Novel matrix metalloproteinase inhibitor [18F]marimastat-aryltrifluoroborate as a probe for in vivo positron emission tomography imaging in cancer.
Cancer Res
; 70(19): 7562-9, 2010 Oct 01.
Article
em En
| MEDLINE
| ID: mdl-20729277
ABSTRACT
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 (18)F-labeled using a shelf-stable arylboronic ester conjugate as a captor for aqueous [(18)F]fluoride in a novel, rapid one-step reaction at ambient temperature. [(18)F]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.
Texto completo:
1
Coleções:
01-internacional
Base de dados:
MEDLINE
Assunto principal:
Neoplasias da Mama
/
Radioisótopos de Flúor
/
Compostos Radiofarmacêuticos
/
Inibidores Enzimáticos
/
Inibidores de Metaloproteinases de Matriz
/
Ácidos Hidroxâmicos
/
Neoplasias Mamárias Experimentais
Limite:
Animals
/
Female
/
Humans
Idioma:
En
Ano de publicação:
2010
Tipo de documento:
Article