The impact of telecom industry employees' stress perception on job burnout: moderated mediation model.

BACKGROUND: The rapid development of the telecommunications industry in the post-COVID-19 era has brought tremendous pressure to employees making them a high-risk group for job burnout. However, prior research paid less attention to the burnout of employees. Furthermore, social support and gender have separate effects on job burnout. This study explores the mechanism of stress perception on job burnout and examines the roles of social support and gender amid it. METHOD: This cross-sectional study was conducted from June 2023 to August 2023 in mainland China. A total of 39,507 were recruited by random sampling and online questionnaires, and 28,204 valid questionnaires were retained. SPSS (version 26.0) and PROCESS (Model 4 & 7) were used for correlation analysis, mediation analysis, and mediated moderation analysis. RESULT: Stress perception can positively predict the level of job burnout of employees in the telecommunications industry, and social support plays a partial mediating role, accounts for 8.01% of the total effect, gender moderates the first half of the path in this mediation model. At the same pressure level, female can perceive more social support than male. CONCLUSIONS: Under high pressure background, employees' job burnout varies depending on gender and the perception of social support. Therefore, telecommunications industry managers should adopt decompression measures and targeted social support resources for different groups.

Remote Interference Discrimination Testbed Employing AI Ensemble Algorithms for 6G TDD Networks.

The Internet-of-Things (IoT) massive access is a significant scenario for sixth-generation (6G) communications. However, low-power IoT devices easily suffer from remote interference caused by the atmospheric duct under the 6G time-division duplex (TDD) mode. It causes distant downlink wireless signals to propagate beyond the designed protection distance and interfere with local uplink signals, leading to a large outage probability. In this paper, a remote interference discrimination testbed is originally proposed to detect interference, which supports the comparison of different types of algorithms on the testbed. Specifically, 5,520,000 TDD network-side data collected by real sensors are used to validate the interference discrimination capabilities of nine promising AI algorithms. Moreover, a consistent comparison of the testbed shows that the ensemble algorithm achieves an average accuracy of 12% higher than the single model algorithm.

A Needs Learning Algorithm Applied to Stable Gait Generation of Quadruped Robot.

Based on Maslow's hierarchy of needs theory, we have proposed a novel machine learning algorithm that combines factors of the environment and its own needs to make decisions for different states of an agent. This means it can be applied to the gait generation of a quadruped robot, which needs to make demand decisions. To evaluate the design, we created an experimental task in order to compare the needs learning algorithm with a reinforcement learning algorithm, which was also derived from psychological motivation theory. It was found that the needs learning algorithm outperformed the reinforcement learning in tasks that involved making decisions between different levels of needs. Finally, we applied the needs learning algorithm to the problem of stable gait generation of quadruped robot, and it had achieved good results in simulation and real robot.

Comprehensive definition of genome features in Spirodela polyrhiza by high-depth physical mapping and short-read DNA sequencing strategies.

Spirodela polyrhiza is a fast-growing aquatic monocot with highly reduced morphology, genome size and number of protein-coding genes. Considering these biological features of Spirodela and its basal position in the monocot lineage, understanding its genome architecture could shed light on plant adaptation and genome evolution. Like many draft genomes, however, the 158-Mb Spirodela genome sequence has not been resolved to chromosomes, and important genome characteristics have not been defined. Here we deployed rapid genome-wide physical maps combined with high-coverage short-read sequencing to resolve the 20 chromosomes of Spirodela and to empirically delineate its genome features. Our data revealed a dramatic reduction in the number of the rDNA repeat units in Spirodela to fewer than 100, which is even fewer than that reported for yeast. Consistent with its unique phylogenetic position, small RNA sequencing revealed 29 Spirodela-specific microRNA, with only two being shared with Elaeis guineensis (oil palm) and Musa balbisiana (banana). Combining DNA methylation data and small RNA sequencing enabled the accurate prediction of 20.5% long terminal repeats (LTRs) that doubled the previous estimate, and revealed a high Solo:Intact LTR ratio of 8.2. Interestingly, we found that Spirodela has the lowest global DNA methylation levels (9%) of any plant species tested. Taken together our results reveal a genome that has undergone reduction, likely through eliminating non-essential protein coding genes, rDNA and LTRs. In addition to delineating the genome features of this unique plant, the methodologies described and large-scale genome resources from this work will enable future evolutionary and functional studies of this basal monocot family.

