3rd Annual

Macrocyclics and Constrained Peptides

Bigger, Better, But hopefully still Oral, Small Molecules

April 22-23, 2015 


This meeting was an eye-opener for me to see how collectively drug delivery scientists can work
with medicinal chemists to bring new pharmaceutical products more effectively to the market.

Hayat O., Professor, University of Illinois at Chicago

Recent advances combining biological and chemical approaches to create libraries of small, synthetic macrocyclic molecules have created a new class of therapeutically promising compounds that exhibit desireable ‘middle ground’ characteristics placing them in size between small molecule drug entities and larger therapeutic antibodies. Similar to small molecules, the smaller macrocyclics can pass through the cell membrane to reach intracellular targets and have the potential to be delivered orally. But their cyclic shape and slightly larger size confers advantages of bigger (but not orally bioavailable) molecules such as biologics and naturally-occurring macrocyclics which have better specificity for disrupting protein-protein interactions. Thus small macrocyclics have the promise to successfully inhibit a largely untapped but medically relevant class of drug targets –intracellular regulatory protein complexes that are dependent on protein-protein interactions.

Cambridge Healthtech Institute’s third annual Macrocyclic and Constrained Peptides meeting, part of our Drug Discovery Chemistry event, will continue to explore this emerging class of molecules and discuss the challenges they are facing as drug candidates now that several have entered clinical development. Constrained peptides, which can be considered macrocyclic because of their 3D shape but are slightly larger (between 2 and 5 kilodaltons) than macrocyclic peptides, will also be covered. Join fellow drug discovery scientists for this day-and-a-half meeting that is in the second half of our larger Drug Discovery Chemistry event.

Topics may include, but are not limited to: 

  • Beyond Lipinski’s rule of five: achieving functional and chemical diversity in libraries by increasing size and shape but retaining oral availability and cell permeability
  • DNA-encoded chemistries for small macrocyclic or constrained peptide libraries
  • Peptide cyclization strategies – chemical, biologic and combined approaches
  • Updates on small macrocyclics progressing in drug development and discussion of their optimization challenges
  • Pros and cons of different macrocycle scaffolds for drug applications
  • Optimizing cell permeability, oral availability and stability features of synthetic macrocyclics
  • Bigger (non-oral), constrained peptides for target validation applications

If you would like to submit a proposal to give a presentation at this meeting, please click here.

The deadline for submission is September 22, 2014 

All proposals are subject to review by the Scientific Advisory Committee to ensure the highest quality of the conference program.  Please note that due to limited speaking slots, preference is given to pharmaceutical and biotech companies, regulators and those from academia. Additionally, vendors/consultants who provide products and services to these biopharmaceutical companies are offered opportunities for podium presentation slots based on a variety of Corporate Sponsorships. 

For more details on the conference, please contact:
Anjani Shah, Ph.D.
Conference Director
Cambridge Healthtech Institute
Phone: (914) 723-0255
Email: ashah@healthtech.com 

For partnering and sponsorship information, please contact:
Carolyn Benton
Business Development Manager
Cambridge Healthtech Institute
Phone: (+1) 781-972-5412
Email: cbenton@healthtech.com