iRGD 1392278-76-0 peptide環(huán)肽? c(CRGDKGPDC) 腫瘤靶向肽?

【中文名稱】RGD環(huán)肽

【英文名稱】c(CRGDKGPDC)，iRGD peptide

【CAS】1392278-76-0

【結(jié)構(gòu)式】

【單字母】H2N-CRGDKGPDC-OH(Disulfide Bridge:C1-C9)

【三字母】H2N-Cys-Arg-Gly-Asp-Lys-Gly-Pro-Asp-Cys-COOH(Disulfide Bridge:Cys1-Cys9)

【氨基酸個(gè)數(shù)】? 9

【分子式】C35H57N13O14S2

【平均分子量】?948.04

【精確分子量】 947.36

【等電點(diǎn)(PI)】8.83

【pH=7.0時(shí)的凈電荷數(shù)】1.91

【平均親水性】1.6666666666667

【疏水性值】-1.42

【外觀與性狀】 粉末狀固體

【體內(nèi)研究】

iRGD inserted in the oncolytic adenovirus ICOVIR15K (ICOVIR15K-iRGD) enhances early adenovirus dissemination through the tumor mass and elevates the antitumor effect in mice[1]. iRGD (4 mmol/kg, i.v.) in combination with 5-FU significantly suppresses the tumor growth in nude mice bearing human gastric cancer cells[2].

MCE has not independently confirmed the accuracy of these methods. They are for reference only.

【體外研究】

iRGD peptide-mediated tumor penetration occurs in three steps: binding to αv-integrins on tumor vasculature or tumor cells, exposure by proteolysis of a C-terminal motif that binds to neuropilin-1 (NRP-1) and cell internalization. iRGD peptide inserted in the ICOVIR15K fiber C terminus enhances binding and internalization only in MCF7 cells, which express NRP-1 and integrins. iRGD insertion does not impair virus infection and replication[1]. iRGD peptide alone has no obvious effect on gastric cancer cells, and when combined with 5-FU, iRGD peptide (0.3 μmol/mL) enhances the chemotherapy efficacy of 5-FU on gastric cancer cells through NRP1[2].

MCE has not independently confirmed the accuracy of these methods. They are for reference only.

【產(chǎn)品簡(jiǎn)介】

iRGD (CRGDKGPDC) (Disulfide bridge: C1-C9)是一種由 9 個(gè)氨基酸組成的二硫鍵環(huán)肽，由第一位半胱氨酸C與末尾的C巰基之間氧化形成二硫鍵。它能夠與整合素結(jié)合后酶解產(chǎn)生 CRGDK ，再與 神經(jīng)纖毛蛋白-1 (neuropilin-1) 相互作用，從而促進(jìn)藥物的組織滲透，具有靶向腫瘤以及腫瘤滲透的作用。iRGD和DSPE-PEG偶聯(lián)后，DSPE-PEG-iRGD可以用來(lái)制作膠束，囊泡等納米顆粒；iRGD-PEG-DSPE形成的脂質(zhì)體可以直接作用于腫瘤靶點(diǎn)，形成主動(dòng)靶向效果。