Blue light-mediated transcriptional activation and repression of gene expression in bacteria.

Light-regulated modules offer unprecedented new ways to control cellular behavior in precise spatial and temporal resolution. The availability of such tools may dramatically accelerate the progression of synthetic biology applications. Nonetheless, current optogenetic toolbox of prokaryotes has potential issues such as lack of rapid and switchable control, less portable, low dynamic expression and limited parts. To address these shortcomings, we have engineered a novel bidirectional promoter system for Escherichia coli that can be induced or repressed rapidly and reversibly using the blue light dependent DNA-binding protein EL222. We demonstrated that by modulating the dosage of light pulses or intensity we could control the level of gene expression precisely. We show that both light-inducible and repressible system can function in parallel with high spatial precision in a single cell and can be switched stably between ON- and OFF-states by repetitive pulses of blue light. In addition, the light-inducible and repressible expression kinetics were quantitatively analysed using a mathematical model. We further apply the system, for the first time, to optogenetically synchronize two receiver cells performing different logic behaviors over time using blue light as a molecular clock signal. Overall, our modular approach layers a transformative platform for next-generation light-controllable synthetic biology systems in prokaryotes.

Correlation of deregulated like-acetylglucosaminyl transferase and aberrant α-dystroglycan expression with human tongue cancer metastasis.

PURPOSE: The present study examined the correlation of α-dystroglycan (α-DG) expression and like-acetylglucosaminyl transferase (LARGE) with metastasis of human tongue cancer. MATERIALS AND METHODS: Fifty human tongue cancer tissues and 2 tongue squamous cell carcinoma cell lines (CAL27 and SCC4) were involved. Immunohistochemistry was used to detect the expression of α-DG and LARGE. Methylation-specific polymerase chain reaction was performed to assess the methylation status of the LARGE gene promoter. CAL27 and SCC4 cells were transfected with exogenous LARGE and treated with 5-aza-2'-deoxycytidine (Aza-dC), respectively. Glycol sites of α-DG were detected by western blotting. In addition, the laminin overlay assay, cell adhesion assay, and invasion assay were performed. RESULTS: Immunohistochemical results showed that decreased expression of VIA4-1 and IIH6 (antibodies that recognize the glycol sites of α-DG) were correlated with the lymph node metastasis of tongue cancer (n = 50; P = .016 and .025, respectively). Decreased LARGE expression and hypermethylation of the LARGE gene promoter were correlated with lymph node metastasis and α-DG glycosylation in human tongue cancer (n = 50; P = .043 and .015 respectively). In addition, LARGE overexpression and Aza-dC treatment actively led to restoration of functional α-DG expression, elevation of laminin binding, and decrease of migratory ability in cancer cells. CONCLUSION: The results suggested that absent α-DG expression and LARGE deregulation were closely associated with nodal metastasis of tongue cancer. Aberrant α-DG expression and glycosylation were attributed at least in part to the abnormal epigenetic modification of LARGE, especially the hypermethylation of its promoter.

Evolutionary Ensemble Learning for EEG-Based Cross-Subject Emotion Recognition.

Electroencephalogram (EEG) has been widely utilized in emotion recognition due to its high temporal resolution and reliability. However, the individual differences and non-stationary characteristics of EEG, along with the complexity and variability of emotions, pose challenges in generalizing emotion recognition models across subjects. In this paper, an end-to-end framework is proposed to improve the performance of cross-subject emotion recognition. A novel evolutionary programming (EP)-based optimization strategy with neural network (NN) as the base classifier termed NN ensemble with EP (EPNNE) is designed for cross-subject emotion recognition. The effectiveness of the proposed method is evaluated on the publicly available DEAP, FACED, SEED, and SEED-IV datasets. Numerical results demonstrate that the proposed method is superior to state-of-the-art cross-subject emotion recognition methods. The proposed end-to-end framework for cross-subject emotion recognition aids biomedical researchers in effectively assessing individual emotional states, thereby enabling efficient treatment and interventions.

