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Release issued 19th March 2012
Researchers at the University of Nebraska Medical Center (UNMC), led by Dr. Janina Baranowska-Kortylewicz, have designed a set of novel targeted radiopharmaceutical compounds for the treatment and diagnosis of cancer, which was recently published on line in the Journal of Medicinal Chemistry (JMC) (http://dx.doi.org/10.1021/jm201482p). The compounds consist of cyclosaligenyl monophosphates and target an enzyme known as butyrycholinesterase (BChE), which is commonly overexpressed in a variety of cancers including ovarian cancer, colon cancer and glioblastoma. These compounds have nanomolar IC50 values and specifically bind to BChE. The compounds can be radiolabeled with SPECT and PET compatible radionuclides and radionuclides suitable for Auger electron therapies. This flexibility allows the compounds to be used for both diagnostic imaging and subsequent therapeutic uses. Studies described in the current JMC article demonstrate the efficacy of these compounds in their ability to kill several malignant cancer cell lines. Furthermore, the UNMC researchers have also conducted in vivo studies in a mouse model of ovarian cancer (un-published) demonstrating efficacy and lack of general toxicity. UNMC has filed patent applications covering the composition and use of these compounds and is actively pursuing collaborations with industry to further advance the development of these compounds (www.unemed.com).
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