The Chemist's Playbook: Impactful Bioisosteres for Modern Drug Design
Flash Talk with Guest, Nicholas Meanwell, Ph.D.
Hosted by Drug Hunter's Director of Industry Research & Relations Dennis Koester, Ph.D.
October 24, 2024 at 8 AM PDT / 11 AM EDT / 5PM CEST
The concept of isosterism between functionalities of similar size and chemical properties has its origins in observations made by Irving Langmuir over 100 years ago who predicted the physicochemical properties of ketene almost 20 years in advance of its first isolation. A bioisosteric relationship between benzene and thiophene rings was established by Landsteiner and Erlenmeyer in the 1930s in the context of antibody recognition of artificial antigens. Against this backdrop, the ever-expanding drug discovery and development enterprise began to exploit this form of molecular recognition to identify and advance candidate molecules. The modern era of bioisosterism in molecular recognition began in 1951 with the introduction of the term by Harris Friedman and design principles have extended the concept well beyond the simple notion of shape mimicry to embrace more sophisticated, higher order functionalities that recapitulate biological rather than physicochemical properties. As a consequence, bioisosterism can be highly contextual in nature, which provides the stimulus to explore refined concepts in molecular recognition for a specific biological target.
In this Flash Talk, Nicholas Meanwell will explore several established and emerging bioisosteres that have been deployed to address a range of challenges in drug discovery and which have had an impact on the contemporary pharmacopeia.
Nicholas Meanwell has over 40 years of experience in Drug Discovery. He led drug discovery programs in the cardiovascular, neurosciences and virology therapeutic areas resulting in the advancement of 33 clinical candidates for the prevention of thrombosis, the treatment of stroke and therapy for viral infections, including human immunodeficiency virus-1 (HIV-1), hepatitis C virus (HCV) and respiratory syncytial virus (RSV).
Nick is the author/co-author of more than 300 publications, review articles, book chapters and editorials and more than 200 meeting abstracts. He is named as inventor/co-inventor of 144 issued U.S. Patents. Nick was inducted in the MEDI ACS Hall of Fame and received the prestigious Hero of Chemistry Award twice. These are just a few among many more awards that he received. Nick obtained his Ph.D. from the University of Sheffield and started his industry career at BMS in 1982 after a postdoc at Wayne State University. Nick retired from his Senior Vice President position at BMS in 2022 but is still very active in the field of Medicinal Chemistry.
Don't miss this opportunity to learn about impactful bioisosters from a legend in the field! Join us and Nick for an exciting talk. Nick will be available for a Q&A session that you won't want to miss!