Nanomedicine is at the cutting edge of science, pushing the frontiers of chemistry, engineering, materials science, biochemistry, and molecular biology. Because the research and technology development are on the nanometer scale, small molecules are the most obvious tools to use to manipulate molecular events. In the Pharmacology Nanomedicine Symposium, we will present four talks that represent the newest advancements in drug discovery and delivery. In the first talk, Dr. Jeanne Hardy will discuss her approach to exploit allosteric sites on proteins for drug discovery. Dr. Wafik El-Deiry will discuss his development of imaging technology to monitor molecular events relevant to tumor progression and therapeutic response. Dr. Scott Diamond will present the strategies being used at the Penn Center for Molecular Discovery to develop microarrays and screens against proteases, kinases, and phosphatases on a nanoliter scale. The last talk of the session by Dr. David Needham will present a novel approach for drug delivery at sites of tumors using bnano-soccerballQ liposomes to control drug release temporally and spatially.