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Effect of Macromolecular Architecture on Adhesion.
Langmuir
January 2025
Physics Department, Lomonosov Moscow State University, Moscow 119991, Russian Federation.
The behavior of single linear chains on a substrate is a well-studied area of polymer science. Herein, one of the most essential issues is the interaction of the chains with the substrate, which determines both macromolecular conformations near the substrate and adhesive properties of polymer materials. However, very little is known about the effect of macromolecular architecture on adhesion.
View Article and Find Full Text PDFThe Dual Mode of Antibacterial Action of the Synthetic Small Molecule DCAP Involves Lipid II Binding.
J Am Chem Soc
September 2024
Institute for Pharmaceutical Microbiology, University of Bonn, University Hospital Bonn, Meckenheimer Allee 168, 53115 Bonn, Germany.
The synthetic small molecule DCAP is a chemically well-characterized compound with antibiotic activity against Gram-positive and Gram-negative bacteria, including drug-resistant pathogens. Until now, its mechanism of action was proposed to rely exclusively on targeting the bacterial membrane, thereby causing membrane depolarization, and increasing membrane permeability (Eun 2012, 134 (28), 11322-11325; Hurley 2015, 6, 466-471). Here, we show that the antibiotic activity of DCAP results from a dual mode of action that is more targeted and multifaceted than previously anticipated.
View Article and Find Full Text PDFOutstanding Superoxide Dismutase Catalytic Activity Of Simple Peptide-Based Nickel(II) Complexes.
Angew Chem Int Ed Engl
October 2024
Univ. Grenoble Alpes, CEA, CNRS, Grenoble INP, IRIG, SyMMES, 38000, Grenoble, France.
We present here the most active synthetic Ni superoxide dismutase (NiSOD) mimic reported to date. Reactive oxygen species are aggressive compounds, which concentrations are tightly regulated in vivo. Among them, the superoxide anion, O⋅, is controlled by superoxide dismutases.
View Article and Find Full Text PDFDevelopment of a natural product optimization strategy for inhibitors against MraY, a promising antibacterial target.
Nat Commun
June 2024
Faculty of Pharmaceutical Sciences, Hokkaido University, Kita-12, Nishi-6, Kita-ku, Sapporo, 060-0812, Japan.
Article Synopsis
- MraY inhibitory natural products are promising candidates for new antibacterial treatments, especially against drug-resistant bacteria, but improving their properties through chemical modifications is challenging due to complex synthesis processes.
- A new strategy has been developed to efficiently create and evaluate a library of 686 MraY analogue compounds, allowing for streamlined preparation and direct assessment of their biological activities.
- This research identifies several potent analogues that are effective against drug-resistant strains and reveals unique binding patterns with MraY, while also demonstrating the method's applicability to other natural products targeting tubulin activities.
Peptide recognition by a synthetic receptor at subnanomolar concentrations.
Chem Sci
April 2024
Department of Chemistry, Trinity University 1 Trinity Place San Antonio TX 78212 USA
This paper describes the discovery and characterization of a dipeptide sequence, Lys-Phe, that binds to the synthetic receptor cucurbit[8]uril (Q8) in neutral aqueous solution with subnanomolar affinity when located at the N-terminus. The thermodynamic and structural basis for the binding of Q8 to a series of four pentapeptides was characterized by isothermal titration calorimetry, NMR spectroscopy, and X-ray crystallography. Submicromolar binding affinity was observed for the peptides Phe-Lys-Gly-Gly-Tyr (FKGGY, 0.
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