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 21st 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.
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