Journal
CANCER RESEARCH
Volume 70, Issue 19, Pages 7562-7569Publisher
AMER ASSOC CANCER RESEARCH
DOI: 10.1158/0008-5472.CAN-10-1584
Keywords
-
Categories
Funding
- German Research Foundation (Deutsche Forschungsgemeinschaft)
- Swiss National Science Foundation
- Novartis Jubilee Foundation
- Alexander von Humboldt Foundation
- Michael Smith and Gladys Estella Laird Fellowships
- CIHR
- Canada Research Chair in Metalloproteinase Proteomics and Systems Biology
- Canadian Breast Cancer Foundation
- Cancer Research Society
Ask authors/readers for more resources
Matrix metalloproteinases (MMP), strongly associated pathogenic markers of cancer, have undergone extensive drug development programs. Marimastat, a noncovalent MMP inhibitor, was conjugated with FITC to label cellular metalloproteinase cancer targets in MDA-MB-231 cells in vitro. Punctate localization of active transmembrane MMP14 was observed. For molecular-targeted positron emission tomography imaging of syngeneic 67NR murine mammary carcinoma in vivo, marimastat was F-18-labeled using a shelf-stable arylboronic ester conjugate as a captor for aqueous [F-18] fluoride in a novel, rapid one-step reaction at ambient temperature. [F-18] Marimastat-aryltrifluoroborate localized to the tumors, with labeling being blocked in control animals first loaded with >10-fold excess unlabeled marimastat. The labeled drug cleared primarily via the hepatobiliary and gastrointestinal tract, with multiple animals imaged in independent experiments, confirming the ease of this new labeling strategy. Cancer Res; 70(19); 7562-9. (C) 2010 AACR.
Authors
I am an author on this paper
Click your name to claim this paper and add it to your profile.
Reviews
Recommended
No Data Available