Macrocycles: An Increasingly Popular Strategy In Drug Design

Recorded: December, 2024

11am ET / 4pm UK

This webinar will review the emergence of macrocycles as a powerful strategy in drug design and discovery, highlighting the principles of rational design and the benefits and challenges of this class of compounds.

Agenda:

• Introductions to macrocycles
  • What are macrocyclic drugs?
  • What are their advantages compared to their acyclic counterparts?
• Macrocycle rational design
  • What are the strategies to design successful macrocycles?
  • What are the known principles for the optimization of physicochemical properties?
• Case Study: the discovery of a novel series of PKCθ inhibitors with exquisite potency and isoform selectivity
  • Success and challenges throughout the lead optimization process

Moderated by:

Kevin Foote, Ph.D. – VP of Drug Discovery at Pharmaron

Speakers

Mike Waring – Professor, Newcastle University, Chair of Medicinal Chemistry

Mike's research interests are related to drug discovery using medicinal chemistry. He is Head of Medicinal Chemistry in the Cancer Research UK Newcastle Drug Discovery Group and Director of Academic Medicinal Chemistry for Cancer Research Horizons, CRUK's innovative organization for therapeutic discovery. He is the Director of the EPSRC Centre for Doctoral Training in Molecular Sciences for Medicine and Editor-in-Chief of RSC Medicinal Chemistry. Mike teaches Pharmacokinetics and Drug Metabolism in the Chemistry with Medicinal Chemistry (BSc and MChem) and Drug Chemistry (MSc) degree programs.
Before joining Newcastle University in 2016, Mike spent 14 years at AstraZeneca, leading medicinal chemistry programs from hit to candidate selection stage.

Sébastien Campos, Ph.D.​ – Senior Director, Medicinal Chemistry at Pharmaron

Sébastien is leading the medicinal chemistry group at Pharmaron in the UK. He and his team are responsible for leading/executing drug design projects at any stage of the discovery process, from hit finding to candidate nomination. Before joining Pharmaron in 2018, he was a medicinal chemistry team leader at GlaxoSmithKline for 15 years. At GSK, Sébastien worked on various target classes, mainly in respiratory and inflammation therapeutic areas, and was involved in discovering various clinical candidates for oral and inhaled administration. He has expertise in Targeted Protein Degradation, acquired from his active contribution to the collaboration between Craig Crews (Yale University) and GSK. Sébastien has an interest and knowledge in chemical biology, mainly developed during an 18-month secondment at the Francis Crick Institute, London. He is co-author/co-inventor of over 45 peer-reviewed publications, patent applications, and oral presentations at major scientific meetings.

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