Chemistry Seminar Series

Wed, 14 Nov 2018
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Dr. William Lubell

Université de Montréal

Synthesis of Heterocyclic Turn Mimics for Allosteric Receptor Modulation in Biomedical Applications

Wednesday, November 14, 2018
B9201 @ 3:30 p.m.

Host: Dr. David Vocadlo

Abstract

Playing critical roles in human physiology, peptides are often used for therapeutic development, but their utility is compromised by conformational flexibility and rapid metabolism.  Hence, modified peptides, so called peptidomimetics are pursued to improve capacity to effectively target receptors for therapeutic indications.  Mining protein receptors, we have pioneered an approach to identify allosteric modulators as leads for peptide-based drugs. Utilizing the power of organic chemistry, we have produced heterocyclic mimics of peptide secondary structures responsible for the biological activity of these modulators. Methods will be presented for making peptide mimics, possessing amino-lactam, azabicycloalkanone, and azepinone structures, which have been used to modulate interleukin and G protein-coupled receptors towards the conception of therapeutic prototypes with improved physiological properties.

Biography

Professor William D. Lubell has been actively advancing the fields of medicinal chemistry and peptide science through the development of seminal methods to create and employ peptide and peptidomimetic prototypes that target and modulate biologically relevant receptors for drug discovery (www.wdlubellgroup.com). Recipient of a B.A. from Columbia College (1984) and Ph.D. from the University of California, Berkeley (1989), where he studied under the supervision of Professor Henry Rapoport, Lubell was a Japan Society for the Promotion of Science Fellow (1990-1991) in the laboratory of Professor Ryoji Noyori at Nagoya University, Japan, before joining the Department of Chemistry at the Université de Montréal in 1991. Co-author of >250 scientific publications, Associate Editor of Organic Letters since 2005, editorial board member of journals in peptide science and drug design, and innovator of intellectual property to launch the Canadian start-up companies Mperia Therapeutics and Rytvel Biotech, his honors include the Boehringer Ingelheim Young Investigator Award, the DuPont Canada Educational Aid Grant, the Danish National Bank Award, the Merck Therapeutic Research Award, the 2013 CSC Bernard Belleau Award for achievements in medicinal chemistry, and in 2018, the Teva Canada Limited Biological and Medicinal Chemistry Lectureship Award. Originator of Molecules of Life (www.moleculesoflife.ca), Lubell explores experiential education techniques to teach elementary school students about molecules.

 

Dr. William D. Lubell

Professeur Titulaire

Départment de Chimie

Université de Montréal

Email: william.lubell@umontreal.ca

Web: https://www.wdlubellgroup.com/