-transparent.png){kind=logo}
We have developed a suitable radiolabeling method for our new type of glycoprotein-liposome conjugate (GCL), in order to investigate its potential utility as a drug carrier that can target the cellular functions of carbohydrate-binding proteins. In order to obtain radiolabeled GCL with high labeling efficiency, we introduced p-hydroxyphenylpropyl groups into the liposome membrane through the amine moiety of a constitutive phospholipid, dipalmitoylphosphatidylethanolamine (DPPE) by using Bolton-Hunter reagent (BHR). Radioiodination of the introduced tyrosyl groups was performed by the Chloramine-T method. The labeling efficiency of the BHR-treated liposome conjugate was high in comparison with that of the BHR-untreated liposome conjugate. An in vitro inhibition study showed that the binding affinity of 125I-labeled BHR-treated GCL (125I-F3S-BH) with lectin was twice as high as that of untreated conjugate (125I-F3S). The biodistribution of 125I-F3S-BH in mice was considerably different from that of 125I-F3S. 125I-F3S-BH was more rapidly taken up by the liver and was more rapidly excreted from the liver than 125I-F3S. Moreover, 125I-F3S-BH accumulated more rapidly into the kidneys, which resulted a lower radioactivity in the blood circulation at an earlier time point than in the case of 125I-F3S. The characteristics of tumor accumulation of 125I-F3S-BH and 125I-F3S were similar to those in blood. If F3S is to be employed as an in vivo targeting ligand in biodistribution studies, BHR would be a suitable tool for radiolabeling because it allows GCL to retain the biological activity and characteristics of the unmodified conjugate.
N Shimura, and
Y Sogawa, and
Y Kawakita, and
M Ikekita, and
N Yamazaki, and
S Kojima
January 2011,
Applied radiation and isotopes : including data, instrumentation and methods for use in agriculture, industry and medicine,
N Shimura, and
Y Sogawa, and
Y Kawakita, and
M Ikekita, and
N Yamazaki, and
S Kojima
October 1980,
Biochemical and biophysical research communications,
N Shimura, and
Y Sogawa, and
Y Kawakita, and
M Ikekita, and
N Yamazaki, and
S Kojima
January 1980,
Methods in enzymology,
N Shimura, and
Y Sogawa, and
Y Kawakita, and
M Ikekita, and
N Yamazaki, and
S Kojima
December 1980,
Clinical chemistry,
N Shimura, and
Y Sogawa, and
Y Kawakita, and
M Ikekita, and
N Yamazaki, and
S Kojima
August 1981,
Analytical biochemistry,
N Shimura, and
Y Sogawa, and
Y Kawakita, and
M Ikekita, and
N Yamazaki, and
S Kojima
December 1978,
Analytical biochemistry,
N Shimura, and
Y Sogawa, and
Y Kawakita, and
M Ikekita, and
N Yamazaki, and
S Kojima
January 1996,
Biochemical and biophysical research communications,
N Shimura, and
Y Sogawa, and
Y Kawakita, and
M Ikekita, and
N Yamazaki, and
S Kojima
January 2011,
Journal of microencapsulation,
N Shimura, and
Y Sogawa, and
Y Kawakita, and
M Ikekita, and
N Yamazaki, and
S Kojima
March 1983,
Annals of clinical biochemistry,
N Shimura, and
Y Sogawa, and
Y Kawakita, and
M Ikekita, and
N Yamazaki, and
S Kojima
February 1994,
Cancer,
