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We also intended to determine the possible mechanism underly
2022-06-02
We also intended to determine the possible mechanism underlying EZH2 upregulation in the PC. Although no recurrent mutations of EZH2 have been described in CLL [27, 28, 29], we aimed to rule out the possibility of activating mutations in the background of EZH2 overexpression. We detected no mutation
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Tyr phosphorylation of AnxA was first
2022-06-02
Tyr23 phosphorylation of AnxA2 was first reported to be involved in endocytosis, particularly in the internalisation of the insulin receptor [20]. Phosphorylated Tyr23 seems to be necessary for the stable association of AnxA2 with endosomes, and for their early-stage transport [14]. The role of AnxA
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The effect of combined A and PD treatment on the
2022-06-02
The effect of combined A-192621 and PD 155080 treatment on the flunixin meglumine during endotoxin infusion is quite different compared to either drug used alone (Wanecek et al., 1999). After administration of both antagonists in combination, cardiac index increased to baseline values within 30 min,
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Acknowledgments The authors would like to thank members of
2022-06-02
Acknowledgments The authors would like to thank members of the Department of Discovery Synthesis (DDS) and Biocon-Bristol Myers Squibb Research Center (BBRC) for scaling up key intermediates, analytical team for analytical experiments, lead profiling group for evaluating compounds in an in vitro AD
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The comparatively low number of H R
2022-06-02
The comparatively low number of H1R agonists is contrasted by the high number of diverse H1R antagonists. Based on pharmacological classification, they are grouped into different generations by considering their target as well as side effects profile. The first generation “antihistamines” consist of
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br Histamine and glycaemia Histamine is involved
2022-06-02
Histamine and glycaemia Histamine is involved in a wide variety of pathophysiological events mostly related to the inflammatory response through four receptors, namely H1-4Rs. The first studies of AVL-292 and diabetes date back to the 1950s. Since that time the involvement of histamine in diabet
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The exact mechanism by which mitochondrial hexokinases such
2022-06-02
The exact mechanism by which mitochondrial hexokinases such as HK1 and HK2 prevent apoptosis is unclear. Mitochondrial hexokinases have been shown to bind with the voltage-dependent anion channel 1 (VDAC1), giving them direct access to ATP for use as an energy source [36]. Akt has been shown to prom
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In the same research group released
2022-06-02
In 2017, the same research group released a free internet accessible database (HemeOxDB, http://www.researchdsf.unict.it/hemeoxdb), to make it easier the analysis of the literature and, consequently, the design of potent and selective HO-1 inhibitors. The database reported the entire set of HO-1 and
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Initial structural and biochemical work showed
2022-06-02
Initial structural and biochemical work showed that Get3 forms an obligate dimer whose conformation is regulated by the bound nucleotide. Analogous to SRP and SR, Get3 contains a P-loop nucleotide hydrolase domain in which the bound ATPs face one another at the dimer interface (Figure 3A, top right
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Here we investigate the structural and
2022-06-02
Here we investigate the structural and biochemical properties of the N-GTPase domain of p190RhoGAP-A. We determine the crystal structure and find that N-GTPase adopts an extended GTPase-like fold with six unique inserts that seem to preclude its ability to bind typical GAP, GEF, or Riociguat molecu
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Two different genes encode GSK
2022-06-02
Two different genes encode GSK-3 isoforms α and β that have very similar catalytic domains but significantly differ in their N- and C-termini. The α and β isoforms split from a common precursor approximately at the emergence of vertebrates, suggesting that at least one of the isoforms took on a new
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GPR co localizes with ghrelin in the duodenum
2022-06-02
GPR120 co-localizes with ghrelin in the duodenum [17], α-gustducin in the small intestine and type II taste bud cells 18, 19, neuropeptide Y centrally in the arcuate nucleus [20] and glucagon-like peptide 1 (GLP-1) in the colon and circumvallate papillae taste bud cells 6, 21, 22. Interestingly GPR1
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Ponceau S Staining Solution br Conclusion In summary a serie
2022-06-01
Conclusion In summary, a series of novel GPR40 agonists bearing phenylpropiolic Ponceau S Staining Solution motif with favorable metabolic stability were prepared and evaluated for their activities as GPR40 agonists. Among them, compound 9 was identified as a structurally distinct GPR40 agonist p
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In vitro studies have shown that some antidepressant
2022-06-01
In vitro studies have shown that some antidepressant drugs bind to NMDA receptors and inhibit the binding of NMDA receptor ligands [18]. Similarly, several research teams have reported that tricyclic antidepressants can modulate the release and/or uptake of glutamate [19]. In this study, we found th
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br Introduction As is now
2022-06-01
Introduction As is now well known, obesity is major risk factor for various diseases such as nonalcoholic fatty liver disease, cardiovascular disease, some cancers (McWilliams and Petersen, 2009), type-2 diabetes mellitus (Jakobsen et al., 2007), and hypertension (Aneja et al., 2004), among other
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