Impact of Mindfulness on sleep quality in innovative corporate employees: A chain mediation of Social Interaction Anxiety and bedtime procrastination.

In the context of innovative enterprises in China, the significance of sleep quality for employees' physical and mental well-being cannot be understated. This study explores the complex relationship between Mindfulness and sleep quality and examines the potential interaction between Social Interaction Anxiety and prolonged sleep behavior. To this end, a thorough evaluation involving the administration of the Mindfulness scale, Social Interaction Anxiety scale, sleep delay scale, and the Pittsburgh Sleep Quality Index (PSQI) was conducted among a significant sample of innovative enterprise employees (N = 1648). The findings reveal that a notable proportion of these employees, 31.1% to be precise (as per PSQI 8), grapple with compromised sleep quality. Subsequent analyses shed light on compelling patterns, underscoring a robust negative correlation between Mindfulness and factors like Social Interaction Anxiety, sleep delay, and sleep quality (ß = -0.71, -0.37, -0.35; P < 0.01). Conversely, a significant positive correlation emerges connecting Social Interaction Anxiety, sleep delay, and sleep quality (ß = 0.23, 0.37, 0.32; P < 0.01). Interestingly, mediation analysis demonstrates that Mindfulness significantly negatively influences sleep quality, independent of demographic factors such as sex and age. This impact is mediated by sleep delay, which also interacts with Social Interaction Anxiety. In summary, the research emphasizes the predictive function of Mindfulness in improving sleep quality among employees in innovative enterprises, achieved through its reduction of Social Interaction Anxiety and bedtime procrastination tendencies.

Oral immunotherapy with enteric-coated capsules for allergic rhinitis caused by house dust mites.

Background: Oral immunotherapy (OIT) is a promising allergen-specific approach in the management of food allergy; however, studies on OIT for allergic rhinitis (AR) have rarely been reported. The purpose of this study is to evaluate the efficacy and safety of OIT using enteric-coated capsules for AR induced by house dust mites. Methods: A total of 49 patients with AR were enrolled, including 25 who received subcutaneous immunotherapy (SCIT) and 24 who received OIT. The clinical efficacy and safety in both groups were evaluated. Results: After 1 year of treatment, both SCIT and OIT demonstrated significant therapeutic effects. OIT was found to be more effective than SCIT in reducing the total AR symptom score and improving the results of nasal provocation tests. Local and systemic adverse reactions were observed in the SCIT group, while none were reported in the OIT group. Conclusion: OIT is an effective and safe treatment for mite-induced AR.

Tumor necrosis factor-α enhanced fusions between oral squamous cell carcinoma cells and endothelial cells via VCAM-1/VLA-4 pathway.

Fusion between cancer cells and host cells, including endothelial cells, may strongly modulate the biological behavior of tumors. However, no one is sure about the driving factors and underlying mechanism involved in such fusion. We hypothesized in this study that inflammation, one of the main characteristics in tumor microenvironment, serves as a prominent catalyst for fusion events. Our results showed that oral cancer cells can fuse spontaneously with endothelial cells in co-culture and inflammatory cytokine tumor necrosis factor-α (TNF-α) increased fusion of human umbilical vein endothelium cells and oral cancer cells by up to 3-fold in vitro. Additionally, human oral squamous cell carcinoma cell lines and 35 out of 50 (70%) oral squamous carcinoma specimens express VLA-4, an integrin, previously implicated in fusions between human peripheral blood CD34-positive cells and murine cardiomyocytes. Expression of VCAM-1, a ligand for VLA-4, was evident on vascular endothelium of oral squamous cell carcinoma. Moreover, immunocytochemistry and flow cytometry analysis revealed that expression of VCAM-1 increased obviously in TNF-α-stimulated endothelial cells. Anti-VLA-4 or anti-VCAM-1 treatment can decrease significantly cancer-endothelial adhesion and block such fusion. Collectively, our results suggested that TNF-α could enhance cancer-endothelial cell adhesion and fusion through VCAM-1/VLA-4 pathway. This study provides insights into regulatory mechanism of cancer-endothelial cell fusion, and has important implications for the development of novel therapeutic strategies for prevention of metastasis.

