Peter W. Schiller
Professor Peter W. Schiller pioneered the medicinal chemistry and molecular pharmacology of opioid peptides. His research produced highly receptor-selective agonists and antagonists that became standard pharmacological tools, as well as bifunctional opioid compounds that offer analgesia with reduced tolerance and dependence. His later discovery of mitochondria-protecting peptides opened new therapeutic avenues for diseases associated with mitochondrial dysfunction.
Schiller was born on February 9, 1942, in Frauenfeld, Switzerland. He studied chemistry at the Swiss Federal Institute of Technology in Zurich, earning his Diplom in 1966 and his Ph.D. in the Institute of Molecular Biology and Biophysics in 1971. He trained as a postdoctoral fellow in the Department of Biology at Johns Hopkins University and in the Laboratory of Chemical Biology at the National Institutes of Health from 1973 to 1974. In 1975 he joined the Clinical Research Institute of Montreal as Director of the Laboratory of Chemical Biology and Peptide Research, a position he held until becoming Research Professor Emeritus in 2020. He also held a research professorship in the Department of Pharmacology and Physiology at the Université de Montréal.
Schiller's group developed conformationally restricted peptide analogs and peptidomimetics to probe the stereochemical requirements of opioid receptor subtypes. This work produced TIPP and related δ-selective antagonists, dermorphin-derived analogs such as DALDA and its extraordinarily potent variant [Dmt1]DALDA, and the mixed μ agonist/δ antagonist DIPP-NH2[Ψ]. The latter compound demonstrated that bifunctional opioids can produce potent analgesia with less tolerance and no physical dependence compared to morphine. In 2015 the crystal structure of the δ opioid receptor bound to DIPP-NH2 was published in Nature Structural and Molecular Biology, enabling structure-based design of improved analgesic candidates. Many compounds from his laboratory are distributed through the NIH Drug Supply System for use by the research community.
Together with Hazel H. Szeto at Cornell Medical College, Schiller co-designed the Szeto-Schiller peptides, cell-penetrating sequences that protect mitochondrial function by promoting efficient electron transfer, enhancing ATP synthesis and reducing free radical production. The lead compound elamipretide advanced to Phase 2 and 3 clinical trials for indications including age-related macular degeneration, Barth syndrome and Leber's hereditary optic neuropathy. The IRCM and Cornell Research Foundation hold joint patents on these compounds.
Schiller served as President of the American Peptide Society from 1995 to 1997 and as Chair of the Section of Drug Design and Discovery of the American Association of Pharmaceutical Scientists in 2003. His honors include the Vincent du Vigneaud Award in 1998, the Prix Galien of Canada for excellence in pharmaceutical research, an NIH MERIT Award and the Canada Pacific Chair in Pain Research. He was elected a Fellow of the Royal Society of Canada in 1991, a Fellow of the American Association of Pharmaceutical Scientists in 1998 and a Fellow of the American Association for the Advancement of Science in 2001. He received the Order of Quebec and held visiting appointments at ETH Zurich, the University of Washington, McGill University, the National University of Singapore and Nanyang Technological University. He has published more than 420 scientific articles and holds 17 patents.
