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Given the involvement of dysregulated S nitrosylation in mul
2022-06-02
Given the involvement of dysregulated S-nitrosylation in multiple pathological conditions, a number of approaches to regulate S-nitrosylation therapeutically are being tried in multiple indications [18]. In the lung, GSNO releasing compounds and GSNOR inhibitors are being considered as potential the
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To gain insights for further
2022-06-02
To gain insights for further improvement of the agonistic activity, we compared the structural features of the -carbamate piperidine moiety in with that of the spirocyclic moiety in –. Obviously, the substituent corresponding to an isopropyl group on the -carbamate in was lacking in the spirocyclic
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Naringin has been shown to have significant anti inflammatio
2022-06-02
Naringin has been shown to have significant anti-inflammation, anti-oxidative stress, glucolipid metabolic regulation, and myocardial protection effects (Gopinath et al., 2011, Gopinath and Sudhandiran, 2012), suggesting that it may mitigate ADC by inhibiting P2X7 receptors. In the present study, na
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Due to the high structural similarity between GlxI
2022-06-02
Due to the high structural similarity between GlxI and FosA, it is possible that GlxI directed evolution experiments could produce FosA enzymatic activity in a GlxI enzyme. Although the current investigation was unable to detect FosA activity by mutation of a key metal liganding residue in the activ
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br Functional organization of postsynaptic
2022-06-01
Functional organization of postsynaptic glutamate receptors Downstream effects of glutamate receptor positioning Mechanisms underlying the subsynaptic positioning of glutamate receptors Conclusions and future prospects The molecular organization of synapses is undoubtedly a critical dete
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According to the aforementioned preclinical and clinical dat
2022-06-01
According to the aforementioned preclinical and clinical data, GHS-R1a blockade appears to be a potential pharmacological approach to treat AUD. Given that GHS-R1a has high constitutive (ligand-independent) activity, inverse agonism of the receptor may exert more potent and desirable effects than pu
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The effects of galanin on anxiety
2022-06-01
The effects of galanin on anxiety may depend on the site of drug administration, on the galanin receptor subtypes activated and on the animal models of anxiety employed (Barrera et al., 2005, Holmes and Picciotto, 2006, Soares et al., 2016a, Soares et al., 2016b). For instance, administration of gal
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N Alkylated quinolinium dyes are the
2022-06-01
N-Alkylated quinolinium dyes are the common fluorescence molecules used in fluorescence sensing and cell imaging because of their attractive optical properties as well as high DNA binding affinities.13, 14, 15, 16, 17, 18, 19, 20 Moreover, the quinolinium moiety usually plays the role of donor in va
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br Role of FPRs in
2022-06-01
Role of FPRs in regulating the inflammatory response Annexin I is a glucocorticoid-regulated protein possessing both pro- and anti-inflammatory activity that might be mediated, in part, by FPR activation [35]. Expressed in a variety of cell types, annexin I is particularly abundant in neutrophils
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Brain derived neurotrophic factor BDNF is the most
2022-06-01
Brain-derived neurotrophic factor (BDNF) is the most abundant growth factor in the brain and is critical for neuronal development and synaptic plasticity (Bekinschtein et al., 2008; Lu et al., 2014). Besides playing an important role in mood and cognition, BDNF is also involved in the regulation of
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Active compounds and were further tested
2022-06-01
Active compounds , , and were further tested and EC and pEC values were determined as shown in . Compound showed EC of 0.97μM (pEC 6.01) with 84.5% maximal response, which suggests that introduction of alkyl chain on aromatic nucleus of , resulted in improved GPR40 agonistic activity than that of
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About of human primary melanomas and
2022-06-01
About 67% of human primary melanomas and 56% of melanoma metastases display cytoplasmic or nuclear β-catenin accumulation (Xue et al., 2016). Of note, active β-catenin stimulates emergence of metastasizing melanoma in mice harboring BrafV600E or NrasQ61K hyperplasia (Damsky et al., 2011, Delmas et a
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NeuroHIV is initiated by HIV crossing the blood brain
2022-06-01
NeuroHIV is initiated by HIV crossing the blood–brain barrier (BBB) to enter the CNS. This is thought to occur primarily via the transmigration of infected CD14+CD16+ monocytes (Williams, 2014), using the monocytes as “Trojan Horses” (Peluso, 1985), although some studies suggest alternate routes of
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One of pathogenesis of COPD is oxidant
2022-05-31
One of pathogenesis of COPD is oxidant/antioxidant imbalance. Indeed, it is well known that chronic tobacco smoking is a major risk factor for the development of COPD, and a defect in the detoxification of reactive species produced by cigarette smoke may predispose smokers to airflow obstruction and
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Recent work by Que et al with mouse
2022-05-31
Recent work by Que et al with mouse models implicates GSNOR in the cause of asthma. GSNOR is expressed in multiple cell types in the lung, including airway epithelial cells and infiltrating leukocytes. After exposure to ovalbumin, GSNOR activity increased in airway lining fluid, perhaps reflecting i
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