EphA2/ephrinA1 mRNA expression and protein production in adenoid cystic carcinoma of salivary gland.

PURPOSE: EphA2/ephrinA1 is believed to play a role in tumor growth and metastasis. The purpose of the present study was to determine the presence of EphA2/ephrinA1 in mRNA and protein adenoid cystic carcinoma. MATERIALS AND METHODS: mRNA and protein expression and protein product of EphA2 and ephrinA1 in adenoid cystic carcinoma was investigated using real-time reverse transcriptase polymerase chain reaction, Western blot, and immunohistochemistry. The tyrosine-phosphorylated state of EphA2 in adenoid cystic carcinoma cells was also investigated. RESULTS: Greater expression of EphA2 and ephrinA1 proteins and mRNA was detected in adenoid cystic carcinoma tissues. EphA2/ephrinA1 staining activities in adenoid cystic carcinoma were more significant than those in normal gland tissue (P < .01). EphA2/ephrinA1 expression correlated significantly to the microvessel density (P < .01). EphA2/ephrinA1 expression and microvessel density correlated with the clinical TNM stage, perineural invasion, and vascular invasion (P < .05). In 3 histologic types of adenoid cystic carcinoma, the expression of EphA2/ephrinA1 and microvessel density was significantly greater in the solid type than in the cribriform and tubular types (P < .01). We also noted that EphA2 was present in a nontyrosine-phosphorylated state. CONCLUSIONS: The present study showed a high expression of EphA2/ephrinA1 in adenoid cystic carcinoma. EphA2/ephrinA1 can serve as a novel therapy target for adenoid cystic carcinoma.

[Evaluation of safety of meningococcal group AC bivalent polysaccharide conjugate vaccine in children aged 5-24 months old].

OBJECTIVE: To evaluate the safety of meningococcal group AC bivalent polysaccharide conjugate vaccine among children aged 5-24 months old. METHODS: From July 2011 to June 2012, a total of 34 411 children aged 5-24 month-old who voluntarily vaccinated meningococcal group AC bivalent polysaccharide conjugate vaccine in Zhongshan city were included. The adverse effects within 72 hours were recorded and analyzed. RESULTS: 34 411 children were recruited, including 18 708 boys (54.36%), whose mean age were ( 11.4 ± 3.9 ) months old.Within 72 hours, the incidence rates of local adverse effects were 0.76% (261/34 411) for erythema,0.57% (197/34 411) for sclerosis,0.56% (191/34 411) for swelling,0.42% (143/34 411) for pain,0.15% (53/34 411) for pruritus, and 0.15% (50/34 411) for rash on the injection site. The overall incidence rate of local adverse effects was 1.61% (554/34 411; 95%CI:1.48%-1.74%). The incidence rates of systemic adverse effects were 0.98% (312/34 411) for fever,0.48% (164/34 411) for anorexia,0.31% (108/34 411) for diarrhea,0.29% (100/34 411) for malaise,0.20% (70/34 411) for nausea and vomiting, and 0.08% (26/34 411) for headache. The overall incidence rate of systemic adverse effects was 1.64% (565/34 411; 95%CI:1.51%-1.78%).25 children (0.07%) had hyperpyrexia ( > 39°C), and the time of duration lasted less than 48 hours.16 children (0.05%) had symptoms of cold, such as cough and catarrh.No accident and other serious events were reported. The incidence rate of systemic adverse effects among boys was 1.79% (334/18 708), which was higher than that of girls (1.47%, 231/15 703), the difference showed statistical significance (χ(2) = 5.22, P < 0.01). The incidence rate of systemic adverse effects among children aged 5-12 month-old was 1.78% (411/23 113), which was higher than that among children aged 13-24 month-old (1.36%, 154/11 298), the difference showed statistical significance (χ(2) = 8.10, P < 0.01). The incidence rate of local adverse effects in children vaccinated the first dose was 1.72% (536/31 129), which was higher than that in children vaccinated the second or third dose (0.55%, 18/3282), the difference showed statistical significance (χ(2) = 25.81, P < 0.01). The incidence rate of systemic adverse effects in children vaccinated the first dose was 1.73% (539/31 129), which was higher than that in children vaccinated the second or third dose (0.79%, 26/5282), whose difference also showed statistical significance (χ(2) = 16.22, P < 0.01). CONCLUSION: The safety of meningococcal group AC bivalent polysaccharide conjugate vaccine among children aged 5-24 months old is relative good.

