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Title: Biomolecule conjugation strategy using novel water-soluble phosphine-based chelating agents

Abstract

This invention describes a novel strategy to produce phosphine-functionalized biomolecules (e.g. peptides or proteins) for potential use in the design and development of site-specific radiopharmaceuticals for diagnosis or therapy of specific cancers. Hydrophilic alkyl phosphines, in general, tend to be oxidatively unstable. Therefore, incorporation of such phosphine functionalities on peptide (and other biomolecule) backbones, without oxidizing the P.sup.III centers, is difficult. In this context this discovery reports on a new technology by which phosphines, in the form of bifunctional chelating agents, can be directly incorporated on biomolecular backbones using manual synthetic or solid phase peptide synthesis methodologies. The superior ligating abilities of phosphine ligands, with various diagnostically (e.g. TC-99m) or therapeutically (e.g. Re186/188, Rh-105, Au-199) useful radiometals, coupled with the findings that the resulting complexes demonstrate high in vivo stability makes this approach useful in the development of radiolabeled biomolecules for applications in the design of tumor-specific radiopharmaceuticals.

Inventors:
; ;
Publication Date:
Research Org.:
Univ. of Missouri, Columbia, MO (United States)
Sponsoring Org.:
USDOE
OSTI Identifier:
1174992
Patent Number(s):
6,780,397
Application Number:
09/386,657
Assignee:
University Of Missouri OSTI
DOE Contract Number:
FG0289ER60875
Resource Type:
Patent
Country of Publication:
United States
Language:
English
Subject:
59 BASIC BIOLOGICAL SCIENCES

Citation Formats

Katti, Kattesh V., Gali, Hariprasad, and Volkert, Wynn A. Biomolecule conjugation strategy using novel water-soluble phosphine-based chelating agents. United States: N. p., 2004. Web.
Katti, Kattesh V., Gali, Hariprasad, & Volkert, Wynn A. Biomolecule conjugation strategy using novel water-soluble phosphine-based chelating agents. United States.
Katti, Kattesh V., Gali, Hariprasad, and Volkert, Wynn A. Tue . "Biomolecule conjugation strategy using novel water-soluble phosphine-based chelating agents". United States. doi:. https://www.osti.gov/servlets/purl/1174992.
@article{osti_1174992,
title = {Biomolecule conjugation strategy using novel water-soluble phosphine-based chelating agents},
author = {Katti, Kattesh V. and Gali, Hariprasad and Volkert, Wynn A.},
abstractNote = {This invention describes a novel strategy to produce phosphine-functionalized biomolecules (e.g. peptides or proteins) for potential use in the design and development of site-specific radiopharmaceuticals for diagnosis or therapy of specific cancers. Hydrophilic alkyl phosphines, in general, tend to be oxidatively unstable. Therefore, incorporation of such phosphine functionalities on peptide (and other biomolecule) backbones, without oxidizing the P.sup.III centers, is difficult. In this context this discovery reports on a new technology by which phosphines, in the form of bifunctional chelating agents, can be directly incorporated on biomolecular backbones using manual synthetic or solid phase peptide synthesis methodologies. The superior ligating abilities of phosphine ligands, with various diagnostically (e.g. TC-99m) or therapeutically (e.g. Re186/188, Rh-105, Au-199) useful radiometals, coupled with the findings that the resulting complexes demonstrate high in vivo stability makes this approach useful in the development of radiolabeled biomolecules for applications in the design of tumor-specific radiopharmaceuticals.},
doi = {},
journal = {},
number = ,
volume = ,
place = {United States},
year = {Tue Aug 24 00:00:00 EDT 2004},
month = {Tue Aug 24 00:00:00 EDT 2004}
}

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