C - Chemistry – Metallurgy – 07 – B
Patent
C - Chemistry, Metallurgy
07
B
C07B 59/00 (2006.01) A61K 51/08 (2006.01) A61K 51/10 (2006.01) C07K 1/107 (2006.01) C07K 1/13 (2006.01) C07K 16/30 (2006.01) C07K 16/46 (2006.01)
Patent
CA 2302360
Thiol-containing peptides can be radiolabeled with fluorine-18 (F-18) by reacting a peptide comprising a free thiol group with an F-18-bound labeling reagent which also has a group that is reactive with thiols. The resulting F-18-labeled peptides may be targeted to a tissue of interest using bispecific antibodies or bispecific antibody fragments having on arm specific for the F-18-labeled peptide or a low molecular weight hapten conjugated to the F-18-labeled peptide, and another arm specific to the targeted tissue. The targeted tissue is subsequently visualized by clinincal positron emission tomography. The method for radiolabeling thiol-containing peptides with fluorine-18(F-18), comprises reacting a peptide comprising a free thiol group with a labelling reagent having the general formula 18F-(CH2)m-CR1,R2-(CH2)n-X, wherein: n is 0, 1 or 2; m is 0, 1 or 2; and n+m is 0, 1, or 2; X is selected from the group consisting of hydroxyl, cyano, iodide, bromide, chloride, azide, tosylate, mesylate, nosylate, triflate, unsubstituted maleimide, maleimide substituted with one or two alkyl groups, and 3-sulfo-maleimide; and R1 and R2 are the same or different and are selected from the group consisting of iodide, bromide, chloride, azide, tosylate, mesylate, nosylate, triflate, hydrogen, -CONH2, carboxyl, hydroxyl, sulfonic acid, tertiary amine, quaternary ammonium, unsubstituted maleimide, maleimide substituted with on or two alkyl groups, 3-sulfo-maleimide, unsubstituted alkyl, substituted alkyl, -COOR',-CONR'2, or COR', wherein the substituents of the substituted alkyl groups are selected from the group consisting of -CONH2, carboxyl, hydroxyl, sulfonic acid, tertiary amine and quaternary ammonium and wherein R' is a C1-C6 alkyl or phenyl.
Selon l'invention, on peut radiomarquer des peptides contenant thiol avec du fluor-18 (F-18), en faisant réagir un peptide comprenant un groupe thiol libre avec un réactif de marquage fixé sur F-18, lequel possède également un groupe qui réagit avec les thiols. Les peptides résultants ainsi marqués au F-18 peuvent être ciblés sur un tissu d'intérêt au moyen d'anticorps à double spécificité ou de fragments de ces anticorps possédant un bras spécifique du peptide marqué au F-18 ou un haptène à bas poids moléculaire conjugué au peptide marqué au F-18, ainsi qu'un autre bras spécifique du tissu ciblé. Le tissu ciblé est ensuite visualisé au moyen d'une tomographie clinique par émission de positrons.
Immunomedics Inc.
Smart & Biggar
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