The newer, synthetic macrocyclic and constrained peptide compounds (ranging in size from .5 -2 kilodaltons) have become possible because of advances in the past decade in combining biological and chemical approaches to create new types of synthetic libraries with molecules that represent the ‘ideal’ class of compounds in theory for new drug entities. The cyclical shape enables solubility and more stability in the case of peptides, affording them the possibility to be developed into oral medications and most are small enough to cross the cell membrane and reach intracellular targets, where many of the causes and solutions to diseases reside. Yet because of macrocyclics’ slightly larger size than typical small molecules, they offer more specificity and have greater chances of disrupting protein-protein interactions.
However, theory has yet to be fully realized. Challenges related to solubility and cell permeability are still being addressed. A few small synthetic macrocyclic or constrained-peptide compounds are progressing in clinical trials, but because this class of molecules is diverse and it is still ‘early days’ in the field. While it’s unlikely there will be one lead optimization strategy that will fit the whole class of molecules, figuring out general guidelines for advancing the field, is very much the focus nowadays. Be a part of the discussions on how to translate the promise of small molecule macrocyclics to reality by joining us at Cambridge Healthtech Institute’s day-and-a-half ‘Macrocyclics’ meeting that is in the second half of our larger Drug Discovery Chemistry event.
Topics will likely include:
- 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
- Different scaffolds of macrocycles for drug applications
- Peptide cyclization strategies – chemical, biologic and combined approaches
- Case studies on optimization challenges of small macrocyclics progressing in drug development
- Using constrained peptides (ones that are too large for oral bioavailability) for target validation application
If you would like to submit a proposal to give a presentation at this meeting, please click here.
The deadline for submission is October 2, 2015
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.
Cambridge Healthtech Institute
Phone: (914) 723-0251
For partnering & sponsorship information, please contact:
Business Development Manager
Cambridge Healthtech Institute
Phone: (+1) 781-972-5412