Precise Regulations at the Subcellular Level through Intracellular Polymerization, Assembly, and Transformation.

A living cell is an intricate machine that creates subregions to operate cell functions effectively. Subcellular dysfunction has been identified as a potential druggable target for successful drug design and therapy. The treatments based on intracellular polymerization, self-assembly, or transformation offer various advantages, including enhanced blood circulation of monomers, long-term drug delivery pharmacokinetics, low drug resistance, and the ability to target deep tissues and organelles.

Rumex japonicus Houtt. leaves: the chemical composition and anti-fungal activity.

Background: Candida albicans is a pathogenic commensal fungus. Trichophyton mentagrophytes and Trichophyton rubrum are the leading pathogens of dermatophysis. Rumex japonicus Houtt.

Bioinspired peptide/polyamino acid assemblies as quorum sensing inhibitors for the treatment of bacterial infections.

Insufficient development of new antibiotics and the rise in antimicrobial resistance are putting the world at risk of losing curative medicines against bacterial infection. Quorum sensing is a type of cellular signaling for cell-to-cell communication that plays critical roles in biofilm formation and antimicrobial resistance, and is expected to be a new type of effective target for drug resistant bacteria. In this review we highlight recent advances in bioinspired peptide/polyamino acid assemblies as quorum sensing inhibitors across various microbial communities.

Negative Differential Resistance with Ultralow Peak-to-Valley Voltage Difference in Td-WTe/2H-MoS Heterostructure.

Negative differential resistance (NDR) devices with a low peak-to-valley voltage difference (Δ) exhibit a high cut off frequency and low power consumption efficiency, which is significant for fabricating high-performance oscillators. However, achieving an ultralow Δ is challenging. In this work, we report the first construction of an NDR device utilizing a van der Waals heterostructure composed of semimetallic Td-WTe and semiconducting 2H-MoS.

Enhanced pharmacological activities of AKR1C3-activated prodrug AST-3424 in cancer cells with defective DNA repair.

AST-3424 is a novel and highly tumor-selective prodrug. AST-3424 is activated by AKR1C3 to release a toxic bis-alkylating moiety, AST 2660. In this study, we have investigated the essential role of DNA repair in AST-3424 mediated pharmacological activities in vitro and in vivo.

inhibits M2 tumor-associated macrophage polarization Wnt/β-catenin pathway modulation to suppress liver cancer.

Background: (CB), used in traditional Chinese medicine, exhibits anti-tumor effects in various cancer models. It also constitutes an integral component of a compound formulation known as Pien Tze Huang, which is indicated for the treatment of liver cancer. However, its impact on the liver cancer tumor microenvironment, particularly on tumor-associated macrophages (TAMs), is not well understood.

Food-related inhibitory control deficits in young male adults with obesity: Behavioral and ERP evidence from a food-related go/no-go task.

Purpose: Obesity poses a pervasive challenge to global public health, which is linked to adverse physical health outcomes and cognitive decline. Cognitive function, particularly food-related cognitive function, plays a critical role in sustaining a healthy weight and mitigating the progression of obesity. The aim of this study was to investigate the behavioral and neuroelectronic aspects of food-related inhibitory functions in young adult males with obesity.

P/P-Catalyzed Beckmann Reaction and Sequential [2,3]-Sigmatropic Rearrangement to Construct 2-Amidopyridines.

An organophosphorus catalytic method for the synthesis of substituted 2-amidopyridines is reported. The method employs a small-ring organophosphorus-based catalyst and a hydrosilane reductant to drive the conversion of ketoximes and pyridine--oxides into 2-amidopyridines through sequential Beckmann rearrangement followed by [2,3]-sigmatropic rearrangement. The readily available ketoximes could be activated to nitrilium ions in P/P redox catalysis and could efficiently participate in the domino reaction of pyridine--oxides, thus providing various substituted 2-amidopyridines in moderate to excellent yields.

Anisotropic sensing based on single ReSflake for VOCs discrimination.

Selective and sensitive detection of volatile organic compounds (VOCs) holds paramount importance in real-world applications. This study proposes an innovative approach utilizing a single ReSfield-effect transistor (FET) characterized by distinct in-plane anisotropy, specifically tailored for VOC recognition. The unique responses of ReS, endowed with robust in-plane anisotropic properties, demonstrate significant difference along the-axis and-axis directions when exposed to four kinds of VOCs: acetone, methanol, ethanol, and IPA.

Characterization of AST-001 non-clinical pharmacokinetics: A novel selective AKR1C3-activated prodrug in mice, rats, and cynomolgus monkeys.

AST-001 is a chemically synthesized inactive nitrogen mustard prodrug that is selectively cleaved to a cytotoxic aziridine (AST-2660) via aldo-keto reductase family 1 member C3 (AKR1C3). The purpose of this study was to investigate the pharmacokinetics and tissue distribution of the prodrug, AST-001, and its active metabolite, AST-2660, in mice, rats, and monkeys. After single and once daily intravenous bolus doses of 1.

Acute high-intensity interval exercise improves food-related cognition in young adults with obesity: An ERP study.

Cognitive function, particularly food-related cognition, is critical for maintaining a healthy weight and preventing the acceleration of obesity. High-Intensity Interval Exercise (HIIE) is an increasingly popular form of exercise and has been shown to improve physical fitness and cognitive function. However, there is limited research on the effects and underlying mechanisms of HIIE on general and food-related cognition among adults with obesity.

Discovery of a brain-permeable bromodomain and extra terminal domain (BET) inhibitor with selectivity for BD1 for the treatment of multiple sclerosis.

