Labeling of monoclonal antibodies with radionuclides

Kuldeep K. Bhargava, Seetharama A. Acharya

Research output: Contribution to journalArticle

28 Citations (Scopus)

Abstract

Antibodies, specifically monoclonal antibodies, are potentially very useful and powerful carriers of therapeutic agents to target tissues and diagnostic agents. The loading or charging of antibodies with agents, especially radiotracers, is reviewed here. The choice of radiosotope for immunodetection and/or immunotherapy is based on its availability, half-life, nature of the radiation emitted, and the metabolic pathways of the radionuclide in the body. Most important of all are the derivatization techniques available for labeling the antibody with the given radionuclide. Isotopes of iodine and divalent metal ions are the most, commonly used radionuclides. Antibodies labeled with iodine at tyrosine residues are metabolized rapidly in vivo. This leads to the incorporation of metabolized radioactive iodine into various tissues, mainly the thyroid gland and stomach, and to the accumulation of high levels of circulating iodine in the blood, which masks tumor uptake considerably. To overcome these limitations, the use of iodohippurate as an iodine-anchoring molecule, to the protein should be considered. When divalent or multivalent metal ions are used as the preferred, radionuclide, bifunctional chelating reagents such as ethylenediaminetetraacetic acid (EDTA) or diethylenetriaminepentaacetic acid (DTPA) are first coupled to the protein or antibody. These chelating molecules are attached to the protein by formation of an isopeptide linkage between the carboxylate of the chelating reagent and the amino group of the protein. Several procedures are available to generate the isopeptide linkage. When the anchoring of the chelating agent through isopeptide linkage results in the inactivation of the antibody, periodate oxidation of the carbohydrate moiety of the antibody, followed by reductive coupling of chelator, could be considered as an alternative. There is still a need for better, simpler, and more direct methods for labeling antibodies with radionuclides.

Original languageEnglish (US)
Pages (from-to)187-201
Number of pages15
JournalSeminars in Nuclear Medicine
Volume19
Issue number3
DOIs
StatePublished - 1989

Fingerprint

Radioisotopes
Monoclonal Antibodies
Antibodies
Iodine
Chelating Agents
Iodine Isotopes
Proteins
Metals
Ions
Cross-Linking Reagents
Masks
Metabolic Networks and Pathways
Edetic Acid
Immunotherapy
Half-Life
Tyrosine
Stomach
Thyroid Gland
Carbohydrates
Radiation

ASJC Scopus subject areas

  • Radiology Nuclear Medicine and imaging
  • Radiological and Ultrasound Technology

Cite this

Labeling of monoclonal antibodies with radionuclides. / Bhargava, Kuldeep K.; Acharya, Seetharama A.

In: Seminars in Nuclear Medicine, Vol. 19, No. 3, 1989, p. 187-201.

Research output: Contribution to journalArticle

Bhargava, Kuldeep K. ; Acharya, Seetharama A. / Labeling of monoclonal antibodies with radionuclides. In: Seminars in Nuclear Medicine. 1989 ; Vol. 19, No. 3. pp. 187-201.
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