Beta-Lactam Chemical Probes for GLT-1 Transporter Related Pathologies: A significant percentage of the United States population is affected by a broad range of glutamate-related neurological and pathological disorders which currently lack efficacious and safe treatments. One of the most promising – and understudied – strategies for managing such conditions is glutamate transporter subtype 1 (GLT-1) activation. The recent identification of b-lactam antibiotics as the only practical pharmaceuticals capable of activating GLT-1 indicates that a structure-activity analysis of b-lactam derivatives, directed towards a separation of GLT-1 and antibiotic activity, will result in the identification of one or more novel, non-antibiotic, b-lactam containing reference probes which will provide a structural template for the future development of attractive GLT-1-directed therapies.
Moulder Center for Drug Discovery Research
Temple University School of Pharmacy
3307 N Broad Street
Philadelphia, PA 19140