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The G protein coupled receptor GPR
2022-04-21

The G protein-coupled receptor, GPR40 (also called FFAR1) responds to medium and long chain unsaturated fatty acids, resulting in increase of insulin secretion during elevated glucose levels. The glucose dependency of insulin secretion makes this receptor a very good target for developing therapies
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br Acknowledgments br Introduction Lung cancer is a
2022-04-21

Acknowledgments Introduction Lung cancer is a common but extremely perilous cancer, with approximately 733,000 new incidences reported annually in China [1]. Lung cancer ranks highest in the causes of tumor-related mortality, accounting for approximately one quarter of all cancer deaths [2]. N
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Whereas Sororin is dispensable in the absence
2022-04-20

Whereas Sororin is dispensable in the absence of Wapl [14], overexpressed Haspin only partly supports cohesion in Sororin-depleted cells. Thus, although Haspin and Sororin have functional similarities, they are not fully redundant at the centromere. Haspin may have a mitosis-specific role in maintai
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l-ascorbic acid To investigate the simultaneous effects of p
2022-04-20

To investigate the simultaneous effects of possible confounding factors in the urinary 1-OHP excretion, multivariate regression analysis was performed (Table 3). Based on stepwise regression analysis, four independent variables (age, CYP1A1⁎4, GSTM1 and GSTP1 polymorphisms) entered into the final mo
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br Acknowledgments br Introduction Myelin one of
2022-04-20

Acknowledgments Introduction Myelin, one of the fundamental adaptations of vertebrates, is a multilamellar structure deriving from the spiral wrapping around the ezh2 inhibitor of the plasma membrane of myelin forming glia, oligodendrocytes in the central nervous system and Schwann cells (SC)
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Sennoside A Ubiquitination of GlyRs subunit on plasma membra
2022-04-20

Ubiquitination of GlyRs-α1 subunit on plasma membrane has been shown to initiate the receptor Sennoside A and subsequent degradation in lysosomes (Buttner et al., 2001). However, the specific E3 ligase responsible for GlyRs-α1 ubiquitination is largely unknown as yet. Also, the functional consequen
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br Materials and Methods br Results All of the studied
2022-04-20

Materials and Methods Results All of the studied transporter genes were expressed at detectable levels in all the analyzed samples at mRNA level by means of applied rt-PCR method (CTMdivi 1 was observed for ABCC4, ABCC1, ABCG2, SLC22A3, and SLC22A18 (less than 10% of mean expression for the ho
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k j and d were then submitted to metabolic stability
2022-04-20

15k, 15j and 14d, were then submitted to metabolic stability studies in human and mouse liver microsomes and permeability test with Caco-2 cells (Table 7). 15k, 15j and 14d all retained excellent permeability (Papp value greater than 15.2 × 10−6 cm/s) and displayed modestly improved metabolic stabil
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We report on four affected
2022-04-20

We report on four affected children from two unrelated consanguineous LY3009120 with moderate to severe ID associated with epilepsy and variable neuropsychiatric features. Using whole-exome sequencing, we identified homozygous missense variants in SLC45A1 (OMIM: 605763), which codes for a neuronal
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Herein in consider of the high similarity between GR
2022-04-19

Herein, in consider of the high similarity between GR HBP site and AR HBP site, we applied rational drug design strategy to develop AR/GR antagonists based on the chemical structures of antiandrogens and crystal structure of GR. The following bioassay identified Z19 as a dual AR/GR antagonist. Z19 i
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When testing the novel DA
2022-04-19

When testing the novel DA-CH3 peptide, it was found that it is superior to liraglutide in the MPTP mouse model of PD at a dose of 25 nmol/kg ip once-daily for 7 days. In the Rotarod and grip strength assessment, DA-CH3 was superior to liraglutide in reversing the MPTP–induced motor impairment. Dopam
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Here we used a designer receptors activated exclusively
2022-04-19

Here, we used a designer receptors activated exclusively by designer drugs (DREADD)-based chemogenetic approach in a novel Ghsr-IRES-Cre knock-in mouse line to test whether the activity of MBH GHSR neurons is required for the normal rebound food intake following fasting. We also used the Ghsr-IRES-C
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In order to test whether the enhanced hyperpolarization in t
2022-04-19

In order to test whether the enhanced hyperpolarization in the presence of increasing amounts of extracellular Ca2+ could be due to an ionophore effect of NS309, red cell uptake of 45Ca and partition of 45Ca into a water/n-octanol phase +/−100 μM NS309 were determined. However, no indication of iono
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Cx has been shown to be
2022-04-19

Cx45 has been shown to be serine phosphorylated by CaMKII, CK1, PKA, and MAPK in HeLa LLY507 [77], [78]. Phosphorylation by PKA and MAPK were associated with decreased junctional conductance [78], suggesting that phosphorylation of Cx45 may influence conduction properties. Overall, the roles of both
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Initially we carried out gap FRAP experiments using the
2022-04-19

Initially, we carried out gap-FRAP experiments using the two-photon configuration of the confocal microscope. A SR101-positive astrocyte was targeted and a 5 × 5 μm square area was exposed to a laser illumination (5 flashes of 5 s each during 25 s). This procedure resulted in a bleaching of this ast
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