Dr Philip S. Portoghese - 2001

“From Models to Molecules in Opioid Research"
Dr Philip S. Portoghese
Department of Medicinal Chemistry
College of Pharmacy
University of Minnesota
Minneapolis, MN, USA

Over the years opioid ligands have been the most investigated class of compounds. The molecular diversity of opioids and the existence of subpopulations of opioid receptors have posed both challenges and opportunities for medicinal chemists. In this presentation, models for the design of opiate-derived ligands as probes are discussed together with their utilization to investigate the architecture of opioid recognition sites and organization of opioid receptors. The combination of structure-activity studies, site-directed mutagenesis, and molecular modeling have provided greater insight of molecular recognition from the perspective of both the ligand and opioid receptor.