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Author Notes:

Franklin C. Wong: fwong@mdanderson.org

The authors acknowledge the logistic support of gamma rays irradiation from Raymond Meyn, Ph.D., of the Division of Radiation Oncology, University of Texas MD Anderson Cancer Center.

None of the authors has any financial interest with any commercial vendor or supplier of material for the conduct of experiments and presentation of work related to this study.


Research Funding:

The report work was partially supported by a research Grant RR00165 from the National Institutes of Health to Dr. Michael Kuhar.


  • Science & Technology
  • Life Sciences & Biomedicine
  • Biotechnology & Applied Microbiology
  • Medicine, Research & Experimental
  • Research & Experimental Medicine
  • H-3 PK 14105
  • PET

Affinity Labeling of Membrane Receptors Using Tissue-Penetrating Radiations


Journal Title:

BioMed Research International


Volume 2013


, Pages 503095-503095

Type of Work:

Article | Final Publisher PDF


Photoaffinity labeling, a useful in vivo biochemical tool, is limited when applied in vivo because of the poor tissue penetration by ultraviolet (UV) photons. This study investigates affinity labeling using tissue-penetrating radiation to overcome the tissue attenuation and irreversibly label membrane receptor proteins. Using X-ray (115 kVp) at low doses ( < 50 cGy or Rad), specific and irreversible binding was found on striatal dopamine transporters with 3 photoaffinity ligands for dopamine transporters, to different extents. Upon X-ray exposure (115 kVp), RTI-38 and RTI-78 ligands showed irreversible and specific binding to the dopamine transporter similar to those seen with UV exposure under other conditions. Similar ly, gamma rays at higher energy (662 keV) also affect irreversible binding of photoreactive ligands to peripheral benzodiazepine receptors (by PK14105) and to the dopamine (D2) membrane receptors (by azidoclebopride), respectively. This study reports that X-ray and gamma rays induced affinity labeling of membrane receptors in a manner similar to UV with photoreactive ligands of the dopamine transporter, D2 dopamine receptor (D2R), and peripheral benzodiazepine receptor (PBDZR). It may provide specific noninvasive irreversible block or stimulation of a receptor using tissue-penetrating radiation targeting selected anatomic sites.

Copyright information:

© 2013 Franklin C. Wong et al.

This is an Open Access work distributed under the terms of the Creative Commons Attribution 3.0 Unported License (http://creativecommons.org/licenses/by/3.0/).

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