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D-galactose receptor-targeted in vivo spectral fluorescence imaging of peritoneal metastasis using galactosamin-conjugated serum albumin-rhodamine green.

Abstract
The wavelength resolved spectral fluorescence imaging technique using a fluorescein-conjugated avidin has been reported to visualize submillimeter implants of ovarian cancer because of its highly targeted and quickly cleared pharmacokinetics. However, clinical application of avidin was hampered by its strong immunogenicity. As a clinically feasible alternative to avidin, which targets the same D-galactose receptor but is made from a nonimmunogenic source, with even better binding capability by multiplying binding sites but still maintaining a favorable characteristic of high isoelectric point, a serum albumin conjugated with 23 galactosamine and 2 rhodamine green molecules (GmSA-RhodG) was designed and synthesized. GmSA-RhodG showed more than 10-fold rapid and higher uptake by SHIN3 ovarian cancer cells than both avidin- and no galactosamine-conjugated albumin (bovine serum)-RhodG. Sensitivity and specificity of GmSA-RhodG to detect red fluorescence labeled peritoneal cancer foci in mouse cancer model were 100%/99% (n=566), respectively for approximately 1-mm lesions and even smaller lesions were detected in vivo. These results indicate that GmSA-RhodG is not only a clinically feasible alternative but more efficient targeting reagent for D-galactose receptors than avidin-RhodG.
AuthorsYukihiro Hama, Yasuteru Urano, Yoshinori Koyama, Peter L Choyke, Hisataka Kobayashi
JournalJournal of biomedical optics (J Biomed Opt) 2007 Sep-Oct Vol. 12 Issue 5 Pg. 051501 ISSN: 1083-3668 [Print] United States
PMID17994865 (Publication Type: Journal Article, Research Support, N.I.H., Extramural, Research Support, N.I.H., Intramural)
Chemical References
  • Fluorescent Dyes
  • Receptors, Cell Surface
  • Rhodamines
  • Serum Albumin
  • galactose receptor
  • Galactosamine
Topics
  • Animals
  • Cell Line, Tumor
  • Drug Delivery Systems (methods)
  • Female
  • Fluorescent Dyes (pharmacokinetics)
  • Galactosamine (pharmacokinetics)
  • Mice
  • Mice, Nude
  • Microscopy, Fluorescence (methods)
  • Ovarian Neoplasms (metabolism, pathology, secondary)
  • Peritoneal Neoplasms (metabolism, pathology, secondary)
  • Receptors, Cell Surface (metabolism)
  • Rhodamines (pharmacokinetics)
  • Serum Albumin (pharmacokinetics)
  • Spectrometry, Fluorescence (methods)

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