Sports resources utilization efficiency, productivity change, and regional production technology heterogeneity in Chinese Provinces: DEA-SBM and Malmquist Index Approaches.

The efficient allocation of sports resources for optimal outcomes remains a pressing national endeavour in China. Over the past two decades, substantial investments by provincial and national governments have been directed toward sports infrastructure development. This initiative aims to foster sports talent, facilitate excellence, host major sporting events, and enhance national pride and soft power. This study employs a comprehensive methodology encompassing Data Envelopment Analysis-Slack Based Measure (DEA-SBM), Meta Frontier Analysis, and Malmquist Productivity Index to assess Sports Resource Utilization Efficiency (SRUE), Technological Gap Ratio (TGR), and Productivity Growth (MI) across China's 31 provinces and 3 distinct regions for the period 2010-2021. The findings indicate that China's average SRUE stands at 0.6307, revealing an inefficiency of 36.93% in sports resource utilization. Noteworthy efficiency was observed in Beijing, Chongqing, Henan, Shaanxi, Shanghai, and Tianjin during the study duration. Furthermore, a consistent upward trajectory in SRUE from 2010 to 2021 highlights gradual and sustained progress. Comparatively, the eastern region showcases higher technological advancement (average TGR of 0.7598) than the central and western regions. The Malmquist Productivity Index (MI), with an average value of 1.05391, highlights a substantial 5.39% productivity growth. Notably, technological advancement emerges as the primary driver of this productivity increase, evident through the higher Total Factor Productivity Change (TC) of 1.0312 compared to the Efficiency Change (EC) of 1.0209. The Central region's outperforming productivity growth is noteworthy relative to the Eastern and Western regions. Conclusively, the Kruskal-Wallis test confirms significant disparities in the average MI, EC, TC, and TGR among all three regions of China.

A Real-Time Defect Detection Strategy for Additive Manufacturing Processes Based on Deep Learning and Machine Vision Technologies.

Nowadays, additive manufacturing (AM) is advanced to deliver high-value end-use products rather than individual components. This evolution necessitates integrating multiple manufacturing processes to implement multi-material processing, much more complex structures, and the realization of end-user functionality. One significant product category that benefits from such advanced AM technologies is 3D microelectronics. However, the complexity of the entire manufacturing procedure and the various microstructures of 3D microelectronic products significantly intensified the risk of product failure due to fabrication defects. To respond to this challenge, this work presents a defect detection technology based on deep learning and machine vision for real-time monitoring of the AM fabrication process. We have proposed an enhanced YOLOv8 algorithm to train a defect detection model capable of identifying and evaluating defect images. To assess the feasibility of our approach, we took the extrusion 3D printing process as an application object and tailored a dataset comprising a total of 3550 images across four typical defect categories. Test results demonstrated that the improved YOLOv8 model achieved an impressive mean average precision (mAP50) of 91.7% at a frame rate of 71.9 frames per second.

