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Eur J Med Chem. 2015 Apr 13;94:471-9. doi: 10.1016/j.ejmech.2014.07.083. Epub 2014 Jul 24.

Lead discovery and optimization strategies for peptide macrocycles.

Author information

1
Ipsen Bioscience, Inc. 650 East Kendall Street, Cambridge, MA 02142, USA. Electronic address: abhijit.bhat@ipsen.com.
2
Pfizer Worldwide Medicinal Chemistry, 200 Cambridge Park Drive, Cambridge, MA 02140, USA. Electronic address: Lee.roberts@pfizer.com.
3
Ferring Research Institute, 4245 Sorrento Valley Blvd., San Diego, CA 92121, USA. Electronic address: John.dwyer@ferring.com.

Abstract

Peptide macrocycles represent a chemical space where the best of biological tools can synergize with the best of chemical approaches in the quest for leads against undruggable targets. Peptide macrocycles offer some key advantages in both lead discovery and lead optimization phases of drug discovery when compared to natural product and synthetic macrocycles. In addition, they are uniquely positioned to capitalize on the therapeutic potential of peptides because cyclization can help drive selectivity, potency and overcome the common limitations of metabolic instability of peptides.

KEYWORDS:

Macrocycles; PPI; Peptides; Phage display; mRNA display

PMID:
25109255
DOI:
10.1016/j.ejmech.2014.07.083
[Indexed for MEDLINE]
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