In the last century, small-molecule natural products were the main inspiration for most drug
discovery programs based either on high-throughput screening (HTS) or rational design …

With the development of modern chemistry and biology, non-proteinogenic amino acids
(NPAAs) have become a powerful tool for develo** peptide-based drug candidates. Drug …

Abstract Development of peptide drugs is challenging but also quite rewarding. Five
blockbuster peptide drugs are currently on the market, and six new peptides received first …

The high affinity and specificity of peptides towards biological targets, in addition to their
favorable pharmacological properties, has encouraged the development of many peptide …

Low bioavailability of peptides following oral administration is attributed to their inactivation
in the gastro–intestinal tract through enhanced enzymatic degradation in the gut wall by a …

The development of techniques for efficient peptide production renewed interest in peptides
as therapeutics. Numerous modifications for improving stability, transport and affinity profiles …

Despite the vast number of techniques developed for the cyclization of small peptides,
cyclization efficiency remains problematic in peptides that lack turn-promoting structures …

DNA-templated organic synthesis enables the translation, selection, and amplification of
DNA sequences encoding synthetic small-molecule libraries. Previously we described the …

The in vivo efficacy of many therapeutic peptides is hampered by their rapid proteolytic
degradation. Cyclization of these therapeutic peptides is an excellent way to render them …

Type 2 diabetes mellitus (T2DM) is increasing in global prevalence and is associated with
serious health problems (eg, cardiovascular disease). Various treatment options are …