Peptidomimetic therapeutics: scientific approaches and opportunities

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

doi:10.1016/j.drudis.2016.11.003

Peptidomimetic therapeutics: scientific approaches and opportunities

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

Stanford University

Research output: Contribution to journal › Review article › peer-review

218 Scopus citations

Abstract

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 language	English
Pages (from-to)	454-462
Number of pages	9
Journal	Drug Discovery Today
Volume	22
Issue number	2
DOIs	https://doi.org/10.1016/j.drudis.2016.11.003
State	Published - 1 Feb 2017
Externally published	Yes

Bibliographical note

Publisher Copyright:
© 2016 Elsevier Ltd

Funding

This review was supported by NIH HL52141 (D.M.R.), NIH HL109212 (E.R.G.), Stanford University SPARK (N.Q.), and Stanford Graduate Fellowship (S.J.S.R.).

Funders	Funder number
Stanford University SPARK
National Institutes of Health	HL52141
National Heart, Lung, and Blood Institute	R00HL109212

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10.1016/j.drudis.2016.11.003

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Peptidomimetic therapeutics: scientific approaches and opportunities

Abstract

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