Optical imaging of COX-2: studies on an autofluorescent 2,3-diaryl-substituted indole-based cyclooxygenase-2 inhibitor.

Abstract:

: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.

authors

Tondera C,Ullm S,Laube M,Meister S,Neuber C,Mosch B,Kniess T,Pietzsch J

doi

10.1016/j.bbrc.2015.01.057

subject

Has Abstract

pub_date

2015-02-27 00:00:00

pages

40-5

issue

1

eissn

0006-291X

issn

1090-2104

pii

S0006-291X(15)00087-X

journal_volume

458

pub_type

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