Genes (Basel)
December 2024
Background/objectives: is distributed in Korea, China, and Japan. It was first identified as the genus and then reclassified as by Kitagawa. Some species are used as herbal medicine and are often confused with the similar form .
View Article and Find Full Text PDFDue to its essential roles in cell proliferation and apoptosis, the precise regulation of the Hippo pathway through LATS presents a viable biological target for developing new drugs for cancer and regenerative diseases. However, currently available probes for selective and highly drug-like inhibition of LATS require further improvement in terms of both activity, selectivity and drug-like properties. Through scaffold hopping aided by docking studies and AI-assisted prediction of metabolic stabilities, we successfully identified an advanced LATS inhibitor demonstrating potent kinase activity, exceptional selectivity against other kinases, and superior oral pharmacokinetic profiles.
View Article and Find Full Text PDFBackground/aim: NUAK family kinase 2 (NUAK2) is a promising target for cancer therapeutics due to its reported role in protein phosphorylation, a critical process in cancer cell survival, proliferation, invasion, and senescence. This study aimed to identify novel inhibitors that disrupt NUAK2 activity. We have already identified two KRICT Hippo kinase inhibitor (KHKI) compounds, such as KHKI-01128 and KHKI-01215.
View Article and Find Full Text PDFA unified diagnostic criterion has yet to be established for sarcopenia. Therefore, we analyzed the reliability and validity of sarcopenia diagnosis using bioelectrical impedance analysis (BIA) compared with the gold standard, dual-energy X-ray absorptiometry (DEXA), and evaluated the predictive accuracy of BIA for diagnosis. The clinical trial, involving a total of 239 participants, was conducted between December 2018 and September 2019 on healthy volunteers without significant medical histories.
View Article and Find Full Text PDFJ Allergy Clin Immunol
June 2024
Hypoxia-inducible factor-1 alpha (HIF-1α) is a transcription factor activated under hypoxic conditions, and it plays a crucial role in cellular stress regulation. While HIF-1α activity is essential in normal tissues, its presence in the tumor microenvironment represents a significant risk factor as it can induce angiogenesis and confer resistance to anti-cancer drugs, thereby contributing to poor prognoses. Typically, HIF-1α undergoes rapid degradation in normoxic conditions oxygen-dependent degradation mechanisms.
View Article and Find Full Text PDFDue to the outbreak of the SARS-CoV-2 virus, drug repurposing and Emergency Use Authorization have been proposed to treat the coronavirus disease 2019 (COVID-19) during the pandemic. While the efficiency of the drugs has been discussed, it was identified that certain compounds, such as chloroquine and hydroxychloroquine, cause QT interval prolongation and potential cardiotoxic effects. Drug-induced cardiotoxicity and QT prolongation may lead to life-threatening arrhythmias such as torsades de pointes (TdP), a potentially fatal arrhythmic symptom.
View Article and Find Full Text PDFMetal-free halogenated anhydrides promote the intramolecular cyclization of -cyano sulfoximines. Trifluoro- or trichloroacetic anhydride (TFAA or TCAA, respectively) activate the -cyano groups of -cyano sulfoximines, leading to the intramolecular cyclization of 2-benzamide--cyano sulfoximines 1. This method results in excellent yields of thiadiazinone 1-oxides 2.
View Article and Find Full Text PDFHighly sensitive rapid testing for COVID-19 is essential for minimizing virus transmission, especially before the onset of symptoms and in asymptomatic cases. Here, we report bioengineered enrichment tools for lateral flow assays (LFAs) with enhanced sensitivity and specificity (BEETLES), achieving enrichment of SARS-CoV-2 viruses, nucleocapsid (N) proteins and immunoglobulin G (IgG) with 3-minute operation. The limit of detection is improved up to 20-fold.
View Article and Find Full Text PDFTo explore the potential of the -cyano sulfilimine group as an amide bond isostere, a derivative of the blockbuster anthranilic diamide, chlorantramiliprole, was synthesized and evaluated with regard to its physicochemical properties, permeability, and biological activity. Given the combination of -cyano sulfilimine chlorantraniliprole 1 and its strong hydrogen bond acceptor character, high permeability, and excellent insecticidal activity, the -cyano sulfilimine functional group could be considered as an amide bond isostere.
View Article and Find Full Text PDFHigh-Mn lightweight steel, Fe-0.9C-29Mn-8Al, was manufactured using steelmaking, ingot-making, forging, and rolling processes. After the final rolling process, a typical austenite single phase was observed on all sides of the thick plate.
