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1.
ACS Med Chem Lett ; 11(10): 1837-1842, 2020 Oct 08.
Article in English | MEDLINE | ID: mdl-33062161

ABSTRACT

Overexpression of cyclooxygenase-1 (COX-1) is associated with the initiation and progression of ovarian cancer, and targeted imaging of COX-1 is a promising strategy for early detection of this disease. We report the discovery of N-[(5-carboxy-X-rhodaminyl)but-4-yl]-3-(1-(4-methoxyphenyl)-5-(p-tolyl)-1H-pyrazol-3-yl)propenamide (CMP) as the first COX-1-targeted optical agent for imaging of ovarian cancer. CMP exhibits light emission at 604 nm (λmax), thereby minimizing tissue autofluorescence interference. In both purified enzyme and COX-1-expressing human ovarian adenocarcinoma (OVCAR-3) cells, CMP inhibits COX-1 at low nanomolar potencies (IC50 = 94 and 44 nM, respectively). CMP's selective binding to COX-1 in OVCAR-3 cells was visualized microscopically as intense intracellular fluorescence. In vivo optical imaging of xenografts in athymic nude mice revealed COX-1-dependent accumulation of CMP in COX-1-expressing mouse ovarian surface epithelial carcinoma (ID8-NGL) and OVCAR-3 cells. These results establish proof-of-principle for the feasibility of targeting COX-1 in the development of new imaging and therapeutic strategies for ovarian cancer.

2.
Br J Radiol ; 88(1056): 20150633, 2015.
Article in English | MEDLINE | ID: mdl-26481696

ABSTRACT

OBJECTIVE: With increased signal to noise ratios, 7.0-T MRI has the potential to contribute unique information regarding anatomy and pathophysiology of a disease. However, concerns for the safety of subjects with metallic medical implants have hindered advancement in this field. The purpose of the present research was to evaluate the MRI safety for 39 commonly used medical implants at 7.0 T. METHODS: Selected metallic implants were tested for magnetic field interactions, radiofrequency-induced heating and artefacts using standardized testing techniques. RESULTS: 5 of the 39 implants tested may be unsafe for subjects undergoing MRI at 7.0 T. CONCLUSION: Implants were deemed either "MR Conditional" or "MR Unsafe" for the 7.0-T MRI environment. Further research is needed to expand the existing database categorizing implants that are acceptable for patients referred for MRI examinations at 7.0 T. ADVANCES IN KNOWLEDGE: Lack of MRI testing for common metallic medical implants limits the translational potential of 7.0-T MRI. For safety reasons, patients with metallic implants are not allowed to undergo a 7.0-T MRI scan, precluding part of the population that can benefit from the detailed resolution of ultra-high-field MRIs. This investigation provides necessary MRI testing of common medical implants at 7.0 T.


Subject(s)
Magnetic Resonance Imaging/instrumentation , Magnetic Resonance Imaging/methods , Metals , Prostheses and Implants/statistics & numerical data , Artifacts , Equipment Safety , Magnetics , Risk Assessment
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