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Before 2006
授权专利(12项目):
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2006  (2 / Total 98 )

  • 1
    Jia B, Shi J, Yang Z, Xu B, Liu Z, Zhao H, Liu S*, Wang F*. 99mTc-Labeled Cyclic RGDfK Dimer: Initial Evaluation for SPECT Imaging of Glioma Integrin αvβ3 Expression. Bioconjugate Chem. 2006, 17(4):1069-1706.

    This report describes the evaluation of biodistribution properties of three radiotracers, [99mTc(SQ168)(EDDA)], [99mTc(SQ168)(tricine)(PDA)], and [99mTc(SQ168)(tricine)(TPPTS)] (SQ168 = [2-[[[5-[carboonyl]-2-pyridinyl]hydrazono]methyl]benzenesulfonic acid]-Glu(cyclo{Lys-Arg-Gly-Asp-d-Phe})-cyclo{Lys-Arg-Gly-Asp-d-Phe}; EDDA = ethylenediamine-N,N‘-diacetic acid; PDA = 2,5-pyridinedicarboxylic acid; TPPTS = trisodium triphenylphosphine-3,3‘,3‘ ‘-trisulfonate), and their potential to image the glioma integrin αvβ3expression in BALB/c nude mice bearing the U87MG human glioma xenografts. It was found that all three radiotracers were able to localize in glioma tumors with a relatively high tumor uptake and long tumor retention time by binding to the integrin αvβ3 expressed on both tumor cells and endothelial cells of tumor neovasculature. It seems that the coligand has minimal effect on integrin αvβ3 targeting capability of the 99mTc-labeled RGDfK dimer, but it has a significant impact on their biodistribution properties. For example, the complex [99mTc(SQ168)(tricine)(TPPTS)] has the lowest liver uptake and the highest metabolic stability in normal BALB/c nude mice. Results from SPECT imaging studies show that the glioma tumors can be clearly visualized with all three radiotracers at 4 h postinjection. Among the three radiotracers evaluated in this study, [99mTc(SQ168)(tricine)(TPPTS)] has the best imaging quality and is a promising candidate for more preclinical evaluations in the future.

    http://dx.doi.org/10.1021/bc060055b

  • 2
    Shao W, Zhao S, Liu Z, Zhang J, Ma S, Sato J, Zhang P, Tong M, Han J, Wang Y, Bai D, Wang F*, Sun L*. Inhibition of Human Tumor Xenograft Growth in Nude Mice by a Conjugate of Monoclonal Antibody LA22 to Epidermal Growth Factor Receptor with Anti-tumor Antibiotics Mitomycin C. Biochem Bioph Res Com. 2006, 349:816-824.

    Abstract

    Anti-EGFR monoclonal antibodies LA22 and Erbitux bind to different epitopes of EGFR. The chemimmunoconjugates of MMC with LA22 or Erbitux were prepared, and in vitro cytotoxicity assays with A549 cells showed that LA22-MMC was much more potent than Erbitux or Erbitux-MMC. Viabilities of A549 cells treated with LA22-MMC, Erbitux or Erbitux-MMC were 35%, 94%, and 81%, respectively. Immunoscintigraphy of xenografts of human A431 and A549 cells in nude mice both showed that (125)I-labeled-LA22-MMC enriched in tumor sites prominently. Most importantly, in vivo assays showed LA22-MMC was significantly more effective than free drug MMC in the treatment of subcutaneous xenografts of human A431 cells innude mice (83% inhibition for LA22-MMC and 30% for MMC). We concluded that LA22-MMC could be a very potent drug for treatment of solid tumors.http://dx.doi.org/10.1016/j.bbrc.2006.08.114

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