The β-pyridyl amide is a critical scaffold in medical discovery yet lacks efficient synthetic methods. Here, we describe, for the first time, a visible-light-induced, redox-neutral radical cross-coupling reaction involving alkenes, oxamic acids, and cyanopyridines that offers a versatile assembly of β-pyridylamides. This approach features mild reaction conditions, high step efficiency, and substrate breadth, providing a green and efficient strategy for alkene pyridyl-carbamoylation.
View Article and Find Full Text PDFChiral cyclobutanamide is a privileged scaffold in drug discovery. Here, we describe, for the first time, the synthesis of axially chiral cyclobutanamides via phosphoric acid-catalyzed enantioselective condensation between -arylcarbamyl cyclobutanones and hydroxylamines. Rational substrate design, incorporating an amide moiety (CONHR) into the cyclobutanone backbone and the formation of a multi-hydrogen bonding network involving the N-H of this amide portion, is responsible for the excellent enantioselectivity achieved in the stereodetermining dehydration process, which is supported by a detailed mechanistic study.
View Article and Find Full Text PDFPaxillin and kindlin are essential regulatory proteins involved in cell adhesion, migration, and signal transduction. Paxillin influences cytoskeletal dynamics by interacting with multiple signaling proteins, while kindlin regulates integrin activation, affecting adhesion and motility. This review examines the structures and functions of these proteins, focusing on their roles in cancer progression, immune response, and therapeutic potential.
View Article and Find Full Text PDFPhotosensitizers (PSs) featuring type I reactive oxygen species (ROS) generation and aggregation-induced emission (AIE) activity offer a promising solution to achieve non-invasive and precise theranostics. However, the reported AIE luminogens (AIEgens) with both AIE characteristic and strong type-I ROS generation are still scarce and the structure-property relationship is still unclear. Herein, an innovative acceptor elongation boosted intersystem crossing (AEBIC) design strategy has been proposed to endow the AIEgen strong type-I ROS producibility.
View Article and Find Full Text PDFMegalurothrips usitatus (Bagnall) (Thysanoptera: Thripidae) is an important pest of cowpeas, Vigna unguiculata (L.) Walp., and can cause severe damage to the crop.
View Article and Find Full Text PDFDisulfiram (DSF), primarily applied in the therapy for alcohol addiction, has been demonstrated to possess the promising capability of anti-tumor in many human cancers, including esophageal squamous cell carcinoma (ESCC). To date, almost all studies about DSF in ESCC are focusing on investigating either drug combinations or nanoparticle-based delivery systems. However, the exact molecular mechanisms mediating the response to DSF in ESCC are totally unknown.
View Article and Find Full Text PDF: is a rare temperate evergreen shrub with high tolerance to low temperature, and understanding the related gene expression regulatory network can help advance research on the mechanisms of plant tolerance to abiotic stress. Here, time-course transcriptome analysis was applied to investigate the gene expression network in under low temperature stress. : A total of 12,606 differentially expressed genes (DEGs) were identified at four time-points during low temperature stress treatment, and multiple pathways, such as plant hormones, secondary metabolism, and cell membranes, were significantly enriched in the DEGs.
View Article and Find Full Text PDFIntroduction: Although inguinal hernia (IH) is prevalent in elderly males, research on its specific diagnostic biomarkers is limited. Protein -glycosylation is one of the most important and ubiquitous post-translational modifications and often results in a remarkable heterogeneity of protein glycoforms. Protein -glycosylation often changes in a disease and holds great potential for discovering non-invasive biomarkers.
View Article and Find Full Text PDFBackground: The health effects of different weight loss strategies vary greatly, and the relationship between weight loss strategies, especially the combination of multiple strategies, and death is still unclear. We aimed to examine the associations of various numbers and combinations of weight loss strategies with all-cause and specific-cause mortality and to further evaluate the associations of different total weight loss volumes with mortality.
Methods: Using data from NHANES (1999-2018) with 48,430 participants aged 20 and above, we collected fourteen self-reported weight loss strategies and identified five clusters using latent class analysis.
