• The atomic model of Ce

  2021-09-08

  

  The atomic model of Ce-INX6 provides an additional interpretation to the Ce-INX6ΔN mutant structure at low-resolution [41]. Given that the N-terminal residues from 2 to 19 are deleted in the Ce-INX6ΔN mutant, the N-terminal funnel found in the pore of the wild-type Ce-INX6 should be lost in the Ce-I

• Recently a lot of synthetic FFA agonists containing acidic m

  2021-09-08

  

  Recently, a lot of synthetic FFA1 agonists containing acidic moieties have been reported (Fig. 1) [13], [14], [15], [16], [17], [18], [19], [20], [21]. Notably, most of FFA1 agonists usually have the common biphenyl scaffold, which resulted in a relative deprivation in structure types of agonists [2

• Although it is well documented that FAAH substrates can

  2021-09-08

  

  Although it is well documented that FAAH substrates can elicit analgesic effects [for review see [47,48] and that systemic poly I:C administration induces mechanical allodynia in rats [14], to our knowledge this is the first study to demonstrate that enhancing FAAH substrate levels can modulate TLR3

• In addition for the function of

  2021-09-07

  

  In addition, for the function of GSNOR in brain, since GSNOR is the sole alcohol dehydrogenase isozyme in brain, the failure to detect ethanol dehydrogenase activity poses a problem if it is assumed that this enzyme has evolved and developed as a protective mechanism for ethanol detoxification in th

• A motivation for this study is the ability of

  2021-09-07

  

  A motivation for this study is the ability of PGD2 to inhibit hair lengthening (). Here we demonstrate that PGD2 also inhibits hair regeneration after wounding. Thus, PGD2 and Gpr44 inhibition of the hair follicle occurs in multiple contexts and may be exploited in future therapies. Pharmaceutical c

• To assess the roles of GPR and GPR

  2021-09-07

  

  To assess the roles of GPR120 and GPR40 in malignant properties of pancreatic cancer cells, we generated GPR120 and GPR40 knockdown (PANC-sh120 and PANC-sh40, respectively) dabigatran etexilate from PANC-1 (Fig. 2A). While no difference of cell growth rate between control PANC-RFP cells and PANC-sh1

• We also observed a significantly higher SLC A gene

  2021-09-07

  

  We also observed a significantly higher SLC10A1 gene expression and NTCP protein level among metastatic individuals vs. donor livers. Na+/taurocholate co-transporting polypeptide (NTCP), which is expressed on the basolateral membrane of hepatocytes and is primarily responsible for the uptake of bil

• Active compounds and were further tested and EC

  2021-09-07

  

  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

• While TUNEL staining is traditionally thought

  2021-09-07

  

  While TUNEL staining is traditionally thought to be an apoptosis marker, studies have shown that TUNEL can stain necrotic DBeQ synthesis [19], [20], [21]. Furthermore, DNA degradation has also been observed in necrotic cells [22]. TUNEL staining alone is therefore insufficient to distinguish apopto

• Growth hormone secretagogue receptor GHSR is a member of

  2021-09-07

  

  Growth hormone secretagogue receptor (GHSR) is a member of G-protein-coupled receptor family [3]. GHSR is predominantly expressed in human pituitary, rhypothalamus and hippocampus [4]. GHSR is also expressed in peripheral tissues including lungs, liver, kidney, and adrenal gland. In cardiovascular s

• In single channel studies Zn primarily

  2021-09-06

  

  In single channel studies, Zn2+ primarily inhibits GABA-A receptors through the reduction of channel opening probability (Smart, 1992, Smart et al., 1994). In slice recordings, Zn2+ significantly reduces phasic mIPSC event amplitude and kinetics, as well as desensitization kinetics (Barberis et al.,

• 72 9 There are multiple docking platforms suitable for use w

  2021-09-06

  

  There are multiple docking platforms suitable for use with nucleic 72 9 receptors. These include: DOCK v4-6 (UCSF) [[68], [69], [70]], AutoDock (Scripps) [71], AutoDock Vina (Scripps) [72], GOLD (Cambridge Crystallographic Data Centre) [73], Surflex-DOCK (BioPharmics) [74], Glide (Schrӧdinger) [75]

• The current lack of effective

  2021-09-06

  

  The current lack of effective treatments for primary or metastatic UM leaves a large therapeutic gap for patients and clinicians underscoring an urgent need for the identification of additional pharmacological targets for therapeutic intervention. As YAP-targeting strategies have remained elusive th

• br The inhibitory effect of ATP B knockdown

  2021-09-06

  

  The inhibitory effect of ATP7B knockdown on lysosomal exocytosis is likely mediated by the resulting oxidative stress induced by Cu, as exposure to oxidative stress induced by tert-Butyl hydroperoxide (TBHP) inhibited β-hex exocytosis as well, indicating that oxidative stress inhibits lysosomal ex

• br Materials and methods br Results br Discussion The

  2021-09-06

  

  Materials and methods Results Discussion The major findings of the present study are that: 1) the response to inverse agonists may be crossregulated by the activation of either fluoxetine hydrochloride H1 or H2 receptors, 2) histamine H1 and H2 receptor inverse agonists crossdesensitize th

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