Nigute ushobora guhuza RGD cyclopeptide

Integrin, cyangwa integrin, ni heterodimer transmembrane glycoprotein reseptor ihuza ingirabuzimafatizo hamwe no gutangaza.Igizwe naα naβ subunits.Ifite uruhare mugutezimbere ibikorwa bitandukanye bya selile harimo kwimuka kwakagari, kwinjiza selile, selile na selile intercellular signal, adhesion selile, hamwe na angiogenez.Integrinαvβ3 ubu irashakishwa cyane.Kugaragara kwa integrinαvβ3 bifitanye isano rya bugufi no kwimuka kw'ibibyimba, angiogenezi, gutwika na osteoporose.Integrin igaragara cyane mubice byose byibyimba hamwe na selile endothelial selile ya neovascularization.Kugaragara kwa integrin bifitanye isano rya hafi no kwimuka kw'ibibyimba na angiogenez.Mu myaka yashize, ubushakashatsi bwa siyansi bwerekanye ko hari 11 integin zishobora guhuza cyane na peptide ya RGD, ari peptide ya antagonistique ya reseptor.

Peptide ya RGD ishyizwe mubice bya RGD peptide na peptide ya RGD.Ugereranije n'umurongo wa RGD peptide, RGD cyclic peptide ifite imbaraga zo guhuza reseptor hamwe na reseptor yihariye.Ibikurikira nuburyo busanzwe hamwe na synthesis uburyo bwa RGD cyclic peptide.

Ubwoko busanzwe bwa peptide ya RGD:

1. Peptide ya cycle irimo urutonde rwa RGD ikorwa na disulfide

2. Peptide ya cycle irimo urutonde rwa RGD rwakozwe na amide bonds

Synthesis ya RGD cyclic peptide:

Moderi yingirakamaro ifitanye isano na RGD cyclic peptide synthesis murwego rwubuhanga bukomeye bwa polypeptide synthesis.Uburyo bushya ni uguhitamo 2-chloro-triphenylmethyl chloride resin nkibisabwa mbere, banza uhuze itsinda rya mbere ryumunyururu wa carboxyl hamwe nitsinda ryihariye ririnda aside aside aside amine, hanyuma uhuze peptide yumurongo wa peptide ya RGD ikurikirana na resin. , na aside amine yanyuma kugirango ikureho itsinda ririnda FMOC idafite piperidine.Cataliseri yasobanuwe yongeweho kugirango ikureho urunigi rwuruhande rwa carboxyl irinda itsinda rya mbere ya D aspartic acide ya resin itaziguye, hanyuma hakurikiraho kongeramo piperidine kugirango ikureho amatsinda arinda amine FMOC ya aside amine yanyuma, hakurikiraho kongerwamo agent kubura umwuma no guhuriza hamwe itsinda rya carboxyl hamwe nitsinda rya amino ryerekanwe kumutwe no kumpera ya peptide y'umurongo uva mubisigarira muburyo bwa amide kugirango bibyare peptide cyclic.Hanyuma, peptide ya cyclicale yaciwe biturutse kumurongo hamwe no gukata.