Towards kit-like 18F-labeling of marimastat, a noncovalent inhibitor drug for in vivo PET imaging cancer associated matrix metalloproteases

Ying Li; Richard Ting; Curtis W. Harwig; Ulrich auf dem Keller; Caroline L. Bellac; Philipp F. Lange; James A. H. Inkster; Paul Schaffer; Michael J. Adam; Thomas J. Ruth; Christopher M. Overall; David M. Perrin

doi:10.1039/C1MD00117E

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MedChemComm

Issue 10, 2011

Rapid communication of research in medicinal chemistry

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Towards kit-like ¹⁸F-labeling of marimastat, a noncovalent inhibitor drug for in vivo PET imaging cancer associated matrix metalloproteases

Ying Li,^a Richard Ting,^a Curtis W. Harwig,^a Ulrich auf dem Keller,^b Caroline L. Bellac,^b Philipp F. Lange,^b James A. H. Inkster,^c Paul Schaffer,^c Michael J. Adam,^a^c Thomas J. Ruth,^c Christopher M. Overall^b and David M. Perrin*^a

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Department of Chemistry, The University of British Columbia, 2036 Main Mall, Vancouver, Canada
E-mail: dperrin@chem.ubc.ca ;
Fax: +1-604-822-2847 ;
Tel: +1-604-822-0567

Centre for Blood Research and Department of Biochemistry and Molecular Biology, The University of British Columbia, 2350 Health Sciences Mall, Vancouver, Canada
E-mail: chris.overall@ubc.ca ;
Fax: +1-604-822-7742 ;
Tel: +1-604-822-2958

TRIUMF, 4004 Wesbrook Mall, Vancouver, Canada
E-mail: truth@triumf.ca ;
Tel: +1-604-222-7526

Med. Chem. Commun., 2011,2, 942-949

DOI: 10.1039/C1MD00117E
Received 05 May 2011, Accepted 07 Jun 2011
First published online 07 Jul 2011

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Marimastat, a clinically trialed drug developed to treat breast cancer by inhibiting cancer-associated matrix metalloproteases (MMPs), was linked to an aryl boronic ester for single-step [¹⁸F]-aqueous fluoride capture and the labeled product revealed tumor associated MMP activity in vivo. Herein, we report important radiosynthetic attributes for labeling marimastat that enabled the first PET images of breast cancer-associated matrix metalloproteases in a syngenic murine model. The advantages of this method include one-step post synthetic labeling in less than one hour at ambient temperature, the ability to work in aqueous media without drying the ¹⁸F-fluoride, observation of high radiochemical purity, and the potential for tripling the specific activity of the fluoride used in labeling. Using low levels of activity e.g. 60 mCi in low volumes this method affords reasonable yields of labeled marimastat with decay-corrected specific activities of 0.39 and 0.75 Ci/μmol, and real specific activities of 0.16 and 0.39 Ci/μmol. Current limitations of this method along with anticipated improvements are discussed.

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Towards kit-like 18F-labeling of marimastat, a noncovalent inhibitor drug for in vivo PET imaging cancer associated matrix metalloproteases

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Towards kit-like ¹⁸F-labeling of marimastat, a noncovalent inhibitor drug for in vivo PET imaging cancer associated matrix metalloproteases