跳至主要内容

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.
SCREENSHOT

RELATED PRODUCTS
All the peptides were synthesized by ChinaPeptides Co, Ltd.
CHAINING
https://onlinelibrary.wiley.com/doi/full/10.1002/jlcr.3514

评论

此博客中的热门博文

The therapeutic effect of anti-CD52 treatment in murine experimental autoimmune encephalomyelitis is associated with altered IL-33 and ST2 expression levels

文献作者:Mark Barbour, Rachel Wood, Shehla U.Hridi, Chelsey Wilson, Grant McKay, Trevor J.Bushell, Hui-Rong Jiang   《Journal of Neuroimmunology》 ABSTRACTS Experimental autoimmune encephalomyelitis  (EAE) mice were administered with murine anti-CD52  antibody  to investigate its therapeutic effect and whether the treatment modulates IL-33 and ST2 expression. EAE severity and  central nervous system  (CNS) inflammation were reduced following the treatment, which was accompanied by peripheral  T and B lymphocyte  depletion and reduced production of various  cytokines  including IL-33, while sST2 was increased. In spinal cords of EAE mice, while the number of IL-33 +  cells remained unchanged, the extracellular level of IL-33 protein was significantly reduced in anti-CD52 antibody treated mice compared with controls. Furthermore the number of ST2 +  cells in the spinal cord of treated EAE mice was  downregulated ...

Mutational analysis of the extracellular disulphide bridges of the atypical chemokine receptor ACKR3/CXCR7 uncovers multiple binding and activation modes for its chemokine and endogenous non-chemokine agonists

Author:Martyna Szpakowska, Max Meyrath, Nathan Reynders,  Manuel Counson, Julien Hanson, Jan Steyaert, Andy Chevigné     《Biochemical Pharmacology》 ABSTRACTS The atypical chemokine receptor ACKR3/CXCR7 plays crucial roles in numerous physiological processes but also in viral infection and cancer. ACKR3 shows strong propensity for activation and, unlike classical chemokine receptors, can respond to chemokines from both the CXC and CC families as well as to the endogenous peptides BAM22 and adrenomedullin. Moreover, despite belonging to the G protein coupled receptor family, its function appears to be mainly dependent on β-arrestin. ACKR3 has also been shown to continuously cycle between the plasma membrane and the endosomal compartments, suggesting a possible role as a scavenging receptor. So far, the molecular basis accounting for these atypical binding and signalling properties remains elusive. Noteworthy, ACKR3 extracellular domains bear three  di...

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...