Ungayenza kanjani i-RGD cyclopeptide

I-Integrin, noma i-integrin, iyisamukeli se-heterodimer transmembrane glycoprotein esilamula ukunamathela kwamangqamuzana ezilwane nokubonisa izimpawu.Yakhiwaα futhiβ amayunithi amancane.Ihilelekile ekuthuthukiseni izenzo ezihlukahlukene zamaselula okuhlanganisa ukufuduka kwamangqamuzana, ukungena kwamaseli, ukusayina kwamaseli kanye ne-intercellular, ukunamathela kwamaseli, nezinqubo ze-angiogenesis.I-Integrinαvβ3 manje isihlolisiswa kabanzi.Ukubonakala kwe-interinαvβI-3 ihlobene eduze nokufuduka kwesimila, i-angiogenesis, ukuvuvukala kanye ne-osteoporosis.I-Integrin ivezwa kakhulu kuzo zonke izicubu zesimila kanye nolwelwesi lwamaseli we-endothelial we-neovascularization.Ukubukeka kwe-integrin kuhlobene eduze nokufuduka kwesimila kanye ne-angiogenesis.Eminyakeni yamuva nje, ucwaningo lwesayensi lubonise ukuthi kukhona ama-integrin angu-11 angabopha ngokuqondile ku-RGD peptide, okungama-peptide aphikisayo ama-interin receptors.

I-peptide ye-RGD ihlukaniswa yaba i-peptide ye-RGD eqondile kanye ne-RGD cyclic peptide.Uma kuqhathaniswa ne-peptide ye-RGD ewumugqa, i-RGD cyclic peptide inokuhambisana okuqinile kwesamukeli kanye nokucaciswa kwesamukeli.Okulandelayo yizinhlobo ezijwayelekile nezindlela zokwenziwa kwe-RGD cyclic peptide.

Izinhlobo ezijwayelekile ze-RGD cyclic peptides:

1. Ama-peptide e-cyclic aqukethe ukulandelana kwe-RGD okwakhiwa ngamabhondi e-disulfide

2. Ama-peptide e-cyclic aqukethe ukulandelana kwe-RGD okwakhiwa ngamabhondi e-amide

Ukuhlanganiswa kwe-RGD cyclic peptide:

Imodeli yokusetshenziswa ihlobene nenqubo ye-RGD cyclic peptide synthesis emkhakheni wobuchwepheshe besigaba esiqinile se-polypeptide synthesis.Indlela entsha ukukhetha i-resin engu-2-chloro-triphenylmethyl chloride njengesithwali esidingekayo, okokuqala xhuma iqembu lokuqala le-carboxyl eseceleni neqembu eliyisivikelo elikhethekile le-D aspartic acid amino acid, bese uxhuma i-peptide yomugqa ye-RGD yokulandelana kwe-peptide ku-resin. , kanye ne-amino acid yokugcina yokususa iqembu elivikelayo le-FOC ngaphandle kwe-piperidine.I-catalyst ecacisiwe yengezwe ukuze kukhishwe iqembu elivikelayo le-carboxyl ye-side chain ye-aspartic acid yokuqala ye-D ngqo kusuka ku-resin, kulandelwa ukufakwa kwe-piperidine ukuze kukhishwe iqembu elivikelayo le-amino i-FOC ye-amino acid yokugcina, kulandelwa ukwengezwa kwe-ejenti ebophayo. ukukhipha amanzi emanzini kanye nokufingqa iqembu le-carboxyl neqembu le-amino elivezwe ekhanda nasekupheleni kwe-peptide eqondile kusuka ku-resin ngendlela ye-amide bond ukukhiqiza i-cyclic peptide.Ekugcineni, i-peptide ye-cyclic isikwa ngokuqondile ku-resin ngesisombululo sokusika.