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In conclusion a series of new carboxamido aryl
2022-03-04

In conclusion, a series of new 3-carboxamido-5-aryl-isoxazoles was designed, synthesized and screened for their inhibitory potency against FAAH. Their cytotoxicity was determined and their lipophilicity was calculated. Compounds bearing a 3-substituted biphenyl moiety with high Log values displayed
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Our previous work demonstrated that
2022-03-03

Our previous work demonstrated that KDM5 regulates cellular oxidative stress in Drosophila (Liu et al., 2014, Liu and Secombe, 2015). It is known that gut epithelial Ethacrynic acid - d5 contacted by enteric commensal bacteria generate reactive oxygen species in response to microbial signals (Jones
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Utilization of fascinating properties such as localized surf
2022-03-03

Utilization of fascinating properties, such as localized surface plasmon resonance (LSPR), high fluorescent quantum yield, biocompatible nature, chromogenic and electrocatalytic functionality of several nanomaterials for histamine sensing is also quite evident where the nanomaterials have served as
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Accessibility and physico chemical features
2022-03-03

Accessibility and physico-chemical features of cysteine residues define their redox-reactivity and the 3-dimensional structure of GSNOR allows to identifying such surface-exposed, redox-sensitive cysteine residues. GSNOR crystal structures are available from human (Protein Data Bank code: 1MP0), tom
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The physiological role of lactate
2022-03-03

The physiological role of lactate-induced antilipolytic effects is less clear. It has been speculated that GPR81 mediates the inhibition of lipolysis during intensive exercise, a condition which results in high systemic lactate plasma concentrations 9, 10. Owing to oxygen shortage resulting from int
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cki receptor GW was also the starting point for a
2022-03-03

GW4064 was also the starting point for a study by an independent research group. The co-crystal structure of GW4064 with FXR suggested the potential for favorable hydrogen bond interactions between the isoxazole 3-aryl group and several receptor residues such as Tyr373 and Ser336. Replacing the 2,6-
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br Conflict of interest br CRediT authorship contribution
2022-03-03

Conflict of interest CRediT authorship contribution statement Magdalena Olga Ciechanowska: Conceptualization, Data curation, Investigation, Methodology, Project administration, Writing - original draft. Magdalena Łapot: Formal analysis, Investigation, Methodology. Marek Kowalczyk: Writing - re
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The aim of this study is
2022-03-03

The aim of this study is to explore new Glo-I inhibitors using the structure-based pharmacophore approach. Eighteen Glo-I co-crystallized structures have been explored to investigate their pharmacophoric features. Ninety two pharmacophoric models were generated. QSAR analysis followed by Ligand Prof
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The transporter was successfully expressed in MSCs and
2022-03-03

The transporter was successfully expressed in MSCs and HEK 293 cells. In both cell types, the expression of YFP-EAAT2 was confirmed by immunological staining and flow cytometry. The functionality of the transporter was determined by [3H]glutamate uptake assays, and the blood glutamate-grabbing activ
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Boswellia papyrifera Del Hochst mostly grows in Sudanian and
2022-03-03

Boswellia papyrifera (Del.) Hochst., mostly grows in Sudanian and Sahelian regions and their oleo-gum resin is used medically in treatment of rheumatism, menorrhagia, amenorrhoea, vaginal infections, ulcers, sores, polyuria, syphilis, bronchitis, scrofulous affections, inflammations, asthma, diarrhe
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The rapid actions of glucocorticoids range from the producti
2022-03-02

The rapid actions of glucocorticoids range from the production of endocannabinoid as a retrograde messenger [9], to regulation of ion channels [10], [11], to inhibitory effects on immune TC-E 5003 [12], [13], [14]. Many different kinase signaling pathways have been implicated in the rapid actions o
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br Experimental Procedures Information on the materials
2022-03-02

Experimental Procedures Information on the materials used in this study and the details of how the in vivo and in vitro assays were performed are provided in Supplemental Information. Acknowledgments This research was supported by the National Research Foundation of Korea (NRF) grant funded b
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The Hippo pathway has been well
2022-03-02

The Hippo pathway has been well established as a tumor suppressor pathway and is involved in many diverse biologic processes including cell growth, cell death, and organ size control in organisms, ranging from Drosophila to mammals [4]. Central to this pathway is a kinase cascade in which the Ste20-
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Another important question for future studies
2022-03-02

Another important question for future studies will be whether FAAH inhibitors work to normalize impairments in fear extinction that are known to be produced by environmental insults such as exposure to abused drugs and stress 97, 103. Indeed, several authors have posited utility of FAAH inhibitors f
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The current study aimed to understand the roles and the
2022-03-02

The current study aimed to understand the roles and the underlying mechanisms of XIST in LSCC, by focusing on the regulation by miR-124-3p, which was previously identified as a target of XIST [12]. We found that the XIST expression is positively correlated with the stages of LSCC in patients. Knockd
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