Thioether Analogues of Disulfide‐Bridged Cyclic Peptides Targeting Death Receptor 5: Conformational Analysis,Dimerisation and Consequences for Receptor Activation

Cyclic peptides containing redox‐stable thioether bridges might provide a useful alternative to disulfide‐bridged bioactive peptides. We report the effect of replacing the disulfide bridge with a lanthionine linkage in a 16‐mer cyclic peptide that binds to death receptor 5 (DR5, TRAIL‐R2). Upon covalent oligomerisation, the disulfide‐bridged peptide has previously shown similar behaviour to that of TNF‐related apoptosis inducing ligand (TRAIL), by selectively triggering the DR5 cell death pathway. The structural and biological properties of the DR5‐binding peptide and its desulfurised analogue were compared. Surface plasmon resonance (SPR) data suggest that these peptides bind DR5 with comparable affinities. The same holds true for dimeric versions of these peptides: the thioether is able to induce DR5‐mediated apoptosis of BJAB lymphoma and tumorigenic BJELR cells, albeit to a slightly lower extent compared to its disulfide homologue. NMR analysis revealed subtle variation in the conformations of the two peptides and suggests that the thioether peptide is slightly less folded than its disulfide homologue. These observations could account for the different capability of the two dimers to cluster DR5 receptors on the cell surface and to trigger apoptosis. Nevertheless, our results suggest that the thioether peptide is a potential candidate for evaluation in animal models.     

Systematic literature review on city logistics: overview,classification and analysis

City logistics is one of the significant branches of supply chain management, dealing with the logistics and transportation activities in urban areas. This research area has recently appropriated an exponential growth of publications. This paper presents a bibliometric analysis along with a systematic literature review to organise the results of surveying more than 370 papers and research works published since 2010. We identify the top contributing research topics. The most common keywords used in the city logistics literature are referred to in order to propose six research categories identifying the main innovative research perspectives.     

Evaluation of in-air hand gestures interaction for older people

Universal Access in the Information Society - In-air gestural interfaces are gaining popularity due to the increasing availability and low cost of gesture recognition hardware. However, the current...     

Parameters effect on proton conductivity to obtain chitosan membranes for use as electrolytes in PEMFC

The chitosan biopolymer can be used as a proton‐conducting membrane in proton‐exchange membrane fuel cell. In the forms that they have normally obtained and tested, chitosan membranes typically show poor performance in conduction of protons, requiring modifications in the structure of the biopolymer or blending with other polymers to increase its proton conductivity. The present work investigates the individual properties of chitosan and relates them to the proton conductivity performance of membranes composed of this polymer. Evaluation was made of the effects of variables such as the degree of deacetylation (DD) and the molar mass (Mv) of chitosan membranes without addition of any other polymer. The DD and Mv values of the chitosan used to produce membranes determined the proton conduction, with lower DD and higher Mv resulting in higher conductivity. The thicker membranes presented greater crystallinity, with conductivity between 2.0 × 10^?4 and 1.8 × 10^?3 S cm^?1. The characteristic stages of degradation of the chitosan membranes were in the ranges 200 to 300°C and 500 to 600°C, indicating good thermal stability of the material.