• 78 2 receptor Here we studied the effects of

  2022-07-19

  

  Here we studied the effects of BZ flurazepam (FZ) at high doses in acute and chronic settings of tolerance and dependence in GluR-A−/− mice (Zamanillo et al., 1999). We used measurements in which the phenomenon of “learning while intoxicated” should play only a minor role in order to find out the si

• GK also called hexokinase IV or D is a

  2022-07-19

  

  GK, also called hexokinase IV or D, is a glycolytic enzyme that converts 5-alpha reductase inhibitors to glucose-6-phosphate. GK has unique characteristics compared with those of the ubiquitously expressed hexokinase isoforms I–III, and is predominantly expressed in the pancreas and liver. In pancr

• The sexual dimorphism in dlGALR a and

  2022-07-19

  

  The sexual dimorphism in dlGALR1a and dlGALR1b receptors found in the gonads of adult fish led us to hypothesize that the gene expression difference between female and males might be attributed to the differences in steroid production between female and male gonads. Interestingly we have found that

• The overall very satisfactory potency profile of

  2022-07-19

  

  The overall very satisfactory potency profile of compounds 7a–l suggests that 1,3,4-thiadiazole-2-carboxamide moiety was a suitable periphery group to add to the 3-phenylpropanoic GDC-0941 core in order to improve affinity to FFA1. The agonist activity in this series appears to be particularly sens

• As a part of our continuing efforts towards discovery of

  2022-07-18

  

  As a part of our continuing efforts towards discovery of new class of compounds against different therapeutic areas and based on the literature reports, we designed a dual pharmacophore which possess a long aliphatic chain of free fatty acids and a phenyl propanoid part of known GPR40 agonists. Here

• In summary although there are still several important questi

  2022-07-18

  

  In summary, although there are still several important questions open on the mechanisms that trigger FAK nuclear localization and FAK-dependent gene regulation, Cardoso et al. (2016) provide important new insights on FAK/MEF2-mediated initiation of cardiac hypertrophy. Acknowledgments The author

• Several named antagonist ligands have

  2022-07-18

  

  Several named antagonist ligands have figured noticeably in preclinical studies, with proved clear ability to release neurotransmitters and having efficacy in preclinical animal models. Consequently, this has encouraged ongoing research on improved agents with potency, selectivity, and better drug-l

• br Materials and methods br Results

  2022-07-18

  

  Materials and methods Results Discussion CRC and PC occupy a good share in cancer-related deaths worldwide. CRC is a common gastrointestinal malignancy with a growing incidence whereas PC is one of the most dreadful malignancies with extremely poor survival rates. Though over the past decad

• We have previously reported on the effects of replacing the

  2022-07-18

  

  We have previously reported on the effects of replacing the isoquinoline P2∗ moiety with a naphthalene ring and modifying the connectivity for this element to the P2 proline ring, as demonstrated by compounds – (). Therein, it was hypothesized that the reduced potency observed with – when compared t

• In order to better manage

  2022-07-18

  

  In order to better manage HBV infection and related liver diseases, it is critical to develop new antiviral strategies to increase the rate of functional or complete cure of HBV infection (HBsAg loss and cccDNA elimination), achieving more than viral suppression (Zeisel et al., 2015). As a result, m

• br Rho family GTPases are molecular

  2022-07-18

  

  Rho-family GTPases are molecular switches; most which cycle from an ‘on’ GTP bound state to an ‘off’ GDP bound state, driven by GEFs (guanine nucleotide exchange factors) and GAPs (GTPase-activating proteins) respectively. Association with lipid membranes through a lipid (farnesyl or geranylgerany

• vx 765 The experiments reported herein were designed to

  2022-07-18

  

  The experiments reported herein were designed to test whether co-expression of MRP and GSTP1-1 offers a level of protection from certain cytotoxic drugs not achieved by the expression of either protein alone. This was accomplished by stable transfection with expression vectors into MCF7/WT cells, w

• Glycogen synthase kinase GSK is an evolutionarily conserved

  2022-07-16

  

  Glycogen synthase kinase-3β (GSK-3β) is an evolutionarily conserved serine/threonine kinase that plays multifaceted role in diverse cellular and neurophysiological processes [8]. GSK-3β is regulated by inhibitory serine and stimulatory tyrosine phosphorylation on Ser9 and Tyr216 respectively [9]. Dy

• Lipid sensing GPCRs as therapeutic targets G protein

  2022-07-16

  

  Lipid-sensing GPCRs as therapeutic targets G-protein-coupled receptors (GPCRs) comprise a family of cell-surface receptors that respond to various extracellular stimuli such as light, odorants, neurotransmitters and hormones, and trigger a cascade of intracellular signaling. There are approximately

• PF 1022A br Methods br Results br

  2022-07-16

  

  Methods Results Discussion Our results show that the DRG and the spinal cord express significant amount of GPR35, a previously orphan Gi protein coupled receptor whose stimulation with zaprinast or with KYNA may reduce inflammatory pain. The receptor is also expressed in primary cultures of

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