The mission of the Vanderbilt University Molecular Libraries Screening Center (VUMLSC) is to engage the research community in the discovery and optimization of biologically active chemical probes that promote the understanding of cellular physiology, particularly the role of G-protein coupled receptors (GPCRs), ion channels and transporters.

The Vanderbilt MLSCN specializes in, but is not limited to G-protein coupled receptors (GPCRs), ion channels, and transporters. These targets are the focus of intense basic research and pharmaceutical development. However, there remains a need for new tools to develop a better understanding of the roles of these proteins in biological systems and to pave the way for discovery of novel therapeutic agents. Although ligand discovery has been performed on these proteins in pharmaceutical companies, their retail product interests often preclude, or greatly delay, the publication of research findings or consider only one of the many possible modes of target/small molecule interaction. Despite intense interest of multiple academic and industry labs, small molecules ligands do not exist for the vast majority of GPCRs, ion channels, and transporters.

The research community, supported by the MLSCN initiative, has an excellent opportunity to develop novel tools to aid in understanding these proteins. Thus, we proposed a MLSCN screening center focused on the generation of chemical tools for the study of G-protein coupled receptors, ion channels, and transporters. We perform cell-based functional HTS for these proteins using industry-standard instrumentation and screening methods. We further enhance our ability to rapidly discover and characterize novel tools for these targets and the signaling pathways/physiological systems of which they are a part by using new technologies to allow more physiologically-relevant interrogation of interactions between these proteins and their partners. We are developing the expertise, technologies, and methods to understand and improve the properties of small molecules discovered through HTS to produce tools to support basic and translational research. Vanderbilt University is well suited to support an MLSCN center due to its combination of basic and industrial research expertise in the proposed target areas, its dedication to translational and chemical biology, and its tradition of excellence in the establishing and maintaining highly-collaborative laboratories and core facilities.