GAYLE DE MARIA¹*, BRUCE H. MORIMOTO²
*Corresponding author
1. Chimica Oggi – Chemistry Today / TKS Publisher
2. Celerion, Redwood City CA 94061, USA
Member of Chimica Oggi / Chemistry Today Scientific Advisory Board

The notable expansion of peptide therapeutics in the late 1990s and 2000s led to an unprecedented number of marketing approvals in 2012, and has provided a robust pipeline that should deliver numerous approvals during the remaining decade (1). Peptides offer certain advantages as drugs; these include their high biological activity, high specificity and low toxicity. However, challenges exist for the drug development of peptide therapeutics. Obstacle number one: in general, peptides need to be parenterally delivered (via injection) because oral administration would lead to their degradation in the digestive tract. Obstacle number two: they have a short half-life because they are quickly broken down by proteolytic enzymes. Obstacle number three: their chemical nature prevents them to a large extent from getting past physiological barriers or membranes (2). That said, why has there been a renaissance with respect to peptide drugs in the pharmaceutical industry? First of all we should say that peptides often target receptors and enzymes that are difficult or impossible to access with small molecules; thereby, providing drug discovery and development of novel targets to potentially o ...