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Peptides in drug discovery


*Corresponding author
Département de Chimie, Université de Montréal, C.P. 6128, Succursale Centre-Ville, 
Montréal, Québec, Canada, H3C 3J7


Recognized for being potent, selective, efficacious, safe and well tolerated, peptides are garnering greater interest in modern drug discovery. Challenges to improve the methods for their production and to surmount issues of peptide metabolism are being met with novel synthetic strategies and the exploration of alternative routes of drug administration. Focusing on five particular examples, this snapshot illustrates the promise of peptides for addressing unmet therapeutic challenges highlighting their importance in drug discovery today.


During the past decade, peptides have demonstrated a wide range of applications in medicine and biotechnology, and gained entrance into a broader therapeutic market. (1) The value of the global peptide drug market is on the rise and predicted to increase from US$14.1 billion in 2011 to US$25.4 billion in 2018. (2) Patients are now benefitting from over 60 peptide drugs on the market; meanwhile, hundreds of novel therapeutic peptides are in preclinical and clinical development. Current peptide-based therapies have targeted important applications such as cancer, diabetes and osteoporosis, as well as tocolytic drugs. Moreover, promising peptide candidates are in development to treat inflammation. (3) Examples of peptide-based therapeutics in development include, LCL-161 1 for treating cancer, (4) PDC31 2 for delaying preterm birth, Saxaglyptin 3 for diabetes, vascular endothelial growth factor (VEGF) inhibitor 4 to curb angiogenesis, and Teriparatide 5 for osteoporosis (Figure 1).

Smac mimetic LCL-161 for treating cancer: LCL-161 (1, Figure 1) is an orally available peptidomimetic of the tetrapeptide N-term ...

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