Title |
Novel targeted nuclear imaging agent for gastric cancer diagnosis: glucose-regulated protein 78 binding peptide-guided 111In-labeled polymeric micelles
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Published in |
International Journal of Nanomedicine, April 2013
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DOI | 10.2147/ijn.s42003 |
Pubmed ID | |
Authors |
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 |
Abstract |
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(ɛ-caprolactone) and then mixed with diethylenetriaminepentaacetic acid (DTPA)-linked poly(ethylene glycol)-poly(ɛ-caprolactone) to form DTPA/GRP78BP-conjugated micelles. The coupling efficiency of micelles with radioisotope indium-111 ((111)In) was measured and analyzed by instant thin layer chromatography. The coupling efficiency of DTPA-conjugated micelles and DTPA/GRP78BP-conjugated micelles with (111)In was 85% and 93%, respectively. For characterization and trace imaging, the radioisotope (111)In-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 (111)In-labeled micelles was statistically higher than that in animals administered with (111)In-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. |
X Demographics
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Unknown | 5 | 100% |
Demographic breakdown
Type | Count | As % |
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Members of the public | 4 | 80% |
Practitioners (doctors, other healthcare professionals) | 1 | 20% |
Mendeley readers
Geographical breakdown
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Unknown | 23 | 100% |
Demographic breakdown
Readers by professional status | Count | As % |
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Student > Ph. D. Student | 7 | 30% |
Student > Bachelor | 4 | 17% |
Other | 2 | 9% |
Researcher | 2 | 9% |
Student > Master | 2 | 9% |
Other | 2 | 9% |
Unknown | 4 | 17% |
Readers by discipline | Count | As % |
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Agricultural and Biological Sciences | 4 | 17% |
Medicine and Dentistry | 3 | 13% |
Pharmacology, Toxicology and Pharmaceutical Science | 2 | 9% |
Materials Science | 2 | 9% |
Business, Management and Accounting | 1 | 4% |
Other | 3 | 13% |
Unknown | 8 | 35% |