Abstract

New materials and methods that enable the simple inclusion of ¹⁸F into cancer-targeting peptides that can be used as radiolabels for PET imaging

Full Description

Positron emission tomography (PET) is a highly sensitive, noninvasive method for the detection of cancer.  Although the technique is generally available in major oncology clinics, its usefulness is nonetheless restricted by limitations in radiolabeling methodology.  PET makes predominant use of the positron-emitting fluorine isotope ¹⁸F.  Currently, the only practical vehicle for clinical application of ¹⁸F in PET is 2-¹⁸F-2-deoxy-D-glucose (FDG), which is taken up by many types of tumor cells.  The exclusive use of FDG however limits the types of cancers which can be imaged by PET.  Certain peptides and small proteins are known to be remarkably sensitive and selective cancer targeting agents.  However, the labeling of these peptides with ¹⁸F is laborious and impractical in a clinical setting.  This invention addresses the above obstacle directly by the attachment of a highly selective fluoride ion binding agent to cancer-specific peptides, allowing immediate radiolabeling with ¹⁸F.  This eliminates the necessity to perform any synthetic chemistry with ¹⁸F, resulting in a highly simplified, automatable labeling protocol which has the potential to revolutionize the application of PET to the cancer problem.

Features/Benefits

The combination of disease-specific imaging with a highly simplified ¹⁸F labeling protocol.

Related Materials

• "Targeting Peptides and Positron Emission Tomography." H. Lundqvist, V. Tolmachev, Biopolymers 2002, 66, 381.
• "Therapeutic Cancer Targeting Peptides." O. H. Aina, T. C. Sroka, M.-L. Chen, K. S. Lam, Biopolymers (Peptide Science) 2002, 66, 184.
• "Somatostatin Analogs and Radiopeptides in Cancer Therapy." S. Froidevaux, A. N. Eberle, Biopolymers (Peptide Science) 2002, 66, 161.
• "Molecular Imaging of Cancer with Positron Emission Tomography." S. S. Gambhir, Nature Reviews Cancer 2002, 2, 683.
• "Positron Emission Tomography in Cancer Research and Treatment." M. Mandelkern, J. Raines, Technology in Cancer Research and Treatment 2002, 1, 423.
• "Precedent and Theory Unite in the Hypothesis of a Highly Selective Fluoride Receptor." M. Mascal, Angewandte Chemie International Edition 2006, 45, 2890.
• "Integrins in Cancer Treatment." J. A. Eble, J. Haier, Curr. Cancer Drug Targets 2006, 6, 89.
• "Fluoride-Selective Host Based on Anion-Pi Interactions, Ion Pairing, and Hydrogen Bonding: Synthesis and Fluoride-Ion Sandwich Complex." M. Mascal, I. Yakovlev, E.B. Nikitin, and J.C. Fettinger, Angewandte Chemie International Edition 2007, 46, 8782-4.

Patent Status

Inventors

• Mascal, Mark J.

Other Information

Contact

Nancy E. Rashid / nerashid@ucdavis.edu / tel: View Phone Number. Please reference Tech ID #19235.

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