Novel targeted nuclear imaging agent for gastric cancer diagnosis: Glucose-regulated protein 78 binding peptide-guided 111In-labeled polymeric micelles

Chun Chia Cheng, Chiung Fang Huang, Ai Sheng Ho, Cheng Liang Peng, Chun Chao Chang, Fu Der Mai, Ling Yun Chen, Tsai Yueh Luo, Jungshan Chang

研究成果: 雜誌貢獻文章同行評審

24 引文 斯高帕斯(Scopus)


Increased expression of cellular membrane bound glucose-regulated protein 78 (GRP78) is considered to be one of the biomarkers for gastric cancers. Therefore, peptides or molecules with specific recognition to GRP78 can act as a guiding probe to direct conjugated imaging agents to localized cancers. Based on this rationale, GRP78-guided polymeric micelles were designed and manufactured for nuclear imaging detection of tumors. Thiolated GRP78 binding peptide (GRP78BP) was first labeled with maleimide-terminated poly(ethylene glycol)-poly(ε-caprolactone) and then mixed with diethylenetriaminepentaacetic acid (DTPA)-linked poly(ethylene glycol)-poly(ε-caprolactone) to form DTPA/GRP78BP-conjugated micelles. The coupling efficiency of micelles with radioisotope indium-111 (111In) was measured and analyzed by instant thin layer chromatography. The coupling efficiency of DTPA-conjugated micelles and DTPA/GRP78BP-conjugated micelles with 111In was 85% and 93%, respectively. For characterization and trace imaging, the radioisotope 111In-targeting tumors were detected and imaged in a xenograft murine model using nano single photon emission computed tomography/computed tomography. The results revealed that the radioactive intensity measured in the animals administered with GRP78BP-guided 111In-labeled micelles was statistically higher than that in animals administered with 111In-labeled micelles, demonstrating that GRP78BP more than doubled the accumulation of micelles to the tumor tissue (P <0.05). The results indicate that the gastric cancer biomarker GRP78 is a probing target in the application of nuclear imaging for tumor diagnosis. This novel GRP78BP-guided micelle agent may be applied in clinical practice to complement the histological diagnosis.

頁(從 - 到)1385-1391
期刊International Journal of Nanomedicine
出版狀態已發佈 - 四月 9 2013

ASJC Scopus subject areas

  • 生物物理學
  • 生物工程
  • 生物材料
  • 有機化學
  • 藥物發現


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