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Title: Bifunctional chelating agent for the design and development of site specific radiopharmaceuticals and biomolecule conjugation strategy

Abstract

There is provided a method of labeling a biomolecule with a transition metal or radiometal in a site specific manner to produce a diagnostic or therapeutic pharmaceutical compound by synthesizing a P.sub.2 N.sub.2 -bifunctional chelating agent intermediate, complexing the intermediate with a radio metal or a transition metal, and covalently linking the resulting metal-complexed bifunctional chelating agent with a biomolecule in a site specific manner. Also provided is a method of synthesizing the --PR.sub.2 containing biomolecules by synthesizing a P.sub.2 N.sub.2 -bifunctional chelating agent intermediate, complexing the intermediate with a radiometal or a transition metal, and covalently linking the resulting radio metal-complexed bifunctional chelating agent with a biomolecule in a site specific manner. There is provided a therapeutic or diagnostic agent comprising a --PR.sub.2 containing biomolecule.

Inventors:
; ; ; ;
Issue Date:
Research Org.:
The Curators of the University of Missouri, Columbia, MO, (United States)
Sponsoring Org.:
USDOE
OSTI Identifier:
1174538
Patent Number(s):
6635235
Application Number:
09/602,487
Assignee:
The Curators of the University of Missouri (Columbia, MO)
Patent Classifications (CPCs):
A - HUMAN NECESSITIES A61 - MEDICAL OR VETERINARY SCIENCE A61K - PREPARATIONS FOR MEDICAL, DENTAL, OR TOILET PURPOSES
DOE Contract Number:  
FG02-89ER60875
Resource Type:
Patent
Country of Publication:
United States
Language:
English
Subject:
37 INORGANIC, ORGANIC, PHYSICAL, AND ANALYTICAL CHEMISTRY

Citation Formats

Katti, Kattesh V., Prabhu, Kandikere R., Gali, Hariprasad, Pillarsetty, Nagavara Kishore, and Volkert, Wynn A. Bifunctional chelating agent for the design and development of site specific radiopharmaceuticals and biomolecule conjugation strategy. United States: N. p., 2003. Web.
Katti, Kattesh V., Prabhu, Kandikere R., Gali, Hariprasad, Pillarsetty, Nagavara Kishore, & Volkert, Wynn A. Bifunctional chelating agent for the design and development of site specific radiopharmaceuticals and biomolecule conjugation strategy. United States.
Katti, Kattesh V., Prabhu, Kandikere R., Gali, Hariprasad, Pillarsetty, Nagavara Kishore, and Volkert, Wynn A. Tue . "Bifunctional chelating agent for the design and development of site specific radiopharmaceuticals and biomolecule conjugation strategy". United States. https://www.osti.gov/servlets/purl/1174538.
@article{osti_1174538,
title = {Bifunctional chelating agent for the design and development of site specific radiopharmaceuticals and biomolecule conjugation strategy},
author = {Katti, Kattesh V. and Prabhu, Kandikere R. and Gali, Hariprasad and Pillarsetty, Nagavara Kishore and Volkert, Wynn A.},
abstractNote = {There is provided a method of labeling a biomolecule with a transition metal or radiometal in a site specific manner to produce a diagnostic or therapeutic pharmaceutical compound by synthesizing a P.sub.2 N.sub.2 -bifunctional chelating agent intermediate, complexing the intermediate with a radio metal or a transition metal, and covalently linking the resulting metal-complexed bifunctional chelating agent with a biomolecule in a site specific manner. Also provided is a method of synthesizing the --PR.sub.2 containing biomolecules by synthesizing a P.sub.2 N.sub.2 -bifunctional chelating agent intermediate, complexing the intermediate with a radiometal or a transition metal, and covalently linking the resulting radio metal-complexed bifunctional chelating agent with a biomolecule in a site specific manner. There is provided a therapeutic or diagnostic agent comprising a --PR.sub.2 containing biomolecule.},
doi = {},
journal = {},
number = ,
volume = ,
place = {United States},
year = {Tue Oct 21 00:00:00 EDT 2003},
month = {Tue Oct 21 00:00:00 EDT 2003}
}

Works referenced in this record:

99m Tc Labeling of Highly Potent Small Peptides
journal, September 1997


In vitro and in vivo characterization of novel water-soluble dithio-bisphosphine 99mTc complexes
journal, October 1997


Synthesis of Phosphine−Rhodium Complexes Attached to a Standard Peptide Synthesis Resin
journal, January 1996


Versatile Building Block for the Synthesis of Phosphine-Containing Peptides: The Sulfide of Diphenylphosphinoserine
journal, May 1994


Syntheses and Characterization of Chemically Flexible, Water-Soluble Dithio−Bis(phosphine) Compounds:  (HOH 2 C) 2 P(CH 2 ) 2 S(CH 2 ) 3 S(CH 2 ) 2 P(CH 2 OH) 2 , (HOH 2 C) 2 PCH 2 CH 2 S(CH 2 ) 4 SCH 2 CH 2 P(CH 2 OH) 2 , and (HOH 2 C) 2 PCH 2 CH 2 CH 2 S(CH 2 ) 3 SCH 2 CH 2 CH 2 P(CH 2 OH) 2 . Systematic Investigation of the Effect of Chain Length on the Coordination Chemistry of Rhenium(V). X-ray Crystal Structures of [ReO 2 (HOH 2 C) 2 P(CH 2 ) 2 S(CH 2 ) 3 S(CH 2 ) 2 P(CH 2 OH) 2 ] 2 (Cl) 2 , [ReO 2 (HOH 2 C) 2 P(CH 2 ) 2 S(CH 2 ) 4 S(CH 2 ) 2 P-(CH 2 OH) 2 ] 2 (ReO 4 - ) 2 , and [ReO 2 (HOH 2 C) 2 P(CH 2 ) 3 S(CH 2 ) 3 S(CH 2 ) 3 P(CH 2 OH) 2 ](Cl)
journal, August 1997