2017
DOI: 10.1002/chem.201702119
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From Peptides to Peptidomimetics: A Strategy Based on the Structural Features of Cyclopropane

Abstract: Peptidomimetics, non-natural mimicries of bioactive peptides, comprise an important class of drug molecules. The essence of the peptidomimetic design is to mimic the key conformation assumed by the bioactive peptides upon binding to their targets. Regulation of the conformation of peptidomimetics is important not only to enhance target binding affinity and selectivity, but also to confer cell-membrane permeability for targeting protein-protein interactions in cells. The rational design of peptidomimetics with … Show more

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Cited by 52 publications
(34 citation statements)
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“…Methods for combatting biofilms using natural peptides seem promising, but their therapeutic relevance is limited by inherently low stability and availability (Kang et al, 2014 ). Therefore, antibiofilm peptidomimetics are being studied as way to mimic natural peptides while avoiding their drawbacks (Mizuno et al, 2017 ).…”
Section: Discussionmentioning
confidence: 99%
“…Methods for combatting biofilms using natural peptides seem promising, but their therapeutic relevance is limited by inherently low stability and availability (Kang et al, 2014 ). Therefore, antibiofilm peptidomimetics are being studied as way to mimic natural peptides while avoiding their drawbacks (Mizuno et al, 2017 ).…”
Section: Discussionmentioning
confidence: 99%
“…For example, poly(L-lactic acid) (PLLA) nanofibers coated with LN enhanced the attachment and proliferation of PC12 cells vs. unmodified fibers ( Figure 1B) (Koh et al, 2008). In some cases, protein fragments containing the binding domains or peptidomimetica are used for surface functionalization instead of the whole protein (Mizuno et al, 2017). Short peptidomimetics are easier to control and manipulate in comparison to the full protein for biomaterial applications.…”
Section: Biomaterials That Support Neuronal Cell Adhesionmentioning
confidence: 99%
“…Peptides have been known to have a crucial function in human physiology-act as hormones, neurotransmitters, growth factors, ion channel ligands, or anti-infective agents. Most of the discovered peptides have undesirable properties for drug application due to their low metabolic stability, low oral activity, rapid excretion, and low cell-membrane permeability (Mizuno et al 2017). Therefore, structural and functional modification of the bioactive peptide has been established to improve the pharmacokinetics drawbacks of the peptide, one of which is through the cyclization method.…”
Section: Introductionmentioning
confidence: 99%