Abstract

Peptide drugs have received more attention as potential next-generation drugs or drug leads. Such attention is primarily due to the higher target selectivities and efficiencies of peptide drugs. Moreover, peptide drugs typically have lower accumulation rates and toxicities. Although peptide drugs have advanced significantly in the 21^st century, two bottlenecks (disadvantages) primarily hinder peptide drug research and development compared to small molecule drugs. One bottleneck is the identification of a valuable peptide in a complicated pool of crude products; the other bottleneck is the ability to prepare sufficient amounts of peptides for preclinical or clinical trials. This review discusses important methodologies for addressing these two bottlenecks.

Keywords: Extracellular expression, intracellular expression, in vitro screening, in vivo screening, methodology, peptide.

Graphical Abstract