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:
- Issue Date:
- Research Org.:
- Univ. of Missouri, Columbia, MO (United States)
- Sponsoring Org.:
- USDOE
- OSTI Identifier:
- 1174992
- Patent Number(s):
- 6780397
- Application Number:
- 09/386,657
- Assignee:
- University Of Missouri
- Patent Classifications (CPCs):
-
A - HUMAN NECESSITIES A61 - MEDICAL OR VETERINARY SCIENCE A61K - PREPARATIONS FOR MEDICAL, DENTAL, OR TOILET PURPOSES
- 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. 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 = {2004},
month = {8}
}
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