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.
申请公布号
EP2231201(A1)
申请公布日期
2010.09.29
申请号
EP20080865548
申请日期
2008.12.12
申请人
GENERAL ELECTRIC COMPANY;HAMMERSMITH IMANET, LTD
发明人
PADILLA DE JESUS, OMAYRA LIZ;KOVACS, ERNEST WILLIAM;GLASER, MATTHIAS EBERHARD;ARSTAD, ERIK;SYUD, FAISAL AHMED