Structured-based drug design: Human Folate receptors and Cancer

on 9/9/10, a speaker by the name of Charles Dann III came to our chemistry seminar session and talked about the Structured-based drug design: human Folate receptors and Cancer. He was a tall caucasian male in his late 30's. He spoke clearly and I thought he had a great "stage personality".

He began by talking about Folic acid, which is a single C transferase. From there, he transitioned into Antifolates. Antifolate design closely resembles folate ligand, but is used to target specific enzymes for inhibition. Using Antifolates, Charles hopes to kill cancer cells in the future. The basic idea, is that these antifolates need to bind the folate receptors, but not on the reduced folate carriers. A surprising fact that he mentioned, was that this field had actually been investigated for over 60 years. He gave multiple examples of experiments that had not worked.

From there, Charles transitioned into crystallography and its proceedures. Basically, the first step is to obtain pure protein. Then, you just have to wait for crystallization trials to succeed. The third step is to blast crystals with X-rays. The fourth and fifth step involved processing the data, then building and refining a model. Crystallography shows the structure of the proteins. The reason he mentioned crystallography seemingly out of nowhere, was because he had tried to see the follate receptor using crystallography. He didn't go very deep into his own research.

Overall, his presentation was very interesting. The audience, including myself was never bored and had many questions for him at the end. One thing that I was dissapointed in, was the fact that he showed many of other people's experiments that had failed, and not alot of his own work was presented on.