Gusobanukirwa peptide ya fosifori

Ifite uruhare runini mubuzima, fosifora Tyrr, Ser, Thr, iherereye kuri peptide.Acide ya fosifora ikunze gukoreshwa mugukora peptide ya fosifori, kuri ubu ikoreshwa muri acide imwe ya fenil fosifori.HBTU / fosifori ya aminide acide ikoreshwa muguhuza uburyo bwa fosifori ya amino acide ya HOBt / DIEA, ariko peptide ya fosifori aside peptide ihitamo ubu buryo bufite inenge, cyane cyane mubyakozwe na peptide peptide ndende cyangwa fosifate ya amino aside, ihuza imikorere ni mike, hasi ubuziranenge bwibicuruzwa byanyuma.Kuri iyi fosifopi, twasuzumye uburyo bwatoranijwe nyuma ya fosifora.Igisekuru cyibikorwa ni ugukuraho gutoranya aminide acide kuruhande-urunigi rukingira amatsinda akeneye gushyirwaho ikimenyetso nyuma ya synthesis ya peptide.Kuri Tyr, Thr irashobora kwitwara neza ukoresheje aside amine hamwe n'iminyururu idakingiye.-Ser (trt), yakuwe muburyo bwa 1% TFA / DCM ibidukikije.

Fosifora, hamwe na fosifora ya benzene ebyiri na fosifori na azote enye zirabyara kandi fosifora tetrazolium ikora hagati, ihuza hydroxy, hanyuma munsi ya acide peroxide oxyde ya fosifori, reaction yuzuye.

Kugeza ubu, uburyo bwo guhindura peptide fosifora hari ubwoko bubiri bwingenzi:

(1) kwinjiza mu buryo butaziguye fosifori ya amine acide yemewe mu buryo bwa polypeptide;

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1) bizagabanya garanti ya fosifori ya amino acide itangiza peptide ikurikiranye:

Nukuvuga ko aside amine ikeneye kuba fosifora izaterwa na fosifori kandi ikarindwa neza hakiri kare ukoresheje (Thr, Ser cyangwa Tyr), hanyuma fosifora ikagabanuka kugeza aho ihitamo indangagaciro ya polypeptide ishingiye kubikorwa bisanzwe bya SPPS. .Ubu buryo bworoshye gukora, bwabaye uburyo nyamukuru bwibikorwa bya peptide bihindura fosifora.

2) nyuma ya resin yabyaye kuri peptide ikurikirana, kuri Ser hydroxy fosifora, Tyr, cyangwa Thr kuruhande:

Imitako ya fosifora ikoresheje fosifora yo kugabanuka kamwe muburyo bwa polypeptide, kubera inzitizi zidasanzwe zatewe nitsinda rinini mugushushanya urunigi, biragoye ko fosifora ya acide amine igabanuka hamwe numuyoboro wa peptide.Mu bihe biri imbere, kwinjiza aminide acide bizagorana cyane cyane mubushushanyo burimo ibibanza byinshi bya fosifora, ibisekuruza bizagorana cyane, ibicuruzwa byanyuma biragoye, bigoye gutandukana, kandi umusaruro ni muke cyane.

Kubwibyo, iyo imbuga nyinshi mumurongo wa peptide zifitwe na fosifori, umuntu arashobora guhitamo kubyara peptide ikurikirana kuri resin hanyuma fosifora ikayinyuza kumurongo wuruhande rwa hydroxyl ya Ser, Tyr, cyangwa Thr: ibisekuruza byayo ahanini bikubiyemo kuvanaho guhitamo kwa itsinda ririnda uruhande rusaba kumenyekanisha aside amine nyuma ya peptide synthesis.Kuri Tyr, Thr irashobora gukoresha mu buryo butaziguye iminyururu ya aminide acide ntabwo irinzwe mugusubiza.

Kurinda urunigi kuruhande 1% TFA / DCM ibidukikije birashobora gukurwaho.Iyo ubu buryo bwatoranijwe, fosiforamide ya tetrazolium ikora hagati irashobora kubyara hakoreshejwe dibenzyl phosphoramidite na tetrazolium, ihujwe nitsinda rya hydroxyl, hanyuma igahumeka kugirango igire itsinda rya fosifori mubidukikije bya peroxyacide kugirango irangize reaction.