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Diamide insecticides with high efficacy against pests and good environmental safety are broadly applied in crop protection. They act at a poorly-defined site in the very complex ryanodine (Ry) receptor (RyR) potentially accessible to a fluorescent probe. Two N-propynyl analogs of the major anthranilic diamide insecticides chlorantraniliprole (Chlo) and cyantraniliprole (Cyan) were accordingly synthesized and converted into two fluorescent ligands by click reaction coupling with 3-azido-7-hydroxy-2H-chromen-2-one. The new diamide analogs and fluorescent ligands were shown to be nearly as potent as Chlo and Cyan in inhibition of [3H]Chlo binding and stimulation of [3H]Ry binding in house fly thoracic muscle RyR. Although the newly synthesized compounds had only moderate activity in insect larvicidal activity assays, their high in vitro potency in a validated insect RyR binding assay encourages further development of fluorescent probes for insect RyRs.

To describe the pharmacokinetics/pharmacodynamics (PK/PD) of a 2 h infusion of ceftazidime‐avibactam (CAZ‐AVI) in critically ill patients with augmented renal clearance (ARC). A retrospective review of all critically ill patients with ARC who were treated with CAZ‐AVI between August 2020 and May 2023 was conducted. Patients whose 12‐h creatinine clearance prior to CAZ‐AVI treatment and steady‐state concentration (Css) of CAZ‐AVI were both monitored were enrolled. The free fraction (fCss) of CAZ‐AVI was calculated from Css. The joint PK/PD targets of CAZ‐AVI were considered optimal when a Css/minimum inhibitory concentration (MIC) ratio for CAZ ≥4 (equivalent to 100% fT > 4 MIC) and a Css/CT ratio of AVI >1 (equivalent to 100% fT > CT 4.0 mg/L) were reached simultaneously, quasioptimal when only one of the two targets was reached, and suboptimal when neither target was reached. The relationship between PK/PD goal achievement, microbial eradication and the clinical efficacy of CAZ‐AVI was evaluated. Four patients were included. Only one patient achieved optimal joint PK/PD targets, while the other three reached suboptimal targets. The patient with optimal PK/PD targets achieved microbiological eradication, while the other three patients did not, but all four patients achieved good clinical efficacy. Standard dosages may not enable most critically ill patients with ARC to reach the optimal joint PK/PD targets of CAZ‐AVI. Optimal drug dose adjustment of CAZ‐AVI in ARC patients requires dynamic drug concentration monitoring. [ABSTRACT FROM AUTHOR]

Simple Summary: The diamondback moth, Plutella xylostella (L.), is an important migratory insect pest worldwide. In this study, the effects of environmental parameters, age, nutritional supplementation and sex on the wingbeat frequency of the insect adult were measured in the laboratory, and the results showed that nutritional status, sex and ambient temperature modulate the wingbeat frequency of the moth. These findings can be helpful for further understanding flight biology of the insect as well as to improve the accuracy using insect radar facility to directly identify migrating moths based on species difference of wingbeat frequency. The diamondback moth, Plutella xylostella L. (Lepidoptera: Plutellidae), is a cosmopolitan horticultural pest that is undergoing a fast, climate-driven range expansion. Its wide geographic distribution, pest status, and high incidence of insecticide resistance are directly tied to long-distance migration. Wingbeat frequency (WBF) is a key aspect of P. xylostella migratory behavior, but has received limited scientific attention. Here, we investigated the effects of environmental parameters, age, adult nutrition, and sex on P. xylostella WBF. Across experimental regimes, WBF ranged from 31.39 Hz to 78.87 Hz. Over a 10–35 °C range, the WBF of both male and female moths increased with temperature up to 62.96 Hz. Though male WBF was unaffected by humidity, females exhibited the highest WBF at 15% relative humidity (RH). WBF was unaffected by adult age, but adult nutrition exerted important impacts. Specifically, the WBF of moths fed honey water (54.66 Hz) was higher than that of water-fed individuals (49.42 Hz). Lastly, males consistently exhibited a higher WBF than females. By uncovering the biological and (nutritional) ecological determinants of diamondback moth flight, our work provides invaluable guidance to radar-based monitoring, migration forecasting, and the targeted deployment of preventative mitigation tactics. [ABSTRACT FROM AUTHOR]

Protein kinases play an important role in every aspect of cellular life. In this study, we systemically identified protein kinases from the predicted proteomes of 59 representative fungi from Ascomycota and Basidiomycota. Comparative analysis revealed that fungi from Ascomycota and Basidiomycota differed in the number and variety of protein kinases. Some groups of protein kinases, such as calmodulin/calcium regulated kinases (CMGC) and those with the highest group percentages are the most prevalent protein kinases among all fungal species tested. In contrast, the STE group (homologs of the yeast STE7, STE11 and STE20 genes), was more abundant in Basidiomycetes than in Ascomycetes. Importantly, the distribution of some protein kinase families appeared to be subphylum-specific. The tyrosine kinase-like (TKL) group had a higher protein kinase density in Agaricomycotina fungi. In addition, the distribution of accessory domains, which could have functional implications, demonstrated that usage bias varied between the two phyla. Principal component analysis revealed a divergence between the main functional domains and associated domains in fungi. This study provides novel insights into the variety and expansion of fungal protein kinases between Ascomycota and Basidiomycota.

Deformation monitoring is one of the most important means of providing feedback to ensure the safety of projects. Problems plague the existing automatic monitoring system, such as the small monitoring range of monitoring devices, the inadequate field safety protection, and the low accuracy under extreme weather conditions. These problems greatly reduce the real time and reliability of deformation monitoring data and restrict the real-time intelligent control of engineering safety risk. In this paper, a multitype instrument-integrated monitoring system based mainly on the total positioning station (TPS) and supplemented by the Global Navigation Satellite System (GNSS) was promoted with the methods of large field angle, data complementation, environmental perception and judgment, automatic status control, and baseline calibration-meteorological fusion correction. The application results of Pubugou Station show that the averages of mean square error of points (APMSE) for the dam are 0.41∼1.65 mm and the averages of mean square error of height (AHMSE) are 0.42∼0.89 mm. Moreover, the APMSE and AHMSE for the slope are less than 3 mm. The maximum relative error of the TPS and GNSS data compared with the artificial monitoring data is less than 10%. Besides, the system has good overall performance and is of significant comprehensive benefits. The proposed system realizes the all-weather real-time monitoring of deformation and enhances the emergency response capability of special conditions in dams during the operation period.