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

Research output: Contribution to journalArticlepeer-review

23 Citations (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.

Original languageEnglish
Pages (from-to)1385-1391
Number of pages7
JournalInternational Journal of Nanomedicine
Publication statusPublished - Apr 9 2013


  • Biomarker
  • Gastric cancer
  • Glucose-regulated protein 78
  • Micelles
  • Nuclear imaging

ASJC Scopus subject areas

  • Biophysics
  • Bioengineering
  • Biomaterials
  • Organic Chemistry
  • Drug Discovery


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