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human folate receptor protein

Human Folate Receptor Model May Aid Antifolate Drug Design

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Model of the human folate receptor and three antifolate drugs used in chemotherapy

Caption: A model of the human folate receptor (top) and three antifolate drugs used in chemotherapy: aminopterin (left), pemetrexed, and methotrexate (right).
Credit: Charles Dann III / Courtesy of Indiana University

Vitamin B9 or folic acid, which is found in dark green leafy vegetables, is essential for cells to grow and divide rapidly—as they do in a growing embryo. This is why women are advised to take folic acid supplements before conception and during pregnancy: inadequate folate raises the risk of brain and spinal cord defects. But while folic acid is key to normal cell growth, rapidly dividing cancer cells also have a tremendous appetite for this vitamin.

Drugs called antifolates have been used for decades in chemotherapy to starve cancer cells of folate, which can help kill the tumor. These drugs have also been used to treat inflammatory diseases like rheumatoid arthritis and Crohn’s disease. But many of these drugs have nasty side effects because they also enter normal healthy cells, depriving them of this essential compound.