Â鶹´«Ã½ — A new class of compounds developed by two University of Kentucky researchers shows promise as a nontoxic treatment of some cancers previously treated with toxic chemotherapy, the researchers report today.

In a study published in the April 30 issue of the academic journal Chemistry & Biology, UK pharmaceutical sciences graduate student Abby Ho mentored by assistant professor Kyung-Bo Kim and ophthalmology and visual sciences assistant professor Royce Mohan describe a compound that acts directly on LMP2, a component of the immune proteasome variant that has been identified abundantly expressed in certain types of tumors, including some prostate cancers.

The compound, dubbed UK-101, inhibits LMP2 while not attacking normal cells, indicating that it could be an effective cancer treatment that does not produce the kinds of unpleasant side effects reported by many patients currently treated with broadly acting proteasome inhibitors and chemotherapeutics.

Kim and Mohan also suggest that UK-101 may be useful in treating a number of diseases in which LMP2 is involved. The researchers are particularly excited about UK-101's potential in treating inflammatory conditions associated with arthritis, rheumatism and cardiovascular diseases.

The researchers report success in using the compound in tests in prostate cancer cells. Importantly, Kim and Mohan point out that in test using highly sensitive vascular endothelial cells obtained from blood vessels that UK-101 was found to be non toxic because they lacked expression of this LMP2 immunoproteasome target.

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Chemistry & Biology (30-Apr-2007)