Identification of Novel Fragments Binding to the PDZ1-2 Domain of PSD-95

Inhibition of PSD-95 has emerged as a promising strategy for the treatment of ischemic stroke, as shown with peptide-based compounds that target the PDZ domains of PSD-95. In contrast, developing potent and drug-like small molecules against the PSD-95 PDZ domains has so far been unsuccessful. Here, we explore the druggability of the PSD-95 PDZ1-2 domain and use fragment screening to investigate if this protein is prone to binding small molecules. We screened 2500 fragments by fluorescence polarization (FP) and validated the hits by surface plasmon resonance (SPR), including an inhibition counter-test, and found four promising fragments. Three ligand efficient fragments were shown by ¹H,¹⁵N HSQC NMR to bind in the small hydrophobic P⁰ pockets of PDZ1-2, and one of them underwent structure-activity relationship (SAR) studies. Overall, we demonstrate that fragment screening can successfully be applied to PDZ1-2 of PSD-95 and disclose novel fragments that can serve as starting points for optimization towards small-molecule PDZ domain inhibitors.     

M2M energy saving strategy in 5G millimeter wave system

Telecommunication Systems - Machine to Machine technology has a broad application prospect in the 5G network, but there is a bottleneck in the energy consumption of intelligent devices powered by...     

Electrodeposition of B,Ni co-doped diamond-like carbon films on AZ91D magnesium alloy: Corrosion and wear resistance

Diamond-like carbon (DLC) possesses brilliant and excellent properties, including excellent corrosion resistance as well as outstanding wear resistance. Ni and B co-doped DLC films were deposited on AZ91D magnesium alloy by electrodeposition under mild conditions (300 V and 25°C). Uniform and dense morphology of co-doped DLC films were observed, and Ni and B were uniformly incorporated into the carbon-based films. Among all the electrodeposits, the appearance of D and G peaks near 1330 and 1570 cm⁻¹ revealed that the as-deposited films were typical DLC films. As the addition of Ni was increased to 0.05 g, the highest microindentation hardness, the lowest friction coefficient, and wear loss were achieved to be 164.5 HV, 0.3, and 0.6 × 10⁻⁵ kg/m, respectively. The amorphous carbon films fabricated at 0.05 g Ni had the lowest corrosion current density and the most positive corrosion potential, which was mainly due to the small and dense granular structure effectively hindering the penetration of corrosion media.     

A Biologically Muscle-Inspired Polyurethane with Super-Tough,Thermal Reparable and Self-Healing Capabilities for Stretchable Electronics

Polymeric elastomers play an increasingly important role in the development of stretchable electronics. A highly demanded elastic matrix is preferred to own not only excellent mechanical properties, but also additional features like high toughness and fast self-healing. Here, a polyurethane (DA-PU) is synthesized with donor and acceptor groups alternately distributed along the main chain to achieve both intra-chain and inter-chain donor-acceptor self-assembly, which endow the polyurethane with toughness, self-healing, and, more interestingly, thermal repair, like human muscle. In detail, DA-PU exhibits an amazing mechanical performance with elongation at break of 1900% and toughness of 175.9 MJ m⁻³. Moreover, it shows remarkable anti-fatigue and anti-stress relaxation properties as manifested by cyclic tensile and stress relaxation tests, respectively. Even in case of large strain deformation or long-time stretch, it can almost completely restore to original length by thermal repair at 60 °C in 60 s. The self-healing speed of DA-PU is gradually enhanced with the increasing temperature, and can be 1.0–6.15 µm min⁻¹ from 60 to 80 °C. At last, a stretchable and self-healable capacitive sensor is constructed and evaluated to prove that DA-PU matrix can ensure the stability of electronics even after critical deformation and cut off.     

Effect of nitriding atmosphere on the morphology of AlN nanofibers from solution blow spinning

High purity AlN fiber is a promising thermal conductive material. In this work, AlN fibers were prepared using solution blow spinning followed by nitridation under N₂ or NH₃ atmosphere. Soluble polymer, such as polyaluminoxane, and allyl-functional novolac resin were adopted as raw materials to form homogeneous distribution of Al₂O₃ and C nanoparticles within the fibers, which could inhibit the growth of alumina crystal and promote their nitridation process. The effect of nitriding atmosphere on the fiber morphology was investigated. XRD results showed that complete nitridation was achieved at 1300 °C in the NH₃ or at 1500 °C in the N₂ atmosphere. Hollowed fiber structure was observed when fiber was nitrided in N₂ at high temperature, which was caused by gaseous Al gas diffusion, and this phenomenon was eliminated in NH₃ atmosphere. The nitridation mechanisms in different atmosphere were analyzed in detail. It was demonstrated that the nitridation of Al₂O₃ fibers in the NH₃ atmosphere offered the favored AlN morphology and chemical quality. Flexible AlN fiber with O content of 0.7 wt% was achieved after nitriding in NH₃ at 1400 °C. The high quality AlN can be used in thermal conductive composite materials.     

