Strategies for transitioning macrocyclic peptides to cell-permeable drug leads.

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ID: 14386
2017
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Abstract
The ready availability of potent peptide binders for any desired target highlights their potential impact as therapeutic agents. Despite their versatility, however, peptides tend to display unfavourable pharmacological properties, such as low bioavailability, high renal clearance and proteolytic degradation rates, and low cell permeability. Fortunately, an increasing number of promising strategies to produce novel peptides and furnish pre-existing scaffolds with more drug-like properties are now becoming available. These strategies include incorporation of non-proteinogenic amino acids, tag appendage to existing peptides and grafting onto scaffolds already possessing desirable pharmacokinetic properties. As a consequence, a variety of promising bioactive macrocyclic peptides have recently been discovered highlighting the promise of this class of molecules as future medicines.
Reference Key
walport2017strategiescurrent Use this key to autocite in the manuscript while using SciMatic Manuscript Manager or Thesis Manager
Authors Walport, Louise J;Obexer, Richard;Suga, Hiroaki;
Journal current opinion in biotechnology
Year 2017
DOI
S0958-1669(17)30046-0
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