• 重慶醫(yī)科大學附屬第一醫(yī)院普外科（重慶400016）;

目的  介紹精氨酸-甘氨酸-天冬氨酸（RGD）肽在腫瘤診治領(lǐng)域的研究現(xiàn)狀、價值及發(fā)展前景。
方法  對RGD肽在腫瘤診治領(lǐng)域的實驗研究新進展進行綜述。
結(jié)果  RGD肽存在于多種生物細胞外基質(zhì)中，能特異性識別細胞表面整和素并與之結(jié)合，從而介導多種重要的生命活動。外源性RGD肽與腫瘤細胞表面整和素結(jié)合后，可作為體內(nèi)RGD肽類物質(zhì)的競爭性抑制劑，從而能抑制腫瘤細胞與細胞外基質(zhì)的黏附與遷移、抑制腫瘤血管形成、誘導腫瘤細胞凋亡，且具有靶向性標記腫瘤顯像以及與其他方法聯(lián)合治療腫瘤的潛在價值。
結(jié)論  RGD肽能從多個環(huán)節(jié)對腫瘤起到抑制作用，且展示出與其他療法聯(lián)合治療腫瘤的前景。

引用本文： 杜果城,吳誠義. RGD肽與腫瘤診治的研究進展. 中國普外基礎(chǔ)與臨床雜志, 2004, 11(6): 558-560. doi: 復(fù)制

