SC7: Enabling Macrocyclic Compounds for Drug Discovery: Opportunities, Challenges and Strategies
TUESDAY, SEPTEMBER 25, 6:00 - 8:30 PM

Macrocyclic compounds occupy an important underexplored chemical space between small molecules and biologics. However, these structures possess critical characteristics typically attributed to only one of these two broad categories, which makes them particularly attractive for modulating traditionally difficult target classes such as protein-protein interactions. With improvements in the past decade in the technologies for accessing these molecules and libraries thereof, significant progress has been realized; the number of synthetic macrocycles entering into clinical trials has steadily increased. This course will discuss important past and recent advances in the field, including an improved understanding of the properties of macrocyclic molecules, particularly as related to their PK-ADME profiles. Specific case studies of these compounds in drug discovery and development will be presented. The course is suitable for all those who wish to learn more about the current state and future potential of this evolving area regardless of their level of knowledge.

Topics to Be Discussed:


  • Unique characteristics and properties of macrocycles
  • Factors affecting cell permeability and PK/ADME properties
  • Synthetic challenges and strategies for macrocyclic compounds and libraries
  • Drug discovery and development case studies
  • Additional medicinal chemistry applications of macrocyclic molecules
  • Perspectives on remaining challenges and future opportunities for macrocyclic molecules

Instructor Biography:

Peterson_MarkMark L. Peterson, PhD, COO, Cyclenium Pharma, Inc.

Dr. Peterson recently co-founded Cyclenium Pharma with a focus on developing and utilizing a next generation macrocyclic technology for novel drug discovery. Prior to Cyclenium, Dr. Peterson was Vice President, IP & Operations at Tranzyme Pharma, a pioneer in the use of small molecule macrocycles in pharmaceutical research, where he led the chemistry R & D efforts during the technology development stage of the company and the initiation of its discovery programs, then later was instrumental in contributing to the development of its clinical portfolio and building an extensive portfolio of over 120 patents and applications. Previously with Monsanto and Advanced ChemTech, he has worked in a variety of research areas including structure-based design, solid phase organic chemistry, combinatorial technologies, synthetic automation, heterocycles, unnatural amino acids, peptides and peptidomimetics. A native of Wisconsin, he received his Ph.D. in Organic Chemistry from Washington State University and conducted post-doctoral research at the University of Minnesota, the last year receiving an NIH National Research Service Award. He is author or co-author of over 85 publications and abstracted presentations plus three book chapters, as well as co-inventor on over 25 patents.

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