Research Advances on RGD Peptides in Diagnosis and Treatment of Neoplasms_CHINESE JOURNAL OF BASES AND CLINICS IN GENERAL SURGERY

Authors：

DU Guocheng , WU Chengyi.

Department of General Surgery, The First Affiliated Hospital, Chongqing University of Medical Sciences, Chongqing 400016, China;

Corresponding author：

Keywords：

Arg-Gly-Asp peptide Integrin Neoplasm diagnosis Neoplasm therapy

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【Abstract】Objective To introduce the current research status, value and development future of Arg-Gly-Asp (RGD) peptides in diagnosis and treatment of neoplasms.
Methods The current literatures on advances about RGD peptides in diagnosis and treatment of neoplasms were reviewed.
Results RGD peptides, specificly recognizing and combining with integrin receptors, exist in extracellular matrix (ECM) of many kinds of organisms. After combining with integrin receptors, extrinsic RGD peptides can prevent tumor cells from adhering to ECM and migrating as the competitive inhibitor of intrinsic RGD peptides, suppress agiogenesis and induce tumor cells apoptosis, showing potential value of tumor specific imaging by targetal labelling neoplasms and treating tumors combining with other methods.
Conclusion RGD peptides may be a new drug for diagnosis and treatment of neoplasms.

Citation： DU Guocheng,WU Chengyi.. Research Advances on RGD Peptides in Diagnosis and Treatment of Neoplasms. CHINESE JOURNAL OF BASES AND CLINICS IN GENERAL SURGERY, 2004, 11(6): 558-560. doi: Copy

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.	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. 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. 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.

CHINESE JOURNAL OF BASES AND CLINICS IN GENERAL SURGERY

Research Advances on RGD Peptides in Diagnosis and Treatment of Neoplasms

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