine isina kudzivirirwa mativi cheni.-Ser (trt), yakawanda yakabviswa pa1% TFA / DCM nharaunda.
Phosphorylation, ine double benzene phosphite phosphoramide uye ina nitrogen inogadzirwa uye phosphoramide tetrazolium inoshanda yepakati, yakabatana nehydroxy, ipapo pasi peasidhi peroxide oxidation phosphoryl kuumbwa, kuita kwakazara.
Parizvino, iyo peptide phosphorylated gadziriso nzira kune maviri makuru marudzi:
(1) kusuma kwakananga kweane mwero yakavimbiswa phosphorylated amino acids mune polypeptide kutevedzana;
(2) mushure meiyo resin yakagadzirwa pakutevedzana kwepeptide, kuSer, Tyr, kana Thr phosphorylation yeside chain hydroxyl.
1) ichave ine mwero vimbiso phosphorylated amino acids inosuma zvakananga peptide kutevedzana:
Kureva kuti, amino acids inoda kuve phosphorylated ichave phosphorylated uye yakachengetedzwa zvakafanira kumberi uchishandisa (Thr,Ser kana Tyr), uye ipapo phosphorylation inozodzikiswa kusvika kunzvimbo yekusarudza yepolypeptide index zvichibva pane yakajairwa SPPS chizvarwa maitiro. .Iyi nzira iri nyore kushanda, yave nzira huru yemabhizinesi epeptide phosphorylated shanduko.
2) mushure meiyo resin yagadzirwa pakutevedzana kwepeptide, kune Ser hydroxy phosphorylation, Tyr, kana Thr parutivi cheni:
Phosphorylation kushongedzwa uchishandisa phosphorylation yekamwe contraction munzira yepolypeptide, nekuda kweiyo steric chipinganidzo inogadzirwa nemapoka makuru mukushongedza kwecheni yepadivi, zvinonetsa kuti phosphorylation yeamino acids iderere neketani yepeptide.Mune ramangwana, kuiswa kwemaamino acids kuchava kwakaoma, kunyanya mukushongedza kune nzvimbo dzakawanda dzephosphorylation, chizvarwa chichava chakaoma zvikuru, chimiro chekupedzisira chechigadzirwa chakaoma, chakaoma kuparadzanisa, uye goho rakaderera zvakanyanya.
Naizvozvo, kana nzvimbo dzakawanda muketani yepeptide dzave phosphorylated, munhu anogona kusarudza kugadzira peptide kutevedzana pane resin uye obva aita phosphorylate nedivi reketani hydroxyl boka reSer, Tyr, kana Thr: chizvarwa chayo chinonyanya kusanganisa kubviswa kweiyo side chain protective boka rinoda kucherechedzwa kweamino acids mushure mekugadzirwa kwepeptide.Kune Tyr, Thr inogona kushandisa zvakananga amino acid parutivi maketani haana kuchengetedzwa mukupindura.
Side cheni yekudzivirira base 1% TFA/DCM nharaunda inogona kubviswa zvakanyanya.Kana iyi nzira yasarudzwa, phosphoramidite tetrazolium inoshanda yepakati inogona kugadzirwa uchishandisa dibenzyl phosphoramidite uye tetrazolium, yakabatana neboka rehydroxyl, yobva yaiswa oxidized kuumba boka rephosphoryl munzvimbo yeperoxyacid kuti ipedze kuita.
Nguva yekutumira: Sep-08-2023