Long noncoding RNAs (lncRNAs), by virtue of their versatility and multilevel gene regulation, have emerged as attractive pharmacological targets for treating heterogeneous complex malignancies like triple-negative breast cancer (TNBC). Despite multiple studies on lncRNA functions in tumor pathology, systemic targeting these "undruggable" macromolecules with conventional approaches remains a challenge. Here, we demonstrate effective TNBC therapy nanoparticle-mediated RNAi the oncogenic DANCR,...

An enantioselective synthesis of pharmaceutically important spirobarbiturates has been achieved via spirocyclic chiral phosphine-catalyzed asymmetric [4 + 2] annulation barbiturate-derived alkenes with allenoates. With the use this tool, various spirobarbiturate-cyclohexenes are obtained in good to excellent yields diastereo- and enantioselectivities. A wide range α-substituted allenoates were tolerated.

With the use of a commercially available chiral phosphine as catalyst, first catalytic enantioselective [4 + 3] annulation allenoates with C,N-cyclic azomethine imines is developed. The reaction works efficiently under mild conditions to afford seven-membered ring-fused quinazoline-based tricyclic heterocycles in high yields good excellent diastereo- and enantioselectivities.

Abstract The bacterial KcsA channel conducts K + cations at high rates while excluding Na cations. Herein, we report an artificial ion‐channel formed by H‐bonded stacks of crown‐ethers, where cation conduction is highly preferred to macrocycles aligned along the central pore surround in a similar manner water around hydrated cation, compensating for energetic cost their dehydration. In contrast, does not fit macrocyclic binding sites, so its dehydration completely compensated. present...

Phosphine-catalyzed [2 + 4] annulation of allenoates with thiazolone-derived alkenes has been achieved under mild conditions, giving biologically important 6,7-dihydro-5H-pyrano[2,3-d]thiazole derivatives in high to excellent yields. With the use Kwon's phosphine as chiral catalyst, optically active products were obtained good yields enantioselectivities.

Abstract A multifunctional chiral phosphine‐catalyzed enantioselective [3+2] annulation of Morita–Baylis–Hillman carbonates with barbiturate‐derived alkenes has been achieved under mild conditions, providing a variety spirobarbiturate‐cyclopentenes in moderate to excellent yields diastereo‐ and enantioselectivities. magnified image

Abstract Artificial Water Channels (AWCs) have been developed during the last decade with hope to construct artificial analogues of Aquaporin (AQP) proteins. Their osmotic water permeability are in range natural transporters, making them suitable candidates that can potentially transport at lower energy and operating cost. Compared AQPs, AWCs would several potential advantages, such as improved stability, simple scalable fabrication higher functional density when confined 2D membrane arrays....

An artificial selective K+ channel is formed from the supramolecular organization on bis(benzo-15-crown-5- ether-ureido)-pillar[5]arene compound. This achieves a selectivity of SK+/Na+ = 5 for an initial transport rate kK+ 3.2 × 10–3 s–1. The cation-file diffusion occurs via macrocyclic-filters anchored inactive supporting pillar[5]arene relays. sandwich-type binding geometry cation by two 15-crown-5 moieties sites key feature influencing efficiency.

Abstract A phosphane‐catalyzed [3+3] annulation of azomethine imines with ynones has been developed. Under mild reaction conditions, the proceeds smoothly to afford tricyclic dinitrogen‐fused heterocyclic compounds in moderate excellent yields stereoselectivies. Using a chiral phosphine as catalyst, could work give cycloadduct yield enantioselectivity. magnified image

The natural KcsA K+ channel, one of the best-characterized biological pore structures, conducts cations at high rates while excluding Na+ cations. channel is primordial inspiration for design artificial channels. Important progress in improving conduction activity and /Na+ selectivity has been achieved with ion-channel systems. However, simple systems exhibiting mimicking biofunctions are unknown. Herein, an ion formed by H-bonded stacks squalyl crown ethers, which highly preferred to...

Abstract With the use of a bifunctional chiral phosphine as catalyst, asymmetric [3+2] annulation Morita–Baylis–Hillman carbonates with cyclic 1‐azadienes proceeded smoothly under mild conditions to give various enantiomerically enriched cyclopentene derivatives bearing three consecutive tertiary stereocenters and sulfamate moiety in moderate excellent yields enantioselectivities diastereoselectivities. magnified image

CRISPR/Cas9 system is a promising approach for gene editing in therapy. Effective requires safe and efficient delivery of target cells. Several new multifunctional pH-sensitive amino lipids were designed synthesized with modification the head groups intracellular system. These exhibited structurally dependent formulation stable nanoparticles DNA plasmids sizes ranging from 100 to 200 nm. The lipid plasmid showed hemolysis minimal hemolytic activity at pH 7.4 increased acidic (pH = 5.5, 6.5)....

A novel water-soluble perylene bisimide derivative 1 was synthesized with two permethyl-β-cyclodextrin grafts at the imide nitrogens, and its structure identified by NMR, Fourier transform infrared spectroscopy (FT-IR), matrix-assisted laser desorption ionization mass spectrometry (MALDI-MS), elemental analysis. Its aggregation behavior in water organic solutions further investigated UV−vis, fluorescence, 1H NMR spectra, showing that exhibits strong π···π water. Especially, optical...

Event detection plays an essential role in video content analysis. In this paper, we present our approach based on motion relativity and feature selection for event detection. First, propose a new feature, namely Expanded Relative Motion Histogram of Bag-of-Visual-Words (ERMH-BoW) to employ ERMH-BoW, by representing what aspect with (BoW), construct relative histograms between different visual words depict the objects' activities or how event. ERMH-BoW thus integrates both aspects complete...

Abstract The bacterial KcsA channel conducts K + cations at high rates while excluding Na cations. Herein, we report an artificial ion‐channel formed by H‐bonded stacks of crown‐ethers, where cation conduction is highly preferred to macrocycles aligned along the central pore surround in a similar manner water around hydrated cation, compensating for energetic cost their dehydration. In contrast, does not fit macrocyclic binding sites, so its dehydration completely compensated. present...

A naphthylthiourea-modified cyclodextrin (1) and its urea derivative (2) were synthesized, their fluorescence behaviors in the presence of various metal ions investigated. Significantly, 1 showed a highly sensitive selective sensing ability for Hg2+ over other both water living cells. That is, addition to an aqueous solution gave significantly enhanced at ∼380 nm. In contrast, induced negligible changes. The possible mechanism may be due transformation thiourea by Hg2+-induced desulfurization water.

Abstract Pillar[n]arenes have been intensively used during the last decade in supramolecular chemistry as host systems for guest recognition and self‐assembly, toward functional materials devices. They present electron‐rich tuneable size cavities, well reactive rims further functionalization. Their unique pillar shape promotes pillar[n]arenes molecular analogues of carbon nanotubes. For this reasons embedded into membranes to construct artificial water, proton, ions channels. This review...

Nanoparticle based siRNA formulations often suffer from aggregation and loss of function during storage. We in this study report a frozen targeted RGD-polyethylene glycol (PEG)-ECO/siβ3 nanoparticle formulation with prolonged shelf life preserved functionality. The RGD-PEG-ECO/siβ3 nanoparticles are formed by step-wised self-assembly RGD-PEG-maleimide, ECO, siRNA. have diameter 224.5 ± 9.41 nm zeta potential to 45.96 3.67 mV water size 234.34 3.01 near neutral saline solution. addition...

[4 + 3] cycloaddition of phthalazinium dicyanomethanides with in situ formed azoalkenes was achieved, providing an access to various 1,2,4-triazepine derivatives moderate excellent yields.