Peptidomimetic therapeutics: scientific approaches and opportunities

Nir Qvit, Samuel J.S. Rubin, Travis J. Urban, Daria Mochly-Rosen, Eric R. Gross

Research output: Contribution to journalReview articlepeer-review

197 Scopus citations


Natural endogenously occurring peptides exhibit desirable medicinal properties, but are often limited in application by rapid proteolysis and inadequate membrane permeability. However, editing naturally occurring peptide sequences to develop peptidomimetic analogs created a promising class of therapeutics that can augment or inhibit molecular interactions. Here, we discuss a variety of chemical modifications, including L to D isomerization, cyclization, and unnatural amino acid substitution, as well as design strategies, such as attachment to cell-penetrating peptides, which are used to develop peptidomimetics. We also provide examples of approved peptidomimetics and discuss several compounds in clinical trials.

Original languageEnglish
Pages (from-to)454-462
Number of pages9
JournalDrug Discovery Today
Issue number2
StatePublished - 1 Feb 2017
Externally publishedYes

Bibliographical note

Publisher Copyright:
© 2016 Elsevier Ltd


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