Multiple sclerosis (MS) is a neuroinflammatory autoimmune disease and lacks effective therapeutic agents. Dysregulation of transcription mediated by bromodomain and extra-terminal domain (BET) proteins containing two different bromodomains (BD1 and BD2) is an important factor in multiple diseases, including MS. Herein, we identified a series of BD1-biased inhibitors, in which compound 16 showed nanomolar potency for BD1 (K = 230 nM) and a 60-fold selectivity for BRD4 BD1 over BD2.

Erratum: A novel selective AKR1C3-activated prodrug AST-3424/OBI-3424 exhibits broad anti-tumor activity.

[This corrects the article on p. 3645 in vol. 11, PMID: 34354865.

A Game Model for Analyzing Wireless Sensor Networks of 5G Environment Based on Adaptive Equilibrium Optimizer Algorithm.

Wireless sensors networks (WSNs) play an important role in life. With the development of 5G, its security issues have also raised concerns. Therefore, it is an important topic to study the offense and defense confrontation in WSNs.

Enhancing NKT cell-mediated immunity against hepatocellular carcinoma: Role of XYXD in promoting primary bile acid synthesis and improving gut microbiota.

Ethnopharmacological Relevance: 'Xiayuxue decoction' (XYXD) is a traditional Chinese medicine compound, composing of three natural medicines: Rheum officinale Baill., Prunus persica (L.) Batsch and Eupolyphaga sinensis Walker.

Discovery of 1-Imidazo[4,5-]pyridine Derivatives as Potent and Selective BET Inhibitors for the Management of Neuropathic Pain.

Neuropathic pain (NP) is an intolerable pain syndrome that arises from continuous inflammation and excitability after nerve injury. Only a few NP therapeutics are currently available, and all of them do not provide adequate pain relief. Herein, we report the discovery of a selective and potent inhibitor of the bromodomain and extra-terminal (BET) proteins for reducing neuroinflammation and excitability to treat NP.

Flexible solar cells based on foldable silicon wafers with blunted edges.

Flexible solar cells have a lot of market potential for application in photovoltaics integrated into buildings and wearable electronics because they are lightweight, shockproof and self-powered. Silicon solar cells have been successfully used in large power plants. However, despite the efforts made for more than 50 years, there has been no notable progress in the development of flexible silicon solar cells because of their rigidity.

Effects of the synbiotic composed of mangiferin and 1-12 on type 2 diabetes mellitus rats.

Many synbiotics are effective for the prevention and treatment of type 2 diabetes mellitus (T2DM). In the treatment of T2DM, synbiotics often regulate the composition of intestinal flora, which autoinducer-2 (AI-2) may play an important role. Whether the changes of intestinal flora are related to AI-2 during synbiotics treatment of T2DM is a topic worth studying.

Protective effect and mechanism of Polygonatum kingianum against hypoxia-induced injury.

Background: Hypoxia is an essential cause of fatigue and aging, and is associated with the occurrence and development of many diseases. (PK) is a deficiency-nourishing Chinese herbal medicine utilized as both medicine and food, and it has long been used to ameliorate human conditions associated with fatigue and aging over 2000 years in China. PK is an important genuine-medicinal-materials cultivated in Yunnan, China, and is used by the Bai, Wa, and Zhuang nationalities as a traditional medicine for enhancing immunity, anti-fatigue, and anti-aging, while the preventive effect of PK on hypoxia-induced injury and the underlying mechanism are indefinite.

A JAK tyrosine kinase and pseudokinase Co-inhibition strategy combines enhanced potency and on-demand activation.

Janus tyrosine kinase (JAK) inhibitors have been on the market for several years, but their use is limited by drug resistance and intolerable side effects. Herein, we propose a novel strategy of JAK tyrosine kinase (TK) and pseudokinase (PK) domain co-inhibition system to consolidate robust JAK inhibition and on-demand activation. A photoexcited prodrug PAT-SIL-TG-1&AT exhibits the synergy effects of TK-PK co-inhibition and enable the spatiotemporal control of JAK2 signaling.

Fully Textured, Production-Line Compatible Monolithic Perovskite/Silicon Tandem Solar Cells Approaching 29% Efficiency.

Perovskite/silicon tandem solar cells are promising avenues for achieving high-performance photovoltaics with low costs. However, the highest certified efficiency of perovskite/silicon tandem devices based on economically matured silicon heterojunction technology (SHJ) with fully textured wafer is only 25.2% due to incompatibility between the limitation of fabrication technology which is not compatible with the production-line silicon wafer.

Effects of Acute Exercise on Cognitive Flexibility in Young Adults with Different Levels of Aerobic Fitness.

This study aimed to evaluate the effects of high-intensity interval exercise (HIIE) and moderate-intensity continuous exercise (MICE) on cognitive flexibility in young adults with differing levels of aerobic fitness. Sixty-six young adults were grouped into high- and low-fit groups based on their final running distance on the 20 m Progressive Aerobic Cardiovascular Endurance Run (PACER) test. Individuals participated in a 10 min HIIE, a 20 min HIIE, a 20 min MICE, and a control session (reading quietly in a chair) in a counterbalanced order.

The Essential Role of Executive Attention in Unconscious Visuomotor Priming.

Many reports have emphasized that unconscious processing demands attention. However, some studies were unable to observe a modulation of attentional load in subliminal visual processing. We proposed that the paradoxical phenomena could be explained based on whether the mental workload task was involved in central executive processes.