RGD肽及其衍生物在肿瘤显像及治疗中的研究进展

王浩; 施培基; 周晓靓; 王荣先

王浩 , 施培基 , 周晓靓 , 王荣先

文章导航 > 国际放射医学核医学杂志 > 2007, 31 > 5: (274-277)

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RGD肽及其衍生物在肿瘤显像及治疗中的研究进展

300192 天津, 中国医学科学院放射医学研究所药物研究室
中图分类号: Q516;R730.5

Research development on RGD peptides and its devivates in tumor imaging and therapy

Department of pharmacy, Institute of Radiation Medicine, Chinese Academy of Medical Sciences. Tianjin 300192, China
CLC number: Q516;R730.5

摘要: 精氨酸-甘氨酸-天冬氨酸(RGD)肽存在于多种生物细胞外基质中,能特异性识别细胞表面整合素并与之结合,从而介导多种重要的生命活动.外源性RGD肽与肿瘤细胞表面整合素结合后,可作为体内RGD肽类物质的竞争性抑制剂,抑制肿瘤细胞与细胞外基质的黏附与迁移、抑制肿瘤血管形成、诱导肿瘤细胞凋亡,且具有靶向性标记肿瘤显像以及作为抗肿瘤药物和基因治疗的靶向性传导系统的作用.
- 肽类 /
- 放射性核素显像 /
- 药物疗法 /
- 药物载体 /
- 精氨酸-甘氨酸-天冬氨酸肽
Abstract: RGD peptides exist in extracelular matrix of many kinds of organisms,and they can specificly recognise and combin with integrin receptors. After combining with integrin receptors, extrinsic RGD peptides can prevent tumor cells them adhering and migrating, suppress agiogenesis and induce trunor cells apoptosis. And the derivates of RGD peptides can be used as specific imaging libelling and targetal drug dilivery system for tumor therapy.
- Peptides /
- Radionuclide imaging /
- Drug therapy /
- Drug carriers /
- Arginine-glycineaspartic acid
本作品遵循Signature-Non-Commercial Use 4.0 International (CC BY-NC 4.0)协议