Corona virus disease 2019 (COVID-19) due to severe acute respiratory syndrome coronavirus 2 (SARS-CoV-2) infection has affected the whole world. Acquired thrombotic thrombocytopenic purpura (TTP) has been reported after administration of mRNA- or adenoviral vector-based COVID-19 vaccines, including Ad26.COV2-S, BNT162b2, mRNA-1273, and ChAdOx1 nCov-19.
View Article and Find Full Text PDFBlueberry leaves (BBL) are a natural source with strong antioxidant activity, but bioactive compounds and their seasonal variation remain vague. Here, two major classes of compounds including four caffeoylquinic acids and eight flavonoids were identified in two southern highbush cultivars ("Lanmei" #1 and "Jewel") grown in China. Major bioactive compounds were discovered using an online HPLC post-column derivatization system and determined as neochlorogenic acid (NeoCA), chlorogenic acid (CA), rutin, hyperoside, and isoquercitrin.
View Article and Find Full Text PDFLacking effective therapeutic targets heavily restricts the improvement of clinical prognosis for patients diagnosed with esophageal squamous cell carcinoma (ESCC). Ubiquitin Specific Peptidase 21 (USP21) is dysregulated in plenty of human cancers, however, its potential function and relevant molecular mechanisms in ESCC malignant progression as well as its value in clinical translation remain largely unknown. Here, in vitro and in vivo experiments revealed that aberrant upregulation of USP21 accelerated the proliferation and metastasis of ESCC in a deubiquitinase-dependent manner.
View Article and Find Full Text PDFMegalurothrips usitatus (Bagnall) (Thysanoptera: Thripidae) is an important pest in Vigna unguiculata (L.) Walp. Neoseiulus barkeri (Hughes) (Acari: Phytoseiidae) is widely used for control of pest mites and insects worldwide.
View Article and Find Full Text PDFPaclitaxel resistance is associated with a poor prognosis in non-small cell lung cancer (NSCLC) patients, and currently, there is no promising drug for paclitaxel resistance. In this study, we investigated the molecular mechanisms underlying the chemoresistance in human NSCLC-derived cell lines. We constructed paclitaxel-resistant NSCLC cell lines (A549/PR and H460/PR) by long-term exposure to paclitaxel.
View Article and Find Full Text PDFAn efficient and atom-economical silver-mediated [2 + 2 + 1] cyclization protocol for the selective synthesis of 2,4- or 3,4-dicarbonylselenophenes has been developed. Readily accessible substrates, commercially available elemental selenium, and good functional group tolerance make this procedure attractive for the selective synthesis of dicarbonylselenophenes. Preliminary mechanistic investigations indicated that silver acetylene species are possible intermediates for the formation of 3,4-dicarbonylselenophenes.
View Article and Find Full Text PDFAsia Pac J Public Health
September 2023
This study aimed to explore the associations of screen time (ST) and its' changes with follow-up body mass index (BMI) in preschool children. Parents of 805 preschoolers participated in our study at baseline and were followed up after 1 year in China. Linear regression models were used to analyze the dynamic relationship between ST and BMI in preschool children.
View Article and Find Full Text PDFBackground: Right hemi-hepatectomy plus total caudate lobectomy is the appropriate procedure for type IIIa or partial type II pCCA. However, the laparoscopic implementation of this procedure remains technically challenging, especially hilar vascular dissection and en bloc resection of the total caudate lobe. Augmented reality navigation can provide intraoperative navigation to enhance visualization of invisible hilar blood vessels and guide the parenchymal transection plane.
View Article and Find Full Text PDFAn efficient silver-mediated [2 + 2 + 1] cyclization protocol of -propioloylbenzonitriles with elemental selenium for the synthesis of 4-indeno[1,2-][1,2]selenazol-4-ones has been developed. One C-Se bond, one N-Se bond, and one C-C bond were rapidly constructed in one step. The reaction might proceed via the formation of a highly reactive selenoketene intermediate, followed by intramolecular cyclization.
View Article and Find Full Text PDFImproving hepatic glucose and lipid metabolisms is an important strategy to treat type 2 diabetes mellitus complicated with non-alcoholic fatty liver disease (T2DM-NAFLD). Silybin (SLB) has the potential hepatoprotection, while its oral bioavailability is poor. This study aims to investigate the functional role and mechanism of liposomal SLB in modulating glucose/lipid metabolism in T2DM-NAFLD.
View Article and Find Full Text PDF