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Latest cancer research features small molecule therapy, and the preventative benefits of sunshine

ORLANDO Among the latest breaking cancer research presented today scientists described a small molecule that locks into DNA structures, inhibiting the expression hard-to-target oncogenes. In another application a of small molecule targeted drug therapy, an agonist turns on a gene-regulating pathway to inhibit growth and metastasis in deadly thyroid tumors. From down under, Australian researchers found that sun worshippers are taking steps to prevent non-Hodgkin Lymphomas. This research was presented here at the 95th Annual Meeting of the American Association for Cancer Research.

In vivo cfficacy of CX-3543, a novel c-Myc oncogene inhibitor: Abstract No. LB-243

Cancer researchers today unveiled a new small molecule drug that specifically targets c-Myc, a key growth promoting regulator in cancers and a gene that has escaped all efforts to control it.

William Rice, Ph.D., the presenting author on a team of scientists from Cylene Pharmaceuticals, San Diego, Calif., said that the small molecule CX-3543 effectively reduced cMyc mRNA expression by 85 percent in colorectal tumor animal models. The small molecule inhibited growth of prostate and pancreatic tumor models in mice as well. Each of those tumor cell types are known to produce high levels of cMyc during tumor growth.

"We have identified a small molecule with drug-like properties that is a candidate for further preclinical development," Rice said.

CX-3543 selectively suppresses cMyc activity by specifically binding to the cMyc quadruplex, he said. G-quadruplex structures are four stranded DNA secondary structures. Certain G-quadruplexes regulate transcription of specific oncogenes, including cMyc. The quadruplex cluster that includes cMyc also includes VEGF, a growth factor that regulates development of blood vessels to tumors. CX-3543 inhibits VEGF expression as well as cMyc.

"We selected CX-3543 as the first 'Oncog
'"/>

Contact: Aimee Frank
amf@spectrumscience.com
202-955-6222
American Association for Cancer Research
31-Mar-2004


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