Radiolabeled Peptide Probes for Liver Cancer Imaging

Liver cancer/Hepatocellular Carcinoma (HCC) is a leading cause of cancer death and represents an important cause of mortality worldwide. Several biomarkers are overexpressed in liver cancer, such as Glypican 3 (GPC3) and Epidermal Growth Factor Receptor (EGFR). These biomarkers play important roles in the progression of tumors and could serve as imaging and therapeutic targets for this disease. Peptides with adequate stability, receptor binding properties, and biokinetic behavior have been intensively studied for liver cancer imaging. A great variety of them have been radiolabeled with clinically relevant radionuclides for liver cancer diagnosis, and many are promising imaging and therapeutic candidates for clinical translation. Herein, we summarize the advancement of radiolabeled peptides for the targeted imaging of liver cancer.

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Increased serum level of epidermal growth factor receptor in liver cancer patients and its association with exposure to arsenic

The Science of The Total Environment ◽

10.1016/j.scitotenv.2012.02.079 ◽

2012 ◽

Vol 424 ◽

pp. 74-78 ◽

Cited By ~ 9

Author(s):

Tzu-I Sung ◽

Ying-Jan Wang ◽

Chi-Yi Chen ◽

Tsui-Lien Hung ◽

How-Ran Guo

Keyword(s):

Epidermal Growth Factor Receptor ◽

Growth Factor ◽

Epidermal Growth Factor ◽

Serum Level ◽

Liver Cancer ◽

Cancer Patients ◽

Growth Factor Receptor ◽

Epidermal Growth

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Epidermal growth factor receptor (EGFR) mutation testing is useful for primary lung cancer diagnosis and appropriate surgical resection: A case series

Respiratory Investigation ◽

10.1016/j.resinv.2021.08.008 ◽

2021 ◽

Author(s):

Atsushi Kitamura ◽

Kenji Ishii ◽

Kouhei Okafuji ◽

Fumitsugu Kojima ◽

Toru Bando

Keyword(s):

Lung Cancer ◽

Epidermal Growth Factor Receptor ◽

Cancer Diagnosis ◽

Egfr Mutation ◽

Primary Lung Cancer ◽

Case Series ◽

Growth Factor Receptor ◽

Lung Cancer Diagnosis ◽

Epidermal Growth ◽

Egfr Mutation Testing

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Investigation of a Pharmacological Approach for Reduction of Renal Uptake of Radiolabeled ADAPT Scaffold Protein

Molecules ◽

10.3390/molecules25194448 ◽

2020 ◽

Vol 25 (19) ◽

pp. 4448

Author(s):

Anzhelika Vorobyeva ◽

Maryam Oroujeni ◽

Sarah Lindbo ◽

Sophia Hober ◽

Tianqi Xu ◽

...

Keyword(s):

Growth Factor Receptor ◽

Scaffold Proteins ◽

High Dose ◽

Radiolabeled Peptides ◽

Renal Uptake ◽

Recent Clinical Study ◽

Clinical Strategies ◽

Sodium Maleate ◽

Epidermal Growth ◽

Prolonged Retention

Albumin binding domain-Derived Affinity ProTeins (ADAPTs) are small (5 kDa) engineered scaffold proteins that are promising targeting agents for radionuclide-based imaging. A recent clinical study has demonstrated that radiolabeled ADAPTs can efficiently visualize human epidermal growth factor receptor 2 (HER2) expression in breast cancer using SPECT imaging. However, the use of ADAPTs directly labeled with radiometals for targeted radionuclide therapy is limited by their high reabsorption and prolonged retention of activity in kidneys. In this study, we investigated whether a co-injection of lysine or gelofusin, commonly used for reduction of renal uptake of radiolabeled peptides in clinics, would reduce the renal uptake of [99mTc]Tc(CO)3-ADAPT6 in NMRI mice. In order to better understand the mechanism behind the reabsorption of [99mTc]Tc(CO)3-ADAPT6, we included several compounds that act on various parts of the reabsorption system in kidneys. Administration of gelofusine, lysine, probenecid, furosemide, mannitol, or colchicine did not change the uptake of [99mTc]Tc(CO)3-ADAPT6 in kidneys. Sodium maleate reduced the uptake of [99mTc]Tc(CO)3-ADAPT6 to ca. 25% of the uptake in the control, a high dose of fructose (50 mmol/kg) reduced the uptake by ca. two-fold. However, a lower dose (20 mmol/kg) had no effect. These results indicate that common clinical strategies are not effective for reduction of kidney uptake of [99mTc]Tc(CO)3-ADAPT6 and that other strategies for reduction of activity uptake or retention in kidneys should be investigated for ADAPT6.

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SERUM LEVEL OF EPIDERMAL GROWTH FACTOR RECEPTOR AS A BIOMARKER OF LIVER CANCER

Epidemiology ◽

10.1097/00001648-200407000-00174 ◽

2004 ◽

Vol 15 (4) ◽

pp. S71

Author(s):

How-Ran Guo ◽

Tzu-I Sung ◽

Ying-Jan Wang ◽

Tsui-Lien Hung ◽

Chi-Yi Chen

Keyword(s):

Epidermal Growth Factor Receptor ◽

Growth Factor ◽

Epidermal Growth Factor ◽

Serum Level ◽

Liver Cancer ◽

Growth Factor Receptor ◽

Epidermal Growth

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Efficient Epidermal Growth Factor Receptor Targeting Oligonucleotide as a Potential Molecule for Targeted Cancer Therapy

International Journal of Molecular Sciences ◽

10.3390/ijms20194700 ◽

2019 ◽

Vol 20 (19) ◽

pp. 4700 ◽

Cited By ~ 7

Author(s):

Tao Wang ◽

Svetlana Philippovich ◽

Jun Mao ◽

Rakesh N. Veedu

Keyword(s):

Breast Cancer ◽

Epidermal Growth Factor Receptor ◽

Growth Factor ◽

Epidermal Growth Factor ◽

Liver Cancer ◽

Growth Factor Receptor ◽

Egfr Inhibitors ◽

Egfr Inhibition ◽

Wide Range ◽

Epidermal Growth

Epidermal growth factor receptor (EGFR) is associated with the progression of a wide range of cancers including breast, glioma, lung, and liver cancer. The observation that EGFR inhibition can limit the growth of EGFR positive cancers has led to the development of various EGFR inhibitors including monoclonal antibodies and small-molecule inhibitors. However, the reported toxicity and drug resistance greatly compromised the clinical outcome of such inhibitors. As a type of chemical antibodies, nucleic acid aptamer provides an opportunity to overcome the obstacles faced by current EGFR inhibitors. In this study, we have developed and investigated the therapeutic potential of a 27mer aptamer CL-4RNV616 containing 2′-O-Methyl RNA and DNA nucleotides. Our results showed that CL-4RNV616 not only displayed enhanced stability in human serum, but also effectively recognized and inhibited the proliferation of EGFR positive Huh-7 liver cancer, MDA-MB-231 breast cancer, and U87MG glioblastoma cells, with an IC50 value of 258.9 nM, 413.7 nM, and 567.9 nM, respectively. Furthermore, TUNEL apoptosis assay revealed that CL-4RNV616 efficiently induced apoptosis of cancer cells. In addition, clinical breast cancer biopsy-based immunostaining assay demonstrated that CL-4RNV616 had a comparable detection efficacy for EGFR positive breast cancer with commonly used commercial antibodies. Based on the results, we firmly believe that CL-4RNV616 could be useful in the development of targeted cancer therapeutics and diagnostics.

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