Folate receptor crystal structure-anti-cancer drug development

Folic acid and vitamin B9 is an essential substance for cell growth. Indiana University scientists have revealed the refined structure and molecular properties of human folate receptors. To provide a basis for scientists to design and develop new drugs for the treatment of cancer and inflammatory diseases without side effects.

The research was completed under the supervision of Professor Charles Dann III of the College of Arts and Sciences at Indiana University, and related reports were published in the recent PNAS magazine. Professor Dann said the research will help chemists develop more effective antifolate drugs.

For nearly 60 years, doctors have been using antifolate drugs to treat cancer. These drugs are usually effective in killing cancer cells, but the problem is that drugs are poorly selective.

Professor Dann said that antifolate drugs used today can also enter and kill normal cells. Our findings help scientists develop specific drugs that attack cancer cells.

Folate receptors are not only present in cancer cells but also expressed in most normal cells. Therefore, antifolate drugs are not highly selective. In this study, the scientists tested the folate receptors specifically expressed in cancer cells. The receptor is not expressed in healthy cells.

Dr. Dann likens the folate receptor to a key that opens the door of a cell. By revealing the appearance and mechanism of the key in more detail, scientists can construct a better key, which is a more effective antifolate drug.

In order to study the structure of the folate receptor, the scientists obtained the crystal of the receptor for the first time. The scientists took “molecular photographs” of the receptor to determine the position of the atom and revealed the conformation of the folate receptor molecule such as the spiral and folding.