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Noninvasive imaging of c(RGD)29R as a potential delivery carrier for transfection of siRNA in malignant tumors

文献作者：Xue Qi Chen, Meng Liu, Rong Fu Wang, Ping Yan, Chun Li Zhang, Chao Ma, Qian Zhao, Lei Yin, Guang Yu Zhao, Feng Qin Guo   《Journal of Labelled Compounds and Radiopharmaceuticals》

ABSTRACTS
The purpose of our study was to develop and evaluate a novel integrin αvβ3specific delivery carrier for transfection of siRNA in malignant tumors. We adopted arginineglycineaspartate (RGD) motif as a tissue target for specific recognition of integrin ανβ3. A chimaeric peptide was synthesized by adding nonamer arginine residues (9arginine [9R]) at the carboxy terminus of cyclicRGD dimer, designated as c(RGD)29R, to enable small interfering RNA (siRNA) binding. To test the applicability of the delivery carrier in vivo, c(RGD)29R was labeled with radionuclide of technetium99m. Biodistribution and γcamera imaging studies were performed in HepG2 xenograftbearing nude mice. As results, an optimal 10:1 molar ratio of 99mTcc(RGD)29R to siRNA was indicated by the electrophoresis on agarose gels. 99mTcc(RGD)29R/siRNA remained stable under a set of conditions in vitro. For in vivo study, tumor radioactivity uptake of 99mTcc(RGD)29R/siRNA in nude mice bearing HepG2 xenografts was significantly higher than that of control probe (P < .05). The xenografts were clearly visualized at 4 hours till 6 hours noninvasively after intravenous injection of 99mTcc(RGD)29R/siRNA, while the xenografts were not visualized at any time after injection of control probe. It was concluded that c(RGD)29R could be an effective siRNA delivery carrier. Technetium99m radiolabeleddelivery carrier represents a potential imaging strategy for RNAibased therapy.
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All the peptides were synthesized by ChinaPeptides Co, Ltd.
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https://onlinelibrary.wiley.com/doi/full/10.1002/jlcr.3514
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Deubiquitinating enzyme USP9X regulates cellular clock function by modulating the ubiquitination and degradation of a core circadian protein BMAL1

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CAS:85466-18-8|Thymopoietin II (32-35)|RKDV

Contact： Liven Qian(钱叶华)-Custom Peptide Mobile: 13761298676（微信） Email：cps037@chinapeptides.net QQ：2880526724 ChinaPeptides Co., Ltd./强耀生物科技有限公司 Name Thymopoietin II (32-35) Code [85466-18-8] The alias Thymopoietin II (32-35) Sequence (single letter abbreviation) RKDV Sequence (three-letter abbreviation) H-Arg-Lys-Asp-Val-OH (trifluoroacetate salt) A basic description TP-4 and TP-3; shortest active thymopoietin II fragments described that exhibit potent immunoregulatory properties in vitro and in vivo. solubility The molecular weight 516.6 Chemical formula C21H40N8O7 The purity 80%，90%，95%，98%，99% Weight 1mg,5mg,10mg,50mg,100mg,1g Storage conditions Store at -20°C. Keep tightly closed. Store in a cool dry place. Number of Residues: 4 1-Letter Code: RKDV 3-Letter Code: Arg-Lys-Asp-Val Molecular weight (Mr): 516.6 g/mol Isoelectric point: 10.1 Net charge at pH 7.0: 1.0 Average hydrophilicity: 1.9 Ratio of hydrophilic residues / total number of residues...
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