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The development of novel approaches to
2020-03-04
The development of novel approaches to study GPCR-mediated transactivation in live Vacquinol-1 is important, and this study describes a unique BRET-based quantification of Grb2 recruitment to the EGFR as a direct readout of GPCR-mediated transactivation. We have previously used the recruitment of Gr
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Proof of concept studies with disulfiram suggest the
2020-03-04
Proof-of-concept studies with disulfiram suggest the potential utility of DβH inhibitors for treatment of cocaine use disorder. In a study of 74 subjects stabilized on methadone and randomized into disulfiram and placebo groups for 10weeks, disulfiram treatment reduced cocaine-positive urines, and d
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Autoradiography studies have shown cerebellum to be devoid o
2020-03-04
Autoradiography studies have shown CRA-024781 to be devoid of D1-R [40], confirming that this region may serve as reference for estimation of free and non-specifically bound radioligand concentration in tissue (= non-displaceable uptake). In initial human studies using [11C]SCH 23390 and [11C]NNC 1
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Lately using receptor TM peptides BiFC and PLA experiments w
2020-03-04
Lately, using receptor TM peptides, BiFC and PLA experiments, we have also obtained experimental evidence for the tetrameric structure of A1R–D1R, which explains the canonical interaction on Gi and Gs, respectively (Fig. 2). We have demonstrated for the first time the presence of this heterotetramer
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DGK negatively regulated the extension
2020-03-04
DGKδ negatively regulated the extension of long axon/neurite (Fig. 4, Fig. 5, Fig. 6). The results strongly suggest that deficiency of DGKδ induces OCD-like behavior by enhancing axon/neurite outgrowth. DGKδ positively regulates growth factor signaling (Crotty et al., 2006). Therefore, DGKδ deficien
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Predictions of enzyme topology for
2020-03-04
Predictions of enzyme topology for DGAT2 are more difficult since the DGAT2 polypeptide sequences are more diverse across species than those of DGAT1. The length and function of the hydrophilic N-terminus preceding the first hydrophobic segment varies with species – for example, segments in fungi ar
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br Deregulation of CDK Many neurotoxic or stress
2020-03-04
Deregulation of CDK5 Many neurotoxic or stress conditions like ischemic elastase inhibitor damage, oxidative stress, mitochondrial dysfunctions, excitotoxicity, Aβ exposure lead to disruption of the tight regulation of Cdk5 (De Strooper et al., 2010). Calpain-mediated cleavage of p35 to p25 is a
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As demonstrated by Mak and colleagues
2020-03-04
As demonstrated by Mak and colleagues, ERβ is known to be a part of the NFκB-HIF-1α signaling pathway during hypoxia as well as chronic inflammation of prostate (Mak et al., 2015), therefore in the next part of the study, we evaluated whether ZEA-induced ROS production is also associated with NFκB-H
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Epitope analyses of AT AA and ET AA
2020-03-03
Epitope analyses of AT1-AA and ET-AA indicate that the BH3I-1 of both autoantibodies are located at the second extracelluar loop of both receptors. The specific epitopes for both autoantibodies are similar to what was reported previously in a cohort of patients from Brazil [6] and for AT1-AA also fr
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Introduction Rotavirus RV a member of Reoviridae family is a
2020-03-03
Introduction Rotavirus (RV), a member of Reoviridae family, is a non-enveloped virus which has a double-stranded RNA genome of 11 segments surrounded by three concentric protein layers. It has been reported to cause estimated 25% of moderate-to-severe illnesses (Kotloff et al., 2013) and 30% of tot
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Initially studies of GPCRs predominantly assessed
2020-03-03
Initially, studies of GPCRs predominantly assessed the signalling pathways downstream of receptors on the cell surface. There is now an understanding that GPCRs can localize to and signal from various intracellular compartments, such as the nucleus (reviewed in [40]). These intracellular pools of re
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The mechanism by which OC use leads to
2020-03-03
The mechanism by which OC use leads to impaired glucose tolerance is yet to be fully clarified. Decreased insulin sensitivity appears to be mainly accounted for by estrogenic component and this effect may be modified by progestogenic component [14], [15]. Estrogenic effect on glucose tolerance has b
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Collectively the results presented here provide new insights
2020-03-03
Collectively, the results presented here provide new insights into ligand binding, clustering, spatial distribution, and phosphorylation of DDR1b and DDR2 in response to soluble collagen I. As depicted in the cartoon of Scheme 1, we postulate a model in which the spatial distribution and assembly of
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Bufalin The enantiomeric ratio ER of chiral compounds accumu
2020-03-03
The enantiomeric ratio (ER) of chiral compounds accumulated in organisms has been found to be different among species (Borga and Bidleman, 2005, Harner et al., 1999, Warner et al., 2005, Wiberg et al., 2000), indicating enantioselective accumulation of chiral compounds are species-specific. The ER o
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CB-839 synthesis br Conclusion br Acknowledgment The authors
2020-03-03
Conclusion Acknowledgment The authors would like to thank “Science and Engineering Research Board (SERB) of Department of Science and Technology (DST) Govt. of India” (Grant No.YSS/2015/002017) for funding the project. Introduction Mutations occurring within EGFR exons 18 to 21 are present
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