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《Journal of Third Military Medical University》 2012-01
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Radionuclide labeling of small molecular inhibitory peptides targeting VEGF receptor

Feng Shibin1,Li Qianwei1,Zheng Lei1,Zou Lingyun2,Zha Lin1,Ren Hao1,Huang Dingde1(1Department of Nuclear Medicine,Southwest Hospital,2Department of Microbiology,Laboratory of Microbiological Engineering,College of Basic Medical Sciences,Third Military Medical University,Chongqing,400038,China)  
Objective To investigate radionuclide labeling methods of small molecular inhibitory peptide targeting vascular endothelial growth factor receptor(VEGF receptor) of tumor with 99Tcm.Methods After being modified by S-acetyl-MAG3,GA(D)GG and HYNIC respectively,QKRKRKKSRKKH and RKRKRKKSRYIVLS were labeled with 99Tcm.Labeling efficiency and radiochemical purity was identified by paper chromatography and HPLC.The inhibitory affect of peptide to tumor cell was testified by 3H-TdR incorporation.Receptor competition binding assay was used to testify the affinity of peptide ligand based on A549 cells.Results The labeling efficiency of two peptide modified by three bifunctional chelating agents was about 78%,40% and 94% respectively.The inhibitory efficiency of HYNIC-QKRKRKKSRKKH and HYNIC-RKRKRKK-SRYIVLS to A549 cells was about(32.86±3.36)% and(61.50±4.50)%,and did not have statistically significant difference with QKRKRKKSRKKH and RKRKRKKSRYIVLS.Meanwhile the 99Tcm-HYNIC-QKRKRKKSRKKH and 99Tcm-HYNIC-RKRKRKKSRYIVLS retained a good stability and binding activity of VEGF receptor in A549 cells.Conclusion HYNIC-QKRKRKKSRKKH and HYNIC-RKRKRKKSRYIVLS have a high labeling efficiency with TPPTS as a reducing agent and collaborative ligand,and the labeled agents retain inhibiting activity and binding activity of receptor to A549 cells.
【Fund】: 国家自然科学基金面上项目(30970848);; 重庆市自然科学基金(CSTC2009BB5337)~~
【CateGory Index】: R394-33
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