iRGD peptide (c(CRGDKGPDC)) is a cyclic peptide composed of 9 amino acids that can specifically bind to av integrin and then be enzymatically hydrolyzed to produce CRGDK/R, which interacts with neuropilin-1 (NRP-1), thereby triggering drug tissue penetration and having tumor targeting and tumor penetration properties[1]. iRGD peptide is a promising cancer imaging peptide and a potential therapeutic agent for a variety of cancers. iRGD peptide can effectively and deeply deliver imaging agents and anticancer drugs into tumors[2]. iRGD peptide does not affect the survival of tumor cells, but can inhibit spontaneous tumor metastasis[3].
In vitro, iRGD peptide (64μM) treatment of A549 cells for 1h significantly enhanced the membrane permeability induced by low concentrations of HPRP-A1 (4μM, 8μM) and improved the anticancer activity of HPRP-A1[4].
In vivo, iRGD peptide (4mmol/kg) was intravenously injected into mice bearing HCG27 and NCI-N87 cell xenografts for 4 weeks, significantly enhancing the chemotherapeutic effect of 5-FU and inhibiting the growth rate of tumors in both tumor-bearing mice[5]. iRGD peptide (4mg/kg) was intravenously injected into mice bearing A549 cell xenografts for 30 days, significantly enhancing the chemotherapeutic effect of gemcitabine, inhibiting tumor cell proliferation and inducing cell apoptosis[6].
References:
[1] Thirumalai A, Girigoswami K, Pallavi P, et al. Cancer therapy with iRGD as a tumor-penetrating peptide[J]. Bulletin du Cancer, 2023, 110(12): 1288-1300.
[2] Zuo H. iRGD: a promising peptide for cancer imaging and a potential therapeutic agent for various cancers[J]. Journal of oncology, 2019, 2019(1): 9367845.
[3] Yin H, Yang J, Zhang Q, et al. iRGD as a tumor‑penetrating peptide for cancer therapy[J]. Molecular medicine reports, 2017, 15(5): 2925-2930.
[4] Hu C, Chen X, Huang Y, et al. Co-administration of iRGD with peptide HPRP-A1 to improve anticancer activity and membrane penetrability[J]. Scientific reports, 2018, 8(1): 2274.
[5] Zhang L I, Xing Y, Gao Q I, et al. Combination of NRP1-mediated iRGD with 5-fluorouracil suppresses proliferation, migration and invasion of gastric cancer cells[J]. Biomedicine & Pharmacotherapy, 2017, 93: 1136-1143.
[6] Zhang Q, Zhang Y, Li K, et al. A novel strategy to improve the therapeutic efficacy of gemcitabine for non-small cell lung cancer by the tumor-penetrating peptide iRGD[J]. PLoS One, 2015, 10(6): e0129865.
iRGD peptide (c(CRGDKGPDC))是一种由9个氨基酸组成的环状肽，能够特异性结合av整合素，然后被酶解产生CRGDK/R与神经纤毛蛋白-1（NRP-1）相互作用，从而触发药物的组织渗透，具有肿瘤靶向和肿瘤穿透特性[1]。iRGD peptide是一种有前景的癌症成像肽和多种癌症的潜在治疗剂，可以将成像剂和抗癌药物有效而深入地递送到肿瘤内[2]。iRGD peptide不影响肿瘤细胞的存活，但能够抑制自发性肿瘤转移[3]。
在体外，iRGD peptide（64μM）处理A549细胞1h，显著增强了低浓度下HPRP-A1（4μM、8μM）诱导的膜通透性，提高了HPRP-A1的抗癌活性[4]。
在体内，iRGD peptide（4mmol/kg）通过静脉注射治疗HCG27和NCI-N87细胞异种移植小鼠4周，显著增强了5-FU的化疗效果，抑制了两种荷瘤小鼠体内肿瘤的生长速度[5]。iRGD peptide（4mg/kg）通过静脉注射治疗A549细胞异种移植小鼠30天，显著增强了吉西他滨（Gemcitabine）的化疗效果，抑制了肿瘤细胞增殖、诱导了细胞凋亡[6]。