Radiolocalization of squamous lung carcinoma with 131I-labeled epidermal growth factor

The human epidermal growth factor receptor (HER) family of receptor tyrosine kinases controls critical pathways involved in epithelial cell differentiation, growth, division, and motility. Alterations and disruptions in the function of the HER-kinase axis can lead to malignancy. Many therapeutic agents targeting the HER-kinase axis are approved for clinical use or are in preclinical/clinical development. The ability to quantitatively image the HER-kinase axis in a noninvasive manner can aid in lesion detection, patient stratification, new drug development/validation, dose optimization, and treatment monitoring. This review summarizes the current status in multimodality imaging of the HER-kinase axis using PET, SPECT, optical, and MR imaging. The targeting ligands used include small-molecule tyrosine kinase inhibitors, peptides, proteins, antibodies, and engineered antibody fragments. EGFR and HER2 imaging have been well documented in the past, and imaging of HER3, HER4, HER heterodimers, and HER-kinase mutants deserves significant research effort in the future. Successful development of new HER-kinase-targeted imaging agents with optimal in vivo stability, targeting efficacy, and desirable pharmacokinetics for clinical translation will enable maximum benefit in cancer patient management.

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Multimodality imaging of the HER-kinase axis in cancer

Cai

Niu

Chen

2007

Eur J Nucl Med Mol Imaging

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Protein-based tumor molecular imaging probes

2010

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Molecular imaging is an emerging discipline which plays critical roles in diagnosis and therapeutics. It visualizes and quantifies markers that are aberrantly expressed during the disease origin and development. Protein molecules remain to be one major class of imaging probes, and the option has been widely diversified due to the recent advances in protein engineering techniques. Antibodies are part of the immunosystem which interact with target antigens with high specificity and affinity. They have long been investigated as imaging probes and were coupled with imaging motifs such as radioisotopes for that purpose. However, the relatively large size of antibodies leads to a half-life that is too long for common imaging purposes. Besides, it may also cause a poor tissue penetration rate and thus compromise some medical applications. It is under this context that various engineered protein probes, essentially antibody fragments, protein scaffolds, and natural ligands have been developed. Compared to intact antibodies, they possess more compact size, shorter clearance time, and better tumor penetration. One major challenge of using protein probes in molecular imaging is the affected biological activity resulted from random labeling. Site-specific modification, however, allows conjugation happening in a stoichiometric fashion with little perturbation of protein activity. The present review will discuss protein-based probes with focus on their application and related site-specific conjugation strategies in tumor imaging.

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Planning for Intracavitary Anti-EGFR Radionuclide Therapy of Gliomas. Literature Review and Data on EGFR Expression

et al. 2005

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Targeting with radionuclide labelled substances that bind specifically to the epidermal growth factor receptor, EGFR, is considered for intracavitary therapy of EGFR-positive glioblastoma multiforme, GBM. Relevant literature is reviewed and examples of EGFR expression in GBM are given. The therapeutical efforts made so far using intracavitary anti-tenascin radionuclide therapy of GBM have given limited effects, probably due to low radiation doses to the migrating glioma cells in the brain. Low radiation doses might be due to limited penetration of the targeting agents or heterogeneity in the expression of the target structure. In this article we focus on the possibilities to target EGFR on the tumour cells instead of an extracellular matrix component. There seems to be a lack of knowledge on the degree of intratumoral variation of EGFR expression in GBM, although the expression seemed rather homogeneous over large areas in most of the examples (n=16) presented from our laboratory. The observed homogeneity was surprising considering the genomic instability and heterogeneity that generally characterises highly malignant tumours. However, overexpression of EGFR is, at least in primary GBMs, one of the steps in the development of malignancy, and tumour cells that lose or downregulate EGFR will probably be outgrown in an expanding tumour cell population. Thus, loss of EGFR expression might not be the critical factor for successful intracavitary radionuclide therapy. Instead, it is likely that the penetration properties of the targeting agents are critical, and detailed studies on this are urgent.

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Radiolocalization of squamous lung carcinoma with 131I-labeled epidermal growth factor

Cited by 10 publications

References 22 publications

Multimodality imaging of the HER-kinase axis in cancer

Multimodality imaging of the HER-kinase axis in cancer

Protein-based tumor molecular imaging probes

Planning for Intracavitary Anti-EGFR Radionuclide Therapy of Gliomas. Literature Review and Data on EGFR Expression

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