Selective radiolabeling of biomolecules

US8071718B2 · kind B2 · utility

Assignee

• General Electric Company · US

Inventors

• Omayra Liz Padilla De Jesus · Clifton Park, US
• Ernest William Kovacs · Albany, US
• Matthias Eberhard Glaser · Norton, GB
• Erik Arstad · London, GB
• Faisal Ahmed Syud · Clifton Park, US

Key dates

• Filing date: Dec 20, 2007
• Grant date: Dec 6, 2011
• Expiry date: Feb 21, 2030

Classification

• Technology area (CPC A): Human Necessities
• CPC primary: A61K51/1051
• WIPO field: Pharmaceuticals
• WIPO sector: Chemistry

Abstract

Provided herein are methods for introducing fluorine atom onto a biomolecule comprising: (i) providing a linker comprising a thiol-reactive terminus and an azido/alkyne-reactive terminus; (ii) reacting the thiol-reactive terminus of the linker with a biomolecule comprising at least one thiol group or a reactive derivative thereof; and (iii) subsequently reacting the azido/alkyne-reactive terminus of the linker with a fluorine-substituted azide or alkyne respectively. Also provided are compositions and method of synthesis of bifunctional linkers and bioconjugates as well as radio-diagnostic agents comprising fluorine-labeled biomolecules.