Ceramides and metabolic profiles of patients with acute coronary disease: a cross-sectional study.

Metabolic Syndrome (MS) is a rapidly growing medical problem worldwide and is characterized by a cluster of age-related metabolic risk factors. The presence of MS increases the likelihood of developing atherosclerosis and significantly raises the morbidity/mortality rate of acute coronary syndrome (ACS) patients. Early detection of MS is crucial, and biomarkers, particularly blood-based, play a vital role in this process. This cross-sectional study focused on the investigation of certain plasma ceramides (Cer14:0, Cer16:0, Cer18:0, Cer20:0, Cer22:0, and Cer24:1) as potential blood biomarkers for MS due to their previously documented dysregulated function in MS patients. A total of 695 ACS patients were enrolled, with 286 diagnosed with MS (ACS-MS) and 409 without MS (ACS-nonMS) serving as the control group. Plasma ceramide concentrations were measured by LC-MS/MS assay and analyzed through various statistical methods. The results revealed that Cer18:0, Cer20:0, Cer22:0, and Cer24:1 were significantly correlated with the presence of MS risk factors. Upon further examination, Cer18:0 emerged as a promising biomarker for early MS detection and risk stratification, as its plasma concentration showed a significant sensitivity to minor changes in MS risk status in participants. This cross-sectional observational study was a secondary analysis of a multicenter prospective observational cohort study (Chinese Clinical Trial Registry, https://www.who.int/clinical-trials-registry-platform/network/primary-registries/chinese-clinical-trial-registry-(chictr), ChiCTR-2200056697), conducted from April 2021 to August 2022.

An Image Recognition Framework for Oral Cancer Cells.

Oral squamous cell carcinoma (OSCC) is a common type of cancer of the oral cavity. Despite their great impact on mortality, sufficient screening techniques for early diagnosis of OSCC often lack accuracy and thus OSCCs are mostly diagnosed at a late stage. Early detection and accurate recognition of OSCCs would lead to an improved curative result and a reduction in recurrence rates after surgical treatment. The introduction of image recognition technology into the doctor's diagnosis process can significantly improve cancer diagnosis, reduce individual differences, and effectively assist doctors in making the correct diagnosis of the disease. The objective of this study was to assess the precision and robustness of a deep learning-based method to automatically identify the extent of cancer on digitized oral images. We present a new method that employs different variants of convolutional neural network (CNN) for detecting cancer in oral cells. Our approach involves training the classifier on different images from the imageNet dataset and then independently validating on different cancer cells. The image is segmented using multiscale morphology methods to prepare for cell feature analysis and extraction. The method of morphological edge detection is used to more accurately extract the target, cell area, perimeter, and other multidimensional features followed by classification through CNN. For all five variants of CNN, namely, VGG16, VGG19, InceptionV3, InceptionResNetV2, and Xception, the train and value losses are less than 6%. Experimental results show that the method can be an effective tool for OSCC diagnosis.

Long noncoding RNA SNHG20 regulates cell migration, invasion, and proliferation via the microRNA-19b-3p/RAB14 axis in oral squamous cell carcinoma.

Oral squamous cell carcinoma (OSCC) is one of the most common digestive tumors, which has high mortality rate. Long non-coding RNAs (lncRNA) and MicroRNAs (miRNAs) are associated with the cell cycle and differentiation during the occurrence and development of malignant tumors. This research aimed to investigate the effects of lncRNA SNHG20 on the progress of oral squamous cell carcinoma (OSCC) cells. Ninety pairs of tumor tissues and paracancerous tissues were collected from patients with OSCC and the CAL27 and SCC25 OSCC cells were selected for the following experiments. RT-qPCR was used for detecting the expression of SNHG20, miR-19b-3p, and RAB14. Western blotting was used to detect the protein levels of RAB14. MTT assay was employed to assess cell proliferation. Transwell assay was used to determine the cell migration and invasion abilities. Furthermore, luciferase reporter and RNA pull-down assays were used to verify the binding of SNHG20/RAB14 to miR-19b-3p. Then, the function of the SNHG20/miR-19b-3p/RAB14 axis in OSCC was explored. The results indicated that lncRNA SNHG20 was upregulated in the tissues. Furthermore, bioinformatic analysis showed that both SNHG20 and RAB14 could bind to miR-19b-3p. RAB14 was upregulated, and miR-19b-3p was downregulated in the tissues. The knockdown of SNHG20 inhibited cell proliferation, migration, and invasion. Contrarily, the knockdown of miR-19b-3p reversed the effects of si-SNHG20 on cell proliferation, migration, and invasion, and the overexpression of RAB14 reversed the effects of miR-19b-3p mimic on the cell biological functions. LncRNA SNHG20 affects cell proliferation, migration, and invasion via the miR-19b-3p/RAB14 axis in OSCC.

