I-Integrin, okanye i-integrin, i-heterodimer transmembrane glycoprotein receptor edibanisa ukunamathela kweeseli zezilwanyana kunye nokubonakaliswa.Yenziwe ngeα kwayeβ iiyunithi ezincinci.Ibandakanyeka ekuphuculeni izenzo ezahlukeneyo zeselula ezibandakanya ukufuduka kweeseli, ukungena kweeseli, i-cell kunye ne-intercellular signaling, i-cell adhesion, kunye neenkqubo ze-angiogenesis.Integrinαvβ3 ngoku iphononongwa ngokubanzi.Imbonakalo ye integrinαvβI-3 inxulumene ngokusondeleyo nokufuduka kwe-tumor, i-angiogenesis, ukuvuvukala kunye ne-osteoporosis.I-Integrin ibonakaliswe kakhulu kuzo zonke izicubu ze-tumor kunye ne-endothelial cell membranes ye-neovascularization.Ukubonakala kwe-integrin kuhambelana ngokusondeleyo nokufuduka kwe-tumor kunye ne-angiogenesis.Kwiminyaka yakutshanje, uphando lwezenzululwazi lubonise ukuba kukho ii-integrin ezili-11 ezinokubophelela ngokukodwa kwi-RGD peptide, eziyi-peptides ezichasayo ze-integrin receptors.
I-peptide ye-RGD ihlelwa ngokwemigca ye-peptide ye-RGD kunye ne-RGD ye-cyclic peptide.Xa kuthelekiswa ne-peptide ye-RGD ehambelanayo, i-RGD cyclic peptide inokuhambelana okunamandla kwe-receptor kunye neenkcukacha ze-receptor.Ezi zilandelayo ziintlobo eziqhelekileyo kunye neendlela zokudibanisa i-RGD cyclic peptide.
Iintlobo eziqhelekileyo ze-RGD cyclic peptides:
1. I-cyclic peptides equlethe ulandelelwano lwe-RGD olwenziwe ngamabhondi e-disulfide
2. Iipeptide ze-cyclic eziqulethe ulandelelwano lwe-RGD olwenziwe ngamabhondi e-amide
Ukwenziwa kwe-RGD cyclic peptide:
Imodeli eluncedo inxulumene nenkqubo ye-RGD ye-cyclic peptide synthesis kwintsimi ye-polypeptide synthesis yesigaba esiqinileyo.Indlela entsha kukukhetha i-resin ye-2-chloro-triphenylmethyl chloride njenge-prerequisite carrier, okokuqala udibanise iqela lokuqala le-carboxyl yecala kunye neqela elikhethekileyo lokukhusela i-D aspartic acid amino acid, emva koko udibanise i-peptide yomgca we-RGD yokulandelelana kwepeptide kwi-resin. , kunye ne-amino acid yokugqibela yokususa iqela elikhuselayo le-FOC ngaphandle kwe-piperidine.I-catalyst ekhankanyiweyo yongezwa ukuba isuse iqela elikhuselayo le-carboxyl yecala lokuqala le-D aspartic acid ngokuthe ngqo kwi-resin, ilandelwa ngokongezwa kwe-piperidine ukususa iqela elikhuselayo le-amino le-FOC ye-amino acid yokugqibela, ilandelwa ngokongezwa kwe-arhente ebophelelayo. ukucima kunye nokunciphisa iqela le-carboxyl kunye neqela le-amino elivezwe ukusuka entloko kunye nesiphelo se-peptide yomgca ngokuthe ngqo kwi-resin ngendlela ye-amide bond ukuvelisa i-peptide ye-cyclic.Ekugqibeleni, i-peptide ye-cyclic inqunywe ngokuthe ngqo kwi-resin kunye nesisombululo sokusika.
Ixesha lokuposa: Apr-24-2023