A potent class of small molecules has reportedly been targeted by researchers in the design of new treatments for diseases, such as multiple sclerosis (MS). The class of molecules pinpointed by researchers of the National Institutes of Health Common Fund and the National Institute of General Medical Science (NIGMS) selectively turn on the S1P1 receptor, according to an NIH news release.

Francis S. Collins, MD, PhD, NIH director, explains that the work exemplifies, “how structural studies can reveal insights into basic principles of protein function and how this may lead to smarter, safer drugs. This approach could be used to design better therapies for a variety of adverse health conditions,” Collins says.

The news release reports that the research team of Raymond Stevens, PhD, and Hugh Rosen, MD, PhD, The Scripps Research Institute, La Jolla, Calif, used technology developed through the Structural Biology Program of the NIH Common Fund, to take molecular snapshots of S1P1 bound to different activators and inhibitors. According to the study’s results, the snapshots indicated that S1P1 exhibits structural features that allow it to bind activators in two ways. Researchers add that one of these structural features varies subtly between related GPCRs, enabling molecules to be designed to activate S1P1 selectively. These molecules may offer promising implications in effective therapies for MS, with potentially fewer side effects than current therapies.

James M. Anderson, MD, PhD, director of the Division of Program Coordination, Planning, and Strategic Initiatives that guides the NIH Common Fund’s programs, notes that the potential impact of the research is far-reaching, pointing to the implication of the GCPR family in diseases, including MS and heart disease. “Using the results from this study, investigators may be able to design drugs that selectively activate or inhibit other important GCPRs,” Anderson emphasizes.

Source: NIH