EPHA2 Promotes the Invasion and Migration of Human Tongue Squamous Cell Carcinoma Cal-27 Cells by Enhancing AKT/mTOR Signaling Pathway.

EPHA2 is a member of the ephrin receptor tyrosine kinase family and is closely related to the malignant tumor progression. The effect of EPHA2 on OSCC is not clear. This study explored the role of EPHA2 and AKT/mTOR signaling pathways in Cal-27 cell invasion and migration. The expression of EPHA2 and EPHA4 in human OSCC and normal oral tissue was detected by immunohistochemistry. EPHA2-overexpressing and EPHA2-knockdown Cal-27 cells were established, and the cells were treated with an AKT inhibitor (MK2206) and mTOR inhibitor (RAD001). The expression of EPHA2 was detected by qRT-PCR, cell proliferation was evaluated by MTT assay, cell migration and invasion were examined by scratch and Transwell assay, and cell morphology and apoptosis were assessed by Hoechst 33258 staining. Western blot was performed to detect the expression of proteins related to AKT/mTOR signaling, cell cycle, and pseudopod invasion. EPHA2 and EPHA4 were highly expressed in clinical human OSCC. Overexpression of EPHA2 promoted the proliferation, migration, and invasion of Cal-27 cells, inhibited cell cycle blockage and apoptosis, and enhanced the activity of the AKT/mTOR signaling pathway. MK2206 (AKT inhibitor) and RAD001 (mTOR inhibitor) reversed the effect of EPHA2 overexpression on the biological behavior of Cal-27 cells. EPHA2 promotes the invasion and migration of Cal-27 human OSCC cells by enhancing the AKT/mTOR signaling pathway.

Discovery of 3-aryl-5-aryl-1,2,4-oxadiazoles as a new series of apoptosis inducers. 2. Identification of more aqueous soluble analogs as potential anticancer agents.

As a continuation of our efforts to discover and develop the 3-aryl-5-aryl-1,2,4-oxadiazole series of apoptosis inducers as potential anticancer agents, we explored substitutions at the 2- and 3-positions of the 3-aryl group to improve the aqueous solubility properties and identify development candidates. A small substitution such as methyl or hydroxymethyl at the 2-position was well tolerated. This modification, in combination with a 3-substituted furan ring as the 5-aryl group, resulted in 4g and 4h, which have improved solubility properties. Compound 4g was found to have good in vivo efficacy in animal studies via intravenous administration.

Discovery and structure-activity relationships of (2-(arylthio)benzylideneamino)guanidines as a novel series of potent apoptosis inducers.

1-(2-(2,5-Dimethoxyphenylthio)benzylidene)semicarbazide (2a) was discovered as a potent apoptosis inducer through our cell based HTS assay. SAR study led to the discovery of a more aqueous soluble analog (2-(2,5-dimethoxyphenylthio)-6-methoxybenzylideneamino)guanidine (5e) with EC(50) value of 60 nM in the caspase activation assay and GI(50) value of 62 nM in the growth inhibition assay in T47D cells. Compound 5e was found to be an inhibitor of tubulin polymerization and efficacious in a MX-1 breast tumor model.