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Chemists’ work will aid drug design to target cancer and inflammatory disease

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Posted August 12, 2013
This image shows models of the human folate receptor (top) and antifolate drugs used in chemotherapy (bottom, from left: aminopterin, pemetrexed and methotrexate). Credit: Charles Dann III

This image shows models of the human folate receptor (top) and antifolate drugs used in chemotherapy (bottom, from left: aminopterin, pemetrexed and methotrexate). Credit: Charles Dann III

Chemists at Indiana University Bloomington have produced detailed descriptions of the structure and molecular properties of human folate receptor proteins, a key development for designing new drugs that can target cancer and inflammatory diseases without serious side effects.

The researchers, from the lab of Charles Dann III, assistant professor of chemistry in the College of Arts and Sciences, published their findings in the Proceedings of the National Academy of Sciences. Dann said the results should help chemists create more effective antifolate drugs, which act by interfering with the ability of folates—also called folic acid or vitamin B9—to perform tasks that are essential for cell growth.

The findings could be especially helpful against epithelial cell cancers, including ovarian cancers that are resistant to treatment and nearly always fatal. They could also guide the design of drugs for inflammatory diseases such as rheumatoid arthritis, Crohn’s disease and psoriasis.

The article, “Structures of human folate receptors reveal biological trafficking states and diversity in folate and antifolate recognition,” is scheduled to be online this week. Lead author is Soca Wibowo, an IU staff scientist and a former graduate student in Dann’s lab. Co-authors include Dann; postdoctoral fellow Mirage Singh; former IU undergraduate researchers Kristen Reeder, Joshua Carter and Alexander Kovach; former IU researchers Wuyi Meng and Faming Zhang; and Manohar Ratnam of the Karmanos Cancer Institute in Detroit.

 

Read more at: Phys.org

 

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