[1]	Zetter BR. On target with tumor blood vessel markers. Nat Biotechnol, 1997, 15(12):1243-1244.
[2]	Janssen M. Oyen W J, Massuger L F, et al. Comparison of a monomeric and dimeric radiolabeled RGD-peplide for tumor targeling. Cancer Biother Radiopharm, 2002, 17(6):641-646.
[3]	Schraa AJ, Kok R J, Moorlag HE, et al. Targeting of RGD-modified proteins to tumor Vasculature:a pharmacokinetic and cellular distribution study. Int J Cancer, 2002,102(5):469-475.
[4]	Pasqualini R, Koivtmen E, Ruoslahti E. A peptide isolated from phage display libraries is a structural and functional mimic of an RGD-binding site on integrins. J Cell Biol, 1995, 130(5):1189-1196.
[5]	Pasqualini R, Ruoslahti E. Organ targeting in vivo using phage displaypeptide libraries. Nature, 1996,380(6572):364-366.
[6]	Rajotte D, Arap W, Hagedorn M, et al. Molecular heterogeneity of the vascular endothelium revealed by in vivo phage display. J Clin Invest, 1998, 102(2):430-437.
[7]	Haubner R, Wester HJ, Weber WA, et al. Noninvasive imaging of α_vβ₃ integrin expression using ¹⁸F-labeled-RGD-containing glycopeptide and positron emission tomography. Cancer Res, 2001, 61(5):1781-1785.
[8]	Su Z.F, Liu G, Gupta S, et al. In vitro and in vivo evaluation of a ^99mTechnetium-labeled cyclic RGD peptide as a specific marker of alpha(V) beta (3) integrin for tumor imaging. Bioconjug Chem, 2002, 13(3):561-570.
[9]	Zitzmann S, Ehemann V, Schwab M. Arginine-glycine-aspartic acid (RGD)-peptide binds to both tumor and tumor-endothelial cells in vivo. Cancer Res, 2002,62(15):5139-5143.
[10]	Achilefu S, Blnch S, Markiewicz MA, et al. Synergistic effects of lightemitting probes and peptides for targeting and monitoring integrin expression. Proc Natl Acal Sci USA, 2005, 102(22):7976-7981.
[11]	Ye Yp, Bloch S, Xu B. Design synthesis and evaluation of near infrared florescent mehimeric RGD peptides for targeting tumors. J Med Chem. 2006, 49(7):2268-2275.
[12]	李前伟,王曙光,郑秀海,等.¹²⁵I-RGD-4CY肿瘤α_vβ₃受体显像的实验研究.第三军医大学学报,2002,24(11):1340-1342.
[13]	程绍钧,李前伟,李忠俊,等.以血管生成为靶点的肿瘤核素显像及治疗的实验研究.第三军医大学学报,2005,27(2):109-111.
[14]	Kok R J, Schraa AJ, Bos EJ, et al. Preparation and functional evaluation of RGD-modified proteins as alpha(v)heta(3) integrin direeted herapeuties. Bioconjug Chore, 2002, 13(1):128-135.
[15]	Buerkle MA, Pahernik SA, Sutter A, et al. Inhibition of the alphanu integrins with a cyclic RGD peptide impairs angiogenesis,growth and metastasis of solid turnouts in vivo. Br J Cancer, 2002, 86(5):788-795.
[16]	Burkhart DJ, Kalet BT, Coleman MP, et al. Doxorubicin-formaldehyde conjugates targeting α_vβ₃ integrin. Mol Cancer Ther, 2004, 3(12):1593-1604.
[17]	Curnis F, Sacchi A, Cortt A. Improving chemotherapeutic drug penetra-tion in tumors by vascular targeting and barrier alteration. J Clin Invest, 2002, 110(4):475-482.
[18]	Curnis F, Gasparri A, Sacchi A, et al. Coupling tumor necrosis factor-alpha with alphaV integriu ligands improves its antineoplastic activity. Cancer Res 2004, 64(2):565-571.
[19]	王芳,蒋建伟,曾慧兰,等.整合素受体介导bcl-2反义核酸联合化疗药物对大肠癌细胞的增殖抑制作用.实用医学杂志,2006,22(7):748-749.
[20]	熊小兵,黄悦,吕万良,等.RGD类似物修饰的阿霉素隐形脂质体的制备及体外细胞结合试验.药学学报,2005,40(12):1085-1090.
[21]	邱峰,陈世知,陈虹,等.新型腺病毒载体的制备及其特性研究.重庆医科大学学报,2006,31(3):330-333.
[22]	Dijkgraaff I, Kruijtzer JA, Lin S, et al. Improved targeting of the α_vβ₃ integrin by muhimerisation of RGD peptides. Eur J Nucl Med Mol Imaging, 2007, 34(2):267-273.
[23]	Halahan DE, Qu S, Geng L, et al. Radialion-medialed control of drug delivery. Am Clin Oncol, 2001, 24(5):473-480.

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RGD肽及其衍生物在肿瘤显像及治疗中的研究进展

300192 天津, 中国医学科学院放射医学研究所药物研究室

收稿日期: 2007-03-27

关键词:

摘要: 精氨酸-甘氨酸-天冬氨酸(RGD)肽存在于多种生物细胞外基质中,能特异性识别细胞表面整合素并与之结合,从而介导多种重要的生命活动.外源性RGD肽与肿瘤细胞表面整合素结合后,可作为体内RGD肽类物质的竞争性抑制剂,抑制肿瘤细胞与细胞外基质的黏附与迁移、抑制肿瘤血管形成、诱导肿瘤细胞凋亡,且具有靶向性标记肿瘤显像以及作为抗肿瘤药物和基因治疗的靶向性传导系统的作用.