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2. Allen CM, Sharman WM, La Madeleine C, et al. Attenuation of photodynamically induced apoptosis by an RGD containing peptide [J]. Photochem Photobiol Sci, 2002; 1(4)∶246.
3. Chavakis E, Riecke B, Lin J, et al. Kinetics of integrin expression in the mouse model of proliferative retinopathy and success of secondary intervention with cyclic RGD peptides [J]. Diabetologia, 2002; 45(2)∶262.
4. Janssen M, Oyen WJ, Massuger LF, et al. Comparison of a monomeric and dimeric radiolabeled RGDpeptide for tumor targeting [J]. Cancer Biother Radiopharm， 2002; 17(6)∶641.
5. Schraa AJ, Kok RJ, Moorlag HE, et al. Targeting of RGDmodified proteins to tumor vasculature: a pharmacokinetic and cellular distribution study [J]. Int J Cancer， 2002; 102(5)∶469.
6. Zhao M, Wang C, Jiang X, et al. Synthesis of RGD containing peptides and their bioactivities [J]. Prep Biochem Biotechnol， 2002; 32(4)∶363.
7. Richards J, Miller M, Abend J, et al. Engineered fibronectin type III domain with a RGDWXE sequence binds with enhanced affinity and specificity to human alphavbeta3 integrin [J]. J Mol Biol， 2003; 326(5)∶1475.
8. Humphries MJ, Mould AP. Structure. An anthropomorphic integrin [J]. Science， 2001; 294(5541)∶316.
9. Su ZF, Liu G, Gupta S, et al. In vitro and in vivo evaluation of a Technetium99mlabeled cyclic RGD peptide as a specific marker of alpha(V)beta(3) integrin for tumor imaging [J]. Bioconjug Chem， 2002; 13(3)∶561.
10. Su ZF, He J, Rusckowski M, et al. In vitro cell studies of technetium99m labeled RGDHYNIC peptide, a comparison of tricine and EDDA as coligands [J]. Nucl Med Biol， 2003; 30(2)∶141.
11. Madeja Z, Sroka J. Contact guidance of Walker carcinosarcoma cells by the underlying normal fibroblasts is inhibited by RGDcontaining synthetic peptides [J]. Folia Histochem Cytobiol， 2002; 40(3)∶251.
12. Buckley CD, Pilling D, Henriquez NV, et al. RGD peptides induce apoptosis by direct caspase3 activation [J]. Nature， 1999; 397(6719)∶534.
13. Kok RJ, Schraa AJ, Bos EJ, et al. Preparation and functional evaluation of RGDmodified proteins as alpha(v)beta(3) integrin directed therapeutics [J]. Bioconjug Chem， 2002; 13(1)∶128.
14. Buerkle MA, Pahernik SA, Sutter A, et al. Inhibition of the alphanu integrins with a cyclic RGD peptide impairs angiogenesis, growth and metastasis of solid tumours in vivo [J]. Br J Cancer， 2002; 86(5)∶788.
15. Zygmunt M, Herr F, KellerSchoenwetter S, et al. Characterization of human chorionic gonadotropin as a novel angiogenic factor [J]. J Clin Endocrinol Metab， 2002; 87(11)∶5290.
16. de Groot FM, Broxterman HJ, Adams HP, et al. Design, synthesis, and biological evaluation of a dual tumorspecific motive containing integrintargeted plasmincleavable doxorubicin prodrug [J]. Mol Cancer Ther， 2002; 1(11)∶901.
17. Burke PA, DeNardo SJ, Miers LA, et al. Cilengitide targeting of alpha(v)beta(3) integrin receptor synergizes with radioimmunotherapy to increase efficacy and apoptosis in breast cancer xenografts [J]. Cancer Res, 2002; 62(15)∶4263.
18. Burke PA, DeNardo SJ, Miers LA,et al. Combined modality radioimmunotherapy. Promise and peril [J]. Cancer， 2002; 94(4 Suppl)∶1320.
  1. 1. 11Kang IC, Kim DS, Jang Y, et al. Suppressive mechanism of salmosin, a novel disintegrin in B16 melanoma cell metastasis [J]. Biochem Biophys Res Commun， 2000; 275(1)∶169 12Anuradha CD, Kanno S, Hirano S. RGD peptideinduced apoptosis in human leukemia HL60 cells requires caspase3 activation [J]. Cell Biol Toxicol， 2000; 16(5)∶275.
  2. 2. Allen CM, Sharman WM, La Madeleine C, et al. Attenuation of photodynamically induced apoptosis by an RGD containing peptide [J]. Photochem Photobiol Sci, 2002; 1(4)∶246.
  3. 3. Chavakis E, Riecke B, Lin J, et al. Kinetics of integrin expression in the mouse model of proliferative retinopathy and success of secondary intervention with cyclic RGD peptides [J]. Diabetologia, 2002; 45(2)∶262.
  4. 4. Janssen M, Oyen WJ, Massuger LF, et al. Comparison of a monomeric and dimeric radiolabeled RGDpeptide for tumor targeting [J]. Cancer Biother Radiopharm， 2002; 17(6)∶641.
  5. 5. Schraa AJ, Kok RJ, Moorlag HE, et al. Targeting of RGDmodified proteins to tumor vasculature: a pharmacokinetic and cellular distribution study [J]. Int J Cancer， 2002; 102(5)∶469.
  6. 6. Zhao M, Wang C, Jiang X, et al. Synthesis of RGD containing peptides and their bioactivities [J]. Prep Biochem Biotechnol， 2002; 32(4)∶363.
  7. 7. Richards J, Miller M, Abend J, et al. Engineered fibronectin type III domain with a RGDWXE sequence binds with enhanced affinity and specificity to human alphavbeta3 integrin [J]. J Mol Biol， 2003; 326(5)∶1475.
  8. 8. Humphries MJ, Mould AP. Structure. An anthropomorphic integrin [J]. Science， 2001; 294(5541)∶316.
  9. 9. Su ZF, Liu G, Gupta S, et al. In vitro and in vivo evaluation of a Technetium99mlabeled cyclic RGD peptide as a specific marker of alpha(V)beta(3) integrin for tumor imaging [J]. Bioconjug Chem， 2002; 13(3)∶561.
  10. 10. Su ZF, He J, Rusckowski M, et al. In vitro cell studies of technetium99m labeled RGDHYNIC peptide, a comparison of tricine and EDDA as coligands [J]. Nucl Med Biol， 2003; 30(2)∶141.
  11. 11. Madeja Z, Sroka J. Contact guidance of Walker carcinosarcoma cells by the underlying normal fibroblasts is inhibited by RGDcontaining synthetic peptides [J]. Folia Histochem Cytobiol， 2002; 40(3)∶251.
  12. 12. Buckley CD, Pilling D, Henriquez NV, et al. RGD peptides induce apoptosis by direct caspase3 activation [J]. Nature， 1999; 397(6719)∶534.
  13. 13. Kok RJ, Schraa AJ, Bos EJ, et al. Preparation and functional evaluation of RGDmodified proteins as alpha(v)beta(3) integrin directed therapeutics [J]. Bioconjug Chem， 2002; 13(1)∶128.
  14. 14. Buerkle MA, Pahernik SA, Sutter A, et al. Inhibition of the alphanu integrins with a cyclic RGD peptide impairs angiogenesis, growth and metastasis of solid tumours in vivo [J]. Br J Cancer， 2002; 86(5)∶788.
  15. 15. Zygmunt M, Herr F, KellerSchoenwetter S, et al. Characterization of human chorionic gonadotropin as a novel angiogenic factor [J]. J Clin Endocrinol Metab， 2002; 87(11)∶5290.
  16. 16. de Groot FM, Broxterman HJ, Adams HP, et al. Design, synthesis, and biological evaluation of a dual tumorspecific motive containing integrintargeted plasmincleavable doxorubicin prodrug [J]. Mol Cancer Ther， 2002; 1(11)∶901.
  17. 17. Burke PA, DeNardo SJ, Miers LA, et al. Cilengitide targeting of alpha(v)beta(3) integrin receptor synergizes with radioimmunotherapy to increase efficacy and apoptosis in breast cancer xenografts [J]. Cancer Res, 2002; 62(15)∶4263.
  18. 18. Burke PA, DeNardo SJ, Miers LA,et al. Combined modality radioimmunotherapy. Promise and peril [J]. Cancer， 2002; 94(4 Suppl)∶1320.