The first copper-catalyzed enantioselective [4 + 1] annulation of yne-allylic esters with 1,3-dicarbonyl compounds was realized through an elegant remote stereocontrol strategy. The very remote ε regioselective nucleophilic substitution was developed by employing a novel chiral copper-vinylvinylidene species from the new C4 synthon yne-allylic esters. Thus, greatly diverse spirocycles were obtained with ample scope and excellent levels of chemo-, regio-, and enantioselectivities. Moreover, detailed mechanistic studies suggest an yne-allylic substitution and Conia-ene cascade pathway on the remote stereochemical induction progress.
The long intergenic non-coding RNA linc01133 is reported to be oncogenic in various malignancies. However, the role and mechanism of linc01133 in regulating gastric cancer growth is still not clear. In the present study, we found that linc01133 was significantly upregulated in gastric cancer tissues compared to non-tumorous gastric tissues. Linc01133 over-expression significantly correlated with tumor size and tumor differentiation in gastric cancer patients. The expression of linc01133 was regulated by c-Jun and c-Fos collaboratively. In both in vitro and in vivo studies, linc01133 was shown to promote gastric cancer cell growth. Linc01133 localized in the cytoplasm and functioned as an endogenous competing RNA of miR-145-5p to upregulate the expression of YES1, which was proved to be the target gene of miR-145-5p. By promoting YES1-dependent YAP1 nuclear translocation, linc01133 upregulated the expression of the key cell cycle regulators CDK4, CDK6 and cyclin D1 to promote G1-S phase transition. Thus, our study unveiled the function and mechanism of linc01133 regulating cell cycle progression in gastric cancer.
Norfloxacin is often found in wastewater treatment plants, groundwater, and even drinking water causing environmental concerns because of its potential undesirable effects on human health or aquatic ecosystems. However, conventional treatments cannot deal with norfloxacin efficiently. This work proposes an efficiently enzymatic degradation of norfloxacin by chloroperoxidase (CPO). 82.18% degradation efficiency of norfloxacin was achieved after 25 min reaction time at pH 5.0 with an enzyme concentration of 1.5 × 10 mol L. HPLC-MS was used to determine the intermediates or final products. The product analysis and determination of the chemical oxygen demand indicated if the enzymatic degradation by CPO was carried out before the usually existing bioremediation techniques (usually activated sludge) in sewage treatment plant, the effluent containing norfloxacin can be decontaminated more efficiently and thoroughly than that only by activated sludge treatment. The eco-toxicity tests using a green algae, Chlorella pyrenoidosa, indicated that the toxicity of degraded products of norfloxacin was lower than the parent norfloxacin molecule. CPO-catalyzed degradation of norfloxacin is a promising alternative for treating effluent containing norfloxacin.
C–H amination at the C5 position of 8-aminoquinolines with azodicarboxylates proceeded efficiently using a nickel/silver co-catalyst at room temperature without any additional ligand, base or oxidant.
An
efficient silver-catalyzed para-selective amination
and aminative dearomatization of phenols with azodicarboxylates was
developed. It afforded the para-aminophenols or amino
cyclohexadieneones from free phenols depending on whether it has a para-substituent. The reaction proceeded smoothly in water
under simple and mild conditions, giving the highly selective products
in good yields within a short reaction time. It also showed broad
substrate scope and good functional group compatibility.
This study gives a critical examination of the performances of three top key opinion leaders (KOLs) on social media in China to explore whether gender serves as an important social factor in their interaction with their followers. A critical analysis of their Weibo posts has revealed that they construct different gender identities through their preferential choices of personality traits, speech acts, and addressing terms. This can be explained in terms of their target consumers and the products they promote. It concludes that although gender can serve as an important factor in top KOLs’ performances on social media, it can be appropriated and exploited in varied ways to serve different communicative purposes.
Gastric cancer is a high molecular heterogeneous disease with a poor prognosis. Although gastric cancer is a hot area of medical research, the mechanism of gastric cancer occurrence and development is still unclear. New strategies for treating gastric cancer need to be further explored. Protein tyrosine phosphatases play vital roles in cancer. A growing stream of studies shows that strategies or inhibitors targeting protein tyrosine phosphatases have been developed. PTPN14 belongs to the protein tyrosine phosphatase subfamily. As an inert phosphatase, PTPN14 has very poor activity and mainly functions as a binding protein through its FERM (four-point-one, ezrin, radixin, and moesin) domain or PPxY motif. The online database indicated that PTPN14 may be a poor prognostic factor for gastric cancer. However, the function and underlying mechanism of PTPN14 in gastric cancer remain unclear. We collected gastric cancer tissues and detected the expression of PTPN14. We found that PTPN14 was elevated in gastric cancer. Further correlation analysis indicated that PTPN14 was relevant with the T stage and cTNM (clinical tumor node metastasis classification) stage. The survival curve analysis showed that gastric cancer patients with higher PTPN14 expression had a shorter survival time. In addition, we illustrated that CEBP/β (CCAAT enhanced binding protein beta) could transcriptionally activate PTPN14 expression in gastric cancer. The highly expressed PTPN14 combined with NFkB (nuclear factor Kappa B) through its FERM domain and accelerated NFkB nucleus translocation. Then, NFkB promoted the transcription of PI3KA and initiated the PI3KA/AKT/mTOR pathway to promote gastric cancer cell proliferation, migration, and invasion. Finally, we established mice models to validate the function and the molecular mechanism of PTPN14 in gastric cancer. In summary, our results illustrated the function of PTPN14 in gastric cancer and demonstrated the potential mechanisms. Our findings provide a theoretical basis to better understand the occurrence and development of gastric cancer.
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