Superior Low-Temperature Reversible Adhesion Based on Bio-Inspired Microfibrillar Adhesives Fabricated by Phenyl Containing Polydimethylsiloxane Elastomers

Gecko-inspired microfibrillar adhesives have achieved great progress in microstructure design and adhesion improvement over the past two decades. Space applications nowadays show great interest in this material for the characteristics of reversible adhesion and universal van der Waals interactions. However, the impact of harsh environment of space on the performance of microfibrillar adhesives, especially the extreme low temperature, is rarely addressed. Herein, microfibrillar adhesives fabricated by phenyl containing polydimethylsiloxane (p-PDMS) elastomers with superior low-temperature reversible adhesion is proposed. p-PDMS elastomers are synthesized through one-pot anionic ring-opening copolymerization, and the resulting elastomers become non-crystallizable with excellent low-temperature elasticity. Low-temperature adhesion tests demonstrate that the adhesion strength of microfibrillar adhesives fabricated by p-PDMS elastomers can be well maintained to as low as −120 °C. In contrast, the adhesion strength of pure PDMS microfibrillar adhesive reduces more than 50% below its crystallization temperature. The low-temperature cyclic adhesion tests further demonstrate that p-PDMS microfibrillar adhesives exhibit superior reversible adhesion compared to that of PDMS microfibrillar adhesives, owing to the sustainable conformal contact and even distribution of loads over repeated cycles. This study provides a new fabrication strategy for microfibrillar adhesives, and is beneficial for the practical application of microfibrillar adhesives.     

Tunable multicolor upconversion luminescence of Yb3+ sensitized Na3La(VO4)2 crystals

Multicolor upconversion luminescence materials show significantly applications in materials science. In this paper, the novel Yb³⁺-sensitized Na₃La(VO₄)₂ upconversion luminescence crystals are synthesized by the solid-state reaction method. Three primary colors upconversion luminescence are successfully achieved in Na₃La(VO₄)₂:Yb³⁺,Tm³⁺, Na₃La(VO₄)₂:Yb³⁺,Er³⁺, and Na₃La(VO₄)₂:Yb³⁺,Ho³⁺ crystals excited by the single 980 nm LD. Multicolor upconversion luminescence can be obtained by simply adjusting the combination ratios of these three samples. Luminescence mechanisms of the Yb³⁺-sensitized system are discussed in detail. In the Na₃La(VO₄)₂ host material, the Yb³⁺/Ho³⁺ codoped system exhibits unusual red upconversion luminescence based on the short decay time of Ho³⁺ ion ⁵I₆ level, which provides the possibility of three primary color luminescence under 980 nm excitation.     

Stable Radicals with Protective Umbrellas Integrated on the Surface of 2D Layered Materials

Radicals are closely related to human life and health and have been widely used in biology, chemistry, functional materials, etc. However, the high reactivity, disorder, and short half-lives limit their wide applications. Therefore, it remains a great challenge to prepare stable and ordered radicals. Herein, radicals are prepared with protective umbrellas (diethylmethyleneamine, DEMA) that are integrated on the surface of 2D layered materials to isolate water and oxygen and enhance the stability of radicals. Taking 2D black phosphorus (BP) as an example: triethylamine reacts with dichloromethane to form quaternary ammonium salts with further Hoffmann elimination to produce DEMA radicals that could react with one electron of a lone pair electrons in P on the surface of BP to produce P radicals, which shows a prolonged half-life of 21 days at room temperature. First-principle calculations and electron paramagnetic resonance fitting confirm that the steric hindrance constructed by dense DEMA passivation layer acts as a protective umbrella and the 2D coupling of P radicals and other P atoms in 2D BP plane to enhance the stability and strong superexchange interaction of P radicals. Furthermore, it is a general strategy to produce stable radicals integrated on the 2D plane.     

Preparation and electrochemical characterization of Ti-based amorphous metallic glass with high strength

Ti-based amorphous metallic glasses have excellent mechanical, physical, and chemical properties, which is an important development direction and research hotspot of metal composite reinforcement. As a stable, simple, efficient, and large-scale preparation technology of metallic powders, the gas atomization process provides an effective way of preparing amorphous metallic glasses. In this study, the controllable fabrication of a Ti-based amorphous powder, with high efficiency, has been realized by using gas atomization. The scanning electron microscope, energy-dispersive spectrometer, and X-ray diffraction are used to analyze surface morphology, element distribution, and phase structure, respectively. A microhardness tester is used to measure the mechanical property. An electrochemical workstation is used to characterize corrosion behavior. The results show that as-prepared microparticles are more uniform and exhibit good amorphous characteristics. The mechanical test shows that the hardness of amorphous powder is significantly increased as compared with that before preparation, which has the prospect of being an important part of engineering reinforced materials. Further electrochemical measurement shows that the corrosion resistance of the as-prepared sample is also significantly improved. This study has laid a solid foundation for expanding applications of Ti-based metallic glasses, especially in heavy-duty and corrosive domains.     

Swarming Microdroplets to a Dexterous Micromanipulator

Many astonishing biological collective behaviors exist in nature, and artificial microrobotic swarms have been developed by emulating these scenarios. However, these microswarms typically have single structures and lack the adaptability that many biological swarms exhibit to thrive in complex environments. Inspired by viscoelastic fire ant aggregations and using a combination of experiment and simulation, a strategy to trigger ferrofluid droplets into forming microswarms exhibiting both liquid-like and solid-like behaviors is reported. By spatiotemporally programming an applied magnetic field, microswarms can be liquefied to implement reversible elongation with a high aspect ratio and solidified into entireties to perform overturning and bending behaviors. It is demonstrated that reconfigurability enables the microswarm to be a mobile dexterous micromanipulator, acting not only as a soft “octopus arm” to explore a confined environment and grasp a targeted object but also adaptively navigate multiple terrains, such as uneven surfaces, curved grooves, complex mazes, high steps, narrow channels, and even wide gaps. This microrobotic swarm can reconfigure both shapes and tasks based on the demands of the environment, presenting novel solutions for a variety of applications.