View Article and Find Full Text PDFThe single nucleotide polymorphisms (SNPs) of complement factor H (CFH) gene are well-known genetic risk factors for age-related macular degeneration (AMD). To identify whether the measurement of plasma protein concentrations of CFH variants using the multiple reaction monitoring (MRM) assay can determine the genotypes of CFH SNP rs1061170 and rs800292, 120 patients with AMD and 26 controls were included in this study. The number of cases were TT:TC:CC = 121:24:1 in CFH SNP Y402H and GG:AG:AA = 72:57:17 in CFH SNP I62V.
View Article and Find Full Text PDFSoft exosuits used for supporting human muscle strength must be lightweight and wearable. Shape memory alloy (SMA) spring-based fabric muscles (SFM) are light and flexible, making them suitable for soft and shape-conformable exosuits. However, SFMs have a slow actuation speed owing to the slow cooling rate of the SMA spring.
View Article and Find Full Text PDFBiosens Bioelectron
September 2022
A lateral flow assay (LFA) platform is a powerful tool for point-of-care testing (POCT), especially for self-testing. Although the LFA platform provides a simple and disposable tool for Coronavirus disease of 2019 (COVID-19) antigen (Ag) and antibody (Ab) screening tests, the lower sensitivity for low virus titers has been a bottleneck for practical applications. Herein, we report the combination of a microfluidic paper-based nanoelectrokinetic (NEK) preconcentrator and an LFA platform for enhancing the sensitivity and limit of detection (LOD).
View Article and Find Full Text PDFHerein, we describe a novel approach for the practical synthesis of thiadiazine 1-oxides . The first example of an intramolecular cyclization with 2--cyano-sulfonimidoyl amides to form the desired thiadiazine 1-oxides was developed. One-pot acid-induced hydrolysis of the cyano group and the intramolecular cyclocondensation protocol readily provided various heterocyclic frameworks in good to moderate yields.
View Article and Find Full Text PDFThe exosome is considered a useful biomarker for the early diagnosis of cancer. However, pretreatment of samples used in diagnosis is time-consuming. Herein, we fabricated a capacitance-based electrical biosensor that requires no pretreatment of the sample; it is composed of a DNA aptamer/molybdenum disulfide (MoS) heterolayer on an interdigitated micro-gap electrode (IDMGE)/printed circuit board (PCB) system for detecting exosomes in an undiluted serum sample.
View Article and Find Full Text PDFHistone deacetylase 6 (HDAC6) is a promising target for cancer treatment because it regulates cell mobility, protein trafficking, cell growth, apoptosis, and metastasis. However, the mechanism of HDAC6-induced anticancer drug resistance is unclear. In this study, we evaluated the anticancer effect of ACY-241, an HDAC6-selective inhibitor, on erlotinib-resistant pancreatic cancer cells that overexpress HDAC6.
View Article and Find Full Text PDFThe aim of the present study was to report two cases of refractory dry eye syndrome (DES) after transconjunctival excision of the palpebral lobe of the lacrimal gland. A 25-year-old female patient with a chief complaint of a palpable mass in both upper eyelids visited our medical center. Preoperative orbital computer tomography showed high-attenuation lesions in both lacrimal glands.
View Article and Find Full Text PDFIn the field of robotics, sensors are crucial in enabling the interaction between robots and their users. To ensure this interaction, sensors mainly measure the user's strength, and based on this, wearable robots are controlled. In this paper, we propose a novel three-axis force/torque sensor for wearable robots that is compact and has a high load capacity.
View Article and Find Full Text PDFCatalytic reaction events occurring on the surface of a nanoparticle constitute a complex stochastic process. Although advances in modern single-molecule experiments enable direct measurements of individual catalytic turnover events occurring on a segment of a single nanoparticle, we do not yet know how to measure the number of catalytic sites in each segment or how the catalytic turnover counting statistics and the catalytic turnover time distribution are related to the microscopic dynamics of catalytic reactions. Here, we address these issues by presenting a stochastic kinetics for nanoparticle catalytic systems.
View Article and Find Full Text PDFThis study proposes a soft inductive coil spring (SICS) strain sensor that can measure the strain of soft actuators. The SICS sensor, produced by transforming a shape memory alloy (SMA) wire with the same materials as that of an SMA spring bundle actuator (SSBA) into a coil spring shape, measures inductance changes according to length changes. This study also proposes a manufacturing method, output characteristics of the SICS sensor applicable to the SSBA among soft actuators, and the structure of the SICS sensor-integrated SSBA (SI-SSBA).
View Article and Find Full Text PDFField-effect transistor (FET)-based biosensors have garnered significant attention for their label-free electrical detection of charged biomolecules. Whereas conventional output parameters such as threshold voltage and channel current have been widely used for the detection and quantitation of analytes of interest, they require bulky instruments and specialized readout circuits, which often limit point-of-care testing applications. In this study, we demonstrate a simple conversion method that transforms the surface potential into an oscillating signal as an output of the FET-based biosensor.
View Article and Find Full Text PDF