PROBLEM: Of the thousands of drugs used to treat disease, most are small molecules–organic compounds that bind with proteins and influence their activity. But researchers must screen many compounds to find potential drugs, and the large number of chemical reactions needed to synthesize any one compound makes the process slow and painstaking.
SOLUTION: Martin Burke, an assistant professor of chemistry, has figured out a way to simply and quickly generate diverse arrays of small molecules by repeatedly using a single reaction to join different organic components. He begins by turning a wide variety of organic molecules into standardized building blocks, each of which has a boronic acid on one end and a halide, such as bromide, on the other. In a test tube, the two ends react to link molecules with a carbon-carbon bond. Burke’s key advance is a way to reversibly obstruct the boronic-acid end, so that chemists can sequentially couple different molecules.
Burke is partnering with a major chemical company to release a set of premade building blocks. Ultimately, he hopes that the ability to quickly create large collections of compounds will help him find highly complex small molecules that can imitate the structure of proteins that malfunction in diseases such as cystic fibrosis. Such “molecular prosthetics” could provide new treatments for a whole array of diseases, saving lives. –Lissa Harris