The Current State of Peptide Drug Discovery: Back to the Future?

Antoine Henninot, James C Collins, John M Nuss,


Journal of medicinal chemistry, July 24, 2017


Over the last decade, peptide drug discovery has experienced a revival of interest and scientific momentum, as the pharmaceutical industry has come to appreciate the role that peptide therapeutics can play in addressing unmet medical needs, and how this class of compounds can be an excellent complement or even preferable alternative to small molecule and biological therapeutics. In this perspective we give a concise description of the recent progress in peptide drug discovery in a holistic manner, highlighting enabling technological advances affecting nearly every aspect of this field: from lead discovery, to synthesis and optimization, to peptide drug delivery. An emphasis is placed on describing research efforts to overcome the inherent weaknesses of peptide drugs, in particular their poor pharmacokinetic properties, and how these efforts have been critical to the discovery, design and subsequent development of novel therapeutics.


Pubmed Link: 28737935

DOI: 10.1021/acs.jmedchem.7b00318