• Determination of enzyme activity differs from other

  2022-01-18

  

  Determination of enzyme activity differs from other analytical procedures. In this omecamtiv case, instead of enzyme concentration, a substrate depletion or product accumulation should be monitored. Such approach allows calculating activity basis of calibration curves performed for enzymatic reacti

• br Acknowledgments br The study was funded by

  2022-01-18

  

  Acknowledgments The study was funded by the European Commission FP7-project Beta-JUDO (Grant 279153), and Swedish Diabetes Association (Grant DIA 2013-043) and Family Ernfors Foundation (Grant 150430). Free fatty BLU 9931 receptors (FFARs) represent a family of G-protein coupled receptors (

• br Materials and methods br Results br Discussion Cell

  2022-01-18

  

  Materials and methods Results Discussion Cell migration not only plays major roles in physiological events, such as embryo implantation, embryogenesis, morphogenesis, neurogenesis, angiogenesis, wound healing and inflammation [[29], [30], [31]], but it is also implicated in the pathophysiol

• Recent findings of us suggest that compounds that inhibit bo

  2022-01-17

  

  Recent findings of us suggest that compounds that inhibit both FAAH and TRPV1 may be more efficacious in pain relief than those targeting only one such protein. As continuation of our efforts to identify new molecules able to target simultaneously both FAAH and TRPV1 receptors, we hypothesized that

• The other possibility for the lack of effects

  2022-01-17

  

  The other possibility for the lack of effects of H1 receptor agonists, e.g. histamine, on the NMDAR-mediated responses is that other neurotransmitters may cause more profound effects than histamine on the gliotransmitter release from astrocytes. For example, recent studies showed that noradrenaline,

• br Acknowledgments br Introduction The incidence of cholangi

  2022-01-17

  

  Acknowledgments Introduction The incidence of cholangiocarcinoma (CCA), a malignant tumor found in both intra- and extra-hepatic biliary epithelia [1], has been increased worldwide over the past two decades [2]. The prognosis of CCA patients are generally poor, due to the lack of early detecti

• Previous studies have shown that zinc interacts with

  2022-01-17

  

  Previous studies have shown that zinc interacts with other allosteric modulators at the glycine receptor (Kirson et al., 2013, McCracken et al., 2010, McCracken et al., 2013). Of note, the chelation of zinc via tricine decreases the effects of alcohol at α1-, α2-, and α3-containing glycine receptors

• LPCs have been previously described as potential anti diabet

  2022-01-17

  

  LPCs have been previously described as potential anti-diabetic factors due to stimulation of secretory activity from the isolated rodent pancreas, L-type cells, ands insulin-producing cell lines, with LPC 18:1 as the main structure of interest (Soga et al., 2005, Sakamoto et al., 2006, Overton et al

• The mammalian AMPA receptor protein family comprises four su

  2022-01-17

  

  The mammalian AMPA receptor protein family comprises four subunits, termed GluR-A through GluR-D (or GluR1 through GluR4), which form hetero-tetrameric receptor complexes Dingledine et al. 1999, Rosenmund et al. 1998. These subunits possess distinctive intracellular C-terminal domains that can be gr

• The regulation of casein expression during lactation is a

  2022-01-17

  

  The regulation of casein expression during lactation is a complex process involving a coordinated response at several levels. A variety of hormones are known to play roles in lactogenesis, such as prolactin (PRL), insulin, and hydrocortisone, and there is now increasing evidence that growth factors,

• NSC 319726 synthesis Through the analysis of various synthet

  2022-01-17

  

  Through the analysis of various synthetic GPR40 agonists as reported in literature, we found that a number of these compounds contained a phenylpropanoic NSC 319726 synthesis motif which was inspired from naturally occurring medium to long chain fatty acids. For instance, in the early period of dis

• br Declaration of interest br Acknowledgments br This work

  2022-01-17

  

  Declaration of interest Acknowledgments This work was supported by grants from the Polish National Science Centre (PRELUDIUM grant no. 2013/11/N/NZ5/00270) and the European Commission FP7 Project Beta-JUDO (grant number 279 153), European Union EIT Health project DeTecT2D, Swedish Diabetes A

• In addition to removing proteins and organelles related

  2022-01-17

  

  In addition to removing proteins and organelles related to iron and lipid metabolism, an alternative mechanism by which autophagy promotes ferroptosis is through the formation of the BECN1-solute carrier family 7 member 11 (SLC7A11) complex [42,43]. SLC7A11 is the main component of the antiporter sy

• haloperidol haldol Recent studies in our laboratory demonstr

  2022-01-15

  

  Recent studies in our laboratory demonstrated that several histamine H1 receptor antagonists induce apo A-I gene expression while histamine itself represses it [20]. In humans, there are three histamine receptor genes (H1, H2, and H3) that code for G-protein-coupled receptors (GPCR's) which bind his

• Arena Pharmaceutical introduced a biaryl sulfone derivative

  2022-01-15

  

  Arena Pharmaceutical introduced a biaryl sulfone derivative with antagonistic activity at H3Rs known as APD-916, ((R)-1-(2-(4'-(3-methoxypropylsulfonyl)biphenyl-4-yl)ethyl)-2-methylpyrrolidine), which was rationally designed from corresponding sulfonamides in order to yield compounds with short dura

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