Trypanothione reductase inhibition and anti-leishmanial activity of all-hydrocarbon stapled α-helical peptides with improved proteolytic stability
نویسندگان
چکیده
منابع مشابه
Diaminodiacid-based solid-phase synthesis of all-hydrocarbon stapled α-helical peptides.
An alternative stapling strategy is described herein using Fmoc-solid phase peptide synthesis (SPPS) that employed pre-prepared diaminodiacid building blocks to introduce all-hydrocarbon staples into peptides by on-resin cyclization. Compared to unstapled native peptides, diaminodiacid-based stapled peptides exhibited an increased α-helicity ratio and stability toward protease. Moreover, the li...
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Antimicrobial peptides are promising candidates for anti-infective pharmaceuticals. Unfortunately, because of their low proteolytic and chemical stability, their usage is generally narrowed down to topical formulations. Until now, numerous approaches to increase peptide stability have been proposed. One of them, peptide hydrocarbon stapling, a modification based on stabilizing peptide secondary...
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Protein structure underlies essential biological processes and provides a blueprint for molecular mimicry that drives drug discovery. Although small molecules represent the lion's share of agents that target proteins for therapeutic benefit, there remains no substitute for the natural properties of proteins and their peptide subunits in the majority of biological contexts. The peptide α-helix r...
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AR-23 is a melittin-related peptide with 23 residues. Like melittin, its high α-helical amphipathic structure results in strong bactericidal activity and cytotoxicity. In this study, a series of AR-23 analogues with low amphipathicity were designed by substitution of Ala1, Ala8 and Ile17 with positively charged residues (Arg or Lys) to study the effect of positively charged residue distribution...
متن کاملMolecular docking based inhibition of Trypanothione reductase activity by Taxifolin novel target for antileishmanial activity
Article history: Received on: 04/10/2012 Revised on: 16/10/2012 Accepted on: 21/10/2012 Available online: 29/10/2012 The theoretical docking study, conducted on a sample of previously reported for anti-inflammatory and antioxidant activities of Taxifolin at the binding site of Leishmania infantum trypanothione reductase (Try R) examine interaction energy. Taxifolin is widely used in the traditi...
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ژورنال
عنوان ژورنال: European Journal of Medicinal Chemistry
سال: 2018
ISSN: 0223-5234
DOI: 10.1016/j.ejmech.2018.02.071