Early detection of cancer: Fluorophore-labeled cyclooxygenase-2 inhibitors for imaging of overexpression

Nov 07, 2013 by Edward Knaus
Early Detection of Cancer
Fluorophore-labeled cyclooxygenase-2 inhibitors for the imaging of cyclooxygenase-2 overexpression in cancer

Molecules that bind and illuminate proteins specific to tumor cells are key to detecting cancer as early as possible. The cyclooxygenase-2 (COX-2) enzyme is just such a protein, as the concentration of COX-2 is greater in cancer cells than in adjacent normal tissues. Therefore, attaching a suitable fluorescent label to a selective COX-2 inhibitor would be an effective strategy for the noninvasive detection of tumors in which COX-2 levels are elevated.

As they report in ChemMedChem, a collaboration led by Frank Wuest, Edward Knaus, and colleagues at the University of Alberta in Canada resulted in an important compound in which a 7-nitrobenzofurazan (NBD) fluorescent label is linked to the well-known anti-inflammatory drug celecoxib (celecoxib–NBD conjugate). Biological studies showed that this conjugate is a potent and of COX-2, a COX-2-specific biomarker for fluorescence imaging of cancer, and a useful optical probe for targeted imaging of COX-2 in cells and small animals, as well as for clinical imaging of tissues suitable for topical or endoluminal illumination, such as esophagus and colon.

"These results will be of interest to researchers and clinicians with specialization in the use of fluorescent biomarkers for the imaging and/or diagnosis of disease states in which the COX-2 isozyme is expressed, such as ," says Knaus. This work marks a significant step forward in efforts to facilitate the detection and diagnosis of cancer as early as possible.

Explore further: Cells build 'cupboards' to store metals

More information: Fluorophore-Labeled Cyclooxygenase-2 Inhibitors for the Imaging of Cyclooxygenase-2 Overexpression in Cancer: Synthesis and Biological Studies, ChemMedChem, dx.doi.org/10.1002/cmdc.201300355

add to favorites email to friend print save as pdf

Related Stories

Fluorescent compounds make tumors glow

Apr 29, 2010

A series of novel imaging agents could light up tumors as they begin to form - before they turn deadly - and signal their transition to aggressive cancers.

Study: Celecoxib can cause arrhythmias

Jan 15, 2008

U.S. medical researchers have determined the anti-inflammatory drug celecoxib (Celebrex) can adversely affect heart rhythm in fruit fly and rat models.

Team discovers potential new way to treat anxiety

Aug 04, 2013

Chemically modified inhibitors of the COX-2 enzyme relieve anxiety behaviors in mice by activating natural "endocannabinoids" without gastrointestinal side effects, Vanderbilt University scientists will report ...

Imaging inflammation in the living brain

Sep 30, 2011

Inflammation occurs in the human brain during illnesses such as Alzheimer's disease, Parkinson’s disease, stroke and traumatic brain injury. Now, a research team in Japan has developed a probe that can ...

Recommended for you

Cells build 'cupboards' to store metals

Dec 17, 2014

Lawrence Livermore researchers in conjunction with collaborators at University of California (link is external), Los Angeles have found that some cells build intracellular compartments that allow the cell ...

Stunning zinc fireworks when egg meets sperm

Dec 15, 2014

Sparks literally fly when a sperm and an egg hit it off. The fertilized mammalian egg releases from its surface billions of zinc atoms in "zinc sparks," one wave after another, a Northwestern University-led ...

User comments : 0

Please sign in to add a comment. Registration is free, and takes less than a minute. Read more

Click here to reset your password.
Sign in to get notified via email when new comments are made.