TY - JOUR
T1 - Peptidomimetic therapeutics
T2 - scientific approaches and opportunities
AU - Qvit, Nir
AU - Rubin, Samuel J.S.
AU - Urban, Travis J.
AU - Mochly-Rosen, Daria
AU - Gross, Eric R.
N1 - Publisher Copyright: © 2016 Elsevier Ltd
PY - 2017/2/1
Y1 - 2017/2/1
N2 - 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.
AB - 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.
UR - http://www.scopus.com/inward/record.url?scp=85008257416&partnerID=8YFLogxK
U2 - https://doi.org/10.1016/j.drudis.2016.11.003
DO - https://doi.org/10.1016/j.drudis.2016.11.003
M3 - مقالة مرجعية
C2 - 27856346
SN - 1359-6446
VL - 22
SP - 454
EP - 462
JO - Drug Discovery Today
JF - Drug Discovery Today
IS - 2
ER -