Novel small peptides derived from VEGF 125-136 : potential drugs for radioactive diagnosis and therapy in A549 tumor-bearing nude mice
Vascular endothelial growth factor receptor (VEGFR) is a critical factor in tumor angiogenesis and has been considered a potential target for receptor-mediated radionuclide imaging and therapy. In this study, we identified two peptides (QKRKRKKSRKKH and RKRKRKKSRYIVLS) derived from VEGF that display...
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Published in | Scientific reports Vol. 7; no. 1; p. 4278 |
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Main Authors | , , , , , , , |
Format | Journal Article |
Language | English |
Published |
England
27.06.2017
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Abstract | Vascular endothelial growth factor receptor (VEGFR) is a critical factor in tumor angiogenesis and has been considered a potential target for receptor-mediated radionuclide imaging and therapy. In this study, we identified two peptides (QKRKRKKSRKKH and RKRKRKKSRYIVLS) derived from VEGF
that displayed high binding affinities to VEGFR and strong inhibition of A549 cell growth.
Tc- and
Re-labeled peptides displayed high labeling efficiency and favorable stability in saline and human plasma. At the cellular level, the radiolabeled peptides could bind with A549 cells and be internalized via the VEGFR-1-mediated pathway.
Tc/
Re-labeled peptide was significantly accumulated at xenograft tumors, as observed with single-photon emission computed tomography (SPECT) planar imaging. Moreover,
Re-labeled peptides significantly inhibited tumor growth, prolonged the survival time of the tumor-bearing nude mice and resulted in much more necrotic regions and apoptotic cells in the A549 xenograft tumors. These results demonstrated that these two peptides as candidate drugs for radionuclide imaging and tumor therapy. |
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AbstractList | Vascular endothelial growth factor receptor (VEGFR) is a critical factor in tumor angiogenesis and has been considered a potential target for receptor-mediated radionuclide imaging and therapy. In this study, we identified two peptides (QKRKRKKSRKKH and RKRKRKKSRYIVLS) derived from VEGF
that displayed high binding affinities to VEGFR and strong inhibition of A549 cell growth.
Tc- and
Re-labeled peptides displayed high labeling efficiency and favorable stability in saline and human plasma. At the cellular level, the radiolabeled peptides could bind with A549 cells and be internalized via the VEGFR-1-mediated pathway.
Tc/
Re-labeled peptide was significantly accumulated at xenograft tumors, as observed with single-photon emission computed tomography (SPECT) planar imaging. Moreover,
Re-labeled peptides significantly inhibited tumor growth, prolonged the survival time of the tumor-bearing nude mice and resulted in much more necrotic regions and apoptotic cells in the A549 xenograft tumors. These results demonstrated that these two peptides as candidate drugs for radionuclide imaging and tumor therapy. |
Author | Liu, Jie Feng, Shibin Xie, Laiping Li, Hongmin Li, Qianwei Huang, Dingde Zheng, Lei Zhang, Xiang |
Author_xml | – sequence: 1 givenname: Xiang surname: Zhang fullname: Zhang, Xiang organization: Department of Nuclear Medicine, Southwest Hospital, Third Military Medical University, 30 Gaotanyan Street, Shapingba District, Chongqing, 400038, China – sequence: 2 givenname: Shibin surname: Feng fullname: Feng, Shibin organization: Department of Nuclear Medicine, Southwest Hospital, Third Military Medical University, 30 Gaotanyan Street, Shapingba District, Chongqing, 400038, China – sequence: 3 givenname: Jie surname: Liu fullname: Liu, Jie organization: Department of Nuclear Medicine, Southwest Hospital, Third Military Medical University, 30 Gaotanyan Street, Shapingba District, Chongqing, 400038, China – sequence: 4 givenname: Qianwei surname: Li fullname: Li, Qianwei organization: Department of Nuclear Medicine, Southwest Hospital, Third Military Medical University, 30 Gaotanyan Street, Shapingba District, Chongqing, 400038, China – sequence: 5 givenname: Lei surname: Zheng fullname: Zheng, Lei organization: Department of Nuclear Medicine, Southwest Hospital, Third Military Medical University, 30 Gaotanyan Street, Shapingba District, Chongqing, 400038, China – sequence: 6 givenname: Laiping surname: Xie fullname: Xie, Laiping organization: Department of Nuclear Medicine, Southwest Hospital, Third Military Medical University, 30 Gaotanyan Street, Shapingba District, Chongqing, 400038, China – sequence: 7 givenname: Hongmin surname: Li fullname: Li, Hongmin organization: Department of Nuclear Medicine, Southwest Hospital, Third Military Medical University, 30 Gaotanyan Street, Shapingba District, Chongqing, 400038, China – sequence: 8 givenname: Dingde surname: Huang fullname: Huang, Dingde email: huangdde@tmmu.edu.cn organization: Department of Nuclear Medicine, Southwest Hospital, Third Military Medical University, 30 Gaotanyan Street, Shapingba District, Chongqing, 400038, China. huangdde@tmmu.edu.cn |
BackLink | https://www.ncbi.nlm.nih.gov/pubmed/28655913$$D View this record in MEDLINE/PubMed |
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Snippet | Vascular endothelial growth factor receptor (VEGFR) is a critical factor in tumor angiogenesis and has been considered a potential target for receptor-mediated... |
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SubjectTerms | Animals Cell Line, Tumor Disease Models, Animal Humans Male Mice Molecular Structure Neoplasms - diagnosis Neoplasms - drug therapy Neoplasms - mortality Neoplasms - pathology Peptide Fragments - chemistry Peptide Fragments - pharmacology Protein Binding Radioisotopes Radiopharmaceuticals Rhenium Tissue Distribution Tomography, Emission-Computed, Single-Photon Vascular Endothelial Growth Factor A - chemistry Xenograft Model Antitumor Assays |
Title | Novel small peptides derived from VEGF 125-136 : potential drugs for radioactive diagnosis and therapy in A549 tumor-bearing nude mice |
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