Imaging agents for imaging protease activity and uses thereof
AssigneeThe United States of America, as represented by the Secretary, Department of Health and Human Services
InventorsXiaoyuan Chen, Seulki Lee, Lei Zhu
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Abstract
Disclosed are imaging agents having the following Formula I: wherein F is a near infrared fluorophore, S is an enzymatically cleavable oligopeptide, Q is a fluorescence quencher molecule, and M is a moiety selected from the group consisting of PEG or derivative thereof and a targeting ligand, and wherein F, Q and M are linked to separate amino acids of the enzymatically cleavable oligopeptide. Compositions comprising such compounds, as well as methods of use, methods of identifying a cell or a population of cells in vivo expressing a protease of interest, and methods of treating a disease through imaging are also disclosed.
Claims12
An imaging agent of formula I:
- wherein:
- F is a near infrared fluorophore selected from the group consisting of fluorescein isothiocyanate (FITC, green), cyanine dyes Cy2, Cy3, Cy3.5, Cy5, Cy5.5, Cy7, Cy7.5, Texas Red, and IRDye800CW;
- S is an oligopeptide consisting only of Gly-Pro-Leu-Gly-Val-Arg-Gly-Lys (SEQ ID NO:
- 3), wherein the oligopeptide does not contain any additional amino acids;
- Q is a fluorescence quencher molecule selected from the group consisting of DABCYL, DABSYL, Black Hole Quencher-1 (BHQ-1), Black Hole Quencher-2 (BHQ-2), Black Hole Quencher-3 (BHQ-3), Blackberry Quencher 650, QSY-7, QSY-9, and QSY-21;
- and
- M is polyethylene glycol having a molecular weight of 104 Daltons to 588 Daltons,
- and wherein F, Q and M are linked to separate amino acids of the oligopeptide.
An imaging agent of formula I:
- wherein:
- F is a near infrared fluorophore selected from the group consisting of fluorescein isothiocyanate (FITC, green), cyanine dyes Cy2, Cy3, Cy3.5, Cy5, Cy5.5, Cy7, Cy7.5, Texas Red, and IRDye800CW;
- S is an oligopeptide consisting only of Leu-Pro-Lys-Gly-Leu (SEQ ID NO:
- 7), wherein the oligopeptide does not contain any additional amino acids;
- Q is a fluorescence quencher molecule selected from the group consisting of DABCYL, DABSYL, Black Hole Quencher-1 (BHQ-1), Black Hole Quencher-2 (BHQ-2), Black Hole Quencher-3 (BHQ-3), Blackberry Quencher 650, QSY-7, QSY-9, and QSY-21;
- and
- M is polyethylene glycol having a molecular weight of 104 Daltons to 588 Daltons,
- and wherein F, Q and M are linked to separate amino acids of the oligopeptide.
An imaging agent of formula I:
- wherein:
- F is a near infrared fluorophore selected from the group consisting of fluorescein isothiocyanate (FITC, green), cyanine dyes Cy2, Cy3, Cy3.5, Cy5, Cy5.5, Cy7, Cy7.5, Texas Red, and IRDye800CW;
- S is an oligopeptide consisting only of Arg-Pro-Lys-Pro-Val-Glu (SEQ ID NO:
- 8), wherein the oligopeptide does not contain any additional amino acids;
- Q is a fluorescence quencher molecule selected from the group consisting of DABCYL, DABSYL, Black Hole Quencher-1 (BHQ-1), Black Hole Quencher-2 (BHQ-2), Black Hole Quencher-3 (BHQ-3), Blackberry Quencher 650, QSY-7, QSY-9, and QSY-21;
- and
- M is polyethylene glycol having a molecular weight of 104 Daltons to 588 Daltons,
- and wherein F, Q and M are linked to separate amino acids of the oligopeptide.
Dependencies are inferred from the claim text.