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Synthesis, radiosynthesis, and metabolism of 131I-Y-c(CGRRAGGSC).

Synthesis, radiosynthesis, and metabolism of 131I-Y-c(CGRRAGGSC).
Author Information (click to view)

Xie J, Pan D, Lu M, Chen X, Chen Y, Zhang T, Xie Y, Zhou H, Liu L, Yang M, Wang J, Chen D,


Xie J, Pan D, Lu M, Chen X, Chen Y, Zhang T, Xie Y, Zhou H, Liu L, Yang M, Wang J, Chen D, (click to view)

Xie J, Pan D, Lu M, Chen X, Chen Y, Zhang T, Xie Y, Zhou H, Liu L, Yang M, Wang J, Chen D,

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Anti-cancer agents in medicinal chemistry 2017 07 13() doi 10.2174/1871520617666170713151647

Abstract
BACKGROUND
The formation of the complex interleukin-11(IL-11) and IL-11 receptor (IL-11R) is closely related with tumor progression. Binding of IL-11 to the IL-11 receptor α-chain (IL-11Rα) has been suggested as a target for human cancer. The cyclic peptide c(CGRRAGGSC) is a mimic of IL-11.

OBJECTIVE
To explore 131I-Y-c(CGRRAGGSC) synthesis and radiosynthesis, and metabolism in SKOV3 tumor-bearing mice.

METHOD
In this study, 131I labeled c(CGRRAGGSC) was designed and characterized. For radiolabeling, tyrosine was used as a linker to connect c(CGRRAGGSC) and 131I. Balb/c nude mice bearing SKOV3 human ovarian carcinoma were used for in vivo studies. Uptake of 131I-cyclic nonapeptide by the tumor was visualized by single photon emission computerized tomography (SPECT).

RESULTS
The entire labeling process, which took 15 min by chloramine-T method, resulted in a high labeling yield (93.03±6.78%), and high radiochemical purity (RCP) (>95%). SPECT imaging showed that accumulation of the probe in the tumor was close to background levels. In addition, biodistribution studies showed that the accumulation of 131I-Y-c(CGRRAGGSC) in normal mice was similar to that of Na131I.

CONCLUSION
Tyrosine is a suitable chelating agent for the use of radioiodine labeling, however the bioactivity of the conjugate needs further investigation.

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