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Preliminary studies suggest that dimerization
2021-02-04

Preliminary studies suggest that dimerization of the AT1 receptor occurred during the biosynthesis in the endoplasmic reticulum before surface expression [27,40], which may explain the presenece of these Necrostatin 1 before the addition of any ligand. Our results showed that the presence of Ang I
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To further confirm the roles of the
2021-02-04

To further confirm the roles of the CYP450 enzymes involved in the metabolism of Dip in rat liver microsomes, we utilized not only chemical inhibitors but also a correlation analysis and a panel of recombinant rat CYP450 enzymes to evaluate the contribution of CYP450 enzymes. The results of the corr
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Argatroban In vitro studies in NSCLC cell lines
2021-02-04

In vitro studies in NSCLC cell lines expressing EGFR mutants (T790M mutation, exon 19 deletion E746-A750, L858R/T790M double mutation), demonstrated that Rociletinib potently inhibits proliferation in the mutant EGFR NSCLC Argatroban with Growth inhibition (GI50) values ranging from 7 to 32 nmol/L.
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DMXAA Mammalian cells have two distinct DNA
2021-02-04

Mammalian DMXAA have two distinct DNA repair pathways for DSBs, NHEJ and HR. Our data are consistent with the suggestion that the DNA–PK-mediated NHEJ pathway recognizes DSBs faster than the HR pathway and acts before the activation of the DNA damage S-phase checkpoint. The activation of NHEJ by DN
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The most significant source of DAG originates
2021-02-03

The most significant source of DAG originates from the PLC family of enzymes, which produces DAG in an agonist-regulated reaction. PLCs constitute a wide family of enzymes acting on both phosphatidilinositols (PI) and phosphatidilcoline (PC) (Li et al., 2010) in the plasma membrane and other intrace
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In vitro study indicated the
2021-02-03

In vitro study indicated the cell death of hippocampal neurons was mediated by DAPK1 following ceramide-3 treatment (Pelled et al., 2002). the same study showed that DAPK1-deficient mice treated by acyl ceramide exhibit a less sensitivity to apoptosis, this proposed that DAPK1 plays a central role i
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br Disclosure and conflicts of interest br Acknowledgements
2021-02-03

Disclosure and conflicts of interest Acknowledgements This research was supported by grant (BT/PR/11293/BRB/10/849/2008) from Department of Biotechnology (DBT), Government of India and a DST YOS Chair Professorship to PB. The mass spectrometry facility is supported by an institutional program
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Introduction Prolyl hydroxylation is a widely observed post
2021-02-03

Introduction Prolyl hydroxylation is a widely observed post translational modification in collagen, an abundant animal protein. The high content (~13% per chain of the triple helical structure) of 4-hydroxyproline (Hyp,O) in collagen, togather with the natural abundance of collagen has led to the e
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Our published results also show that the Y and
2021-02-03

Our published results also show that the Y2 and the Y5, but not the Y1, receptors mediate NPY-induced excitation-secretion coupling in EECs (Abdel-Samad et al., 2012). Thus, it is highly important to consider controlling ET-1 circulating level via blockade of Y2 and/or Y5 receptor activation (Abdel-
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Replacement of the saturated propoxy group in compound with
2021-02-03

Replacement of the saturated -propoxy group in compound with the unsaturated allyloxy group to obtain compound resulted in 10-fold decrease in ET receptor antagonism and more than 20-fold decrease in ET-selectivity. Analogous unsaturated allyloxy compound in the tetrazole series was found to have
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The H E staining and Nissl staining results showed that
2021-02-03

The H&E staining and Nissl staining results showed that damage to the pyramidal neurons in the CA1 and CA3 regions of the hippocampus were observed in the 50 mg/kg/day DBP group, accompanied by an absence of Nissl bodies, suggesting that DBP exposure can lead to pathological changes in the neurons o
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The role of Epac in
2021-02-03

The role of Epac in the regulation of intracellular Ca homeostasis and contractility is still matter of debate. In rat adult cardiomyocytes, acute Epac stimulation decreased the amplitude of Ca transients [6], [9], [10] with either no changes [6] or increments [9] in cell shortening, suggesting an e
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To develop antagonists selective for the mouse EP receptor
2021-02-03

To develop antagonists selective for the mouse EP1 receptor, we started with compound (), synthesized as previously described (). Diethyl dipicolinic Cy5.5 NHS ester () was reduced with NaBH to . Parikh–Doering oxidation of with sulfur trioxide–pyridine complex and DMSO produced the unstable alde
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Altogether the results of this study demonstrate that periph
2021-02-03

Altogether, the results of this study demonstrate that peripheral blockade of both ETA and ETB receptors reduces tumor-induced facial heat hyperalgesia and increased spontaneous grooming, without modifying ongoing nociception. It is possible to suggest that bosentan is acting upon both receptors pre
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DGK is a key enzyme in
2021-02-02

DGKδ is a key enzyme in glucose uptake in skeletal muscle. Chibalin et al. demonstrated that a decrease in DGKδ expression increases the severity of type 2 diabetes [20]. Additionally, DGKδ expression was increased in people who exhibited enhanced insulin sensitivity after exercise training [56]. Fr
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