Modulating ion channel properties of transmembrane peptide nanotubes through heteromeric supramolecular assemblies

A selective heteromeric supramolecular assembly process is devised to create functional single channels of altered ion conductance, charge selectivity, and rectification. The hollow transmembrane tubular structure produced spontaneously from the self-assembly of cyclic-d,l-alpha-peptides in lipid bilayers is modified by designer cyclic peptide "cap" subunits that bind site-selectively at the mouth of the channel assembly.     

Heterocyclic peptide backbone modifications in an alpha-helical coiled coil

In this paper, we present 1,2,3-triazole epsilon2-amino acids incorporated as a dipeptide surrogate at three positions in the sequence of a known alpha-helical coiled coil. Biophysical characterization indicates that the modified peptides retain much of the helical structure of the parent sequence, and that the thermodynamic stability of the coiled coil depends on the position of the incorporation of the epsilon-residue. Crystal structures obtained for each peptide give insight into the chemical behavior and conformational preferences of the non-natural amino acid and show that the triazole ring can participate in the backbone hydrogen bonding of the alpha-helix as well as template an interhelical crossing between chains in the bundle.     

Discovery of a biologically active thiostrepton fragment

Design, synthesis, and biological evaluation of several domains of the thiopeptide antibiotic thiostrepton led to the discovery of a biologically active fragment. The biological properties of this novel small organic molecule include antibiotic activity against methicillin-resistant Staphylococcus aureus (MRSA) and vancomycin-resistant Enterococcus faecalis (VREF) bacterial strains, as well as cytotoxic action against a number of cancer cell lines.     

Numerical methods for solving singular integral equations obtained by fracture mechanical analysis of cracked wedge简

The numerical solutions to the singular integral equations obtained by the fracture mechanical analyses of a cracked wedge under three different conditions are considered. The three considered conditions are: (i) a radial crack on a wedge with a non-finite radius under the traction-traction boundary condition, (ii) a radial crack on a wedge with a finite radius under the traction-traction boundary condition, and (iii) a radial crack on a finite radius wedge under the traction-displacement boundary condition. According to the boundary conditions, the extracted singular integral equations have different forms. Numerical methods are used to solve the obtained coupled singular integral equations, where the Gauss-Legendre and the Gauss-Chebyshev polynomials are used to approximate the responses of the singular integral equations. The results are presented in figures and compared with those obtained by the analytical response. The results show that the obtained Gauss-Chebyshev polynomial response is closer to the analytical response.