This study aimed at in vivo visualization of cyclooxygenase-2 (COX-2) by optical imaging using a representative compound of a class of autofluorescent 2,3-diaryl-substituted indole-based selective COX-2 inhibitors (2,3-diaryl-indole coxibs). COX-2 was successfully visualized in mice models with phorbol myristate ester (TPA)-induced inflammation or bearing xenografted human melanoma cells by 2-[4-(aminosulfonyl)phenyl]-3-(4-methoxyphenyl)-1H-indole (C1). COX-2 protein expression in both TPA-induced inflammatory sites and human melanoma xenografts was confirmed by immunoblotting. Control experiments using surrogate markers, sham injections, and non-COX-2 expressing melanoma cells further confirmed specificity of tissue association of C1. The merging of therapeutic and diagnostic properties of 2,3-diaryl-indole coxibs may widen the range of applications of COX-2-targeted treatment, e.g., for in situ-guided surgery and ex vivo diagnostics.
CITATION STYLE
Tondera, C., Ullm, S., Laube, M., Meister, S., Neuber, C., Mosch, B., … Pietzsch, J. (2015). Optical imaging of COX-2: Studies on an autofluorescent 2,3-diaryl-substituted indole-based cyclooxygenase-2 inhibitor. Biochemical and Biophysical Research Communications, 458(1), 40–45. https://doi.org/10.1016/j.bbrc.2015.01.057
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