Thiolation of proteins for radionuclide-based radioimmunodetecti

Drug – bio-affecting and body treating compositions – Radionuclide or intended radionuclide containing; adjuvant... – In an organic compound

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424 111, 424 165, 424 91, 424 149, 4241301, 5303871, A61K 5100, A61M 3614

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active

060106808

ABSTRACT:
A method of radiolabeling a protein with a radionuclide including contacting the protein with a protected tertiary thiol-containing bifunctional chelating agent that is capable of reacting with the protein at one end of the agent and is capable of complexing with a radionuclide at the other end of the agent, to form a protein-acetyl-t-thiol-containing conjugate. The protein-acetyl-t-thiol-containing conjugate then is deprotected and admixed with a reducing agent for the radionuclide, where the radionuclide is added in a subsequent step, to form a mixture of reducing agent and protein-t-thiol-containing conjugate. This mixture then is reacted with a radionuclide whereby the radionuclide reacts with pendant sulfhydryl groups present on the protein-t-thiol-containing conjugate. Methods of radioimmunotherapy and diagnostic kits suitable for forming a composition to be administered to a human patient also are disclosed.

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