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br Regulation of gonadotropins by GnRH GnRH is released from
2022-06-29
Regulation of gonadotropins by GnRH GnRH is released from the hypothalamus, and its release pattern is known to be pulsatile. That is, the pulse frequency and amplitude of GnRH release vary physiologically during reproductive cycles in females, and differentially stimulate the production and rele
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We started our investigation by
2022-06-29
We started our investigation by evaluating the impact of changes to the piperidine moiety of (). As demonstrated with morpholine and piperazine , attenuation of nitrogen basicity resulted in complete loss of activity, suggesting that a basic heterocyclic nitrogen is important for potent inhibition
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Due to the therapeutic potential of GlyT inhibitors
2022-06-29
Due to the therapeutic potential of GlyT1 inhibitors, numerous drug screening campaigns have been started - and are still going on - which aimed at the identification of compounds with biological activity at or affinity for this drug target. For characterization of biological activity at GlyT1, tran
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Elevated methylglyoxal levels also contribute to carbonyl st
2022-06-29
Elevated methylglyoxal levels also contribute to carbonyl stress, cytotoxicity, DNA damage, apoptosis and cell death. These mechanisms may be important for normal aging of the nervous system as well as for the development of neurodegenerative diseases such as Alzheimer's and Parkinson's disease wher
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Although glycine receptors predominate in
2022-06-29
Although glycine receptors predominate in the brain stem and spinal cord, they are also expressed in higher brain regions such as the nucleus accumbens, frontal cortex, and hippocampus (Jonsson et al., 2012, Jonsson et al., 2009, Molander and Söderpalm, 2005b). A variety of drugs of abuse, including
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br Characterization and regional localization of Glu
2022-06-29
Characterization and regional localization of Glu transporters Molecular studies led to the description of five subtypes of plasma membrane Glu transporters termed in accordance to their human or rodent origin (Kanai and Hediger, 1992, Pines et al., 1992, Storck et al., 1992). In humans, these tr
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Glucose uptake a critical metabolic control point in
2022-06-29
Glucose uptake, a critical metabolic control point in glycolysis, is mediated by the GLUT (SLC2) family of integral membrane transporters (Mueckler and Thorens, 2013). GLUT1 (SLC2A1), one of the most well-studied members of the SLC2 family, exhibits a wide tissue distribution; cell surface expressio
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Instead our results reveal that autophagy controls the
2022-06-29
Instead, our results reveal that autophagy controls the membrane association of the cargo-selective SNX-BAR retromer assembly (comprised of the VPS35/29/26 trimer in association with SNX1/2 and SNX5/6), which has been demonstrated to promote GLUT1 surface recycling. Accordingly, GLUT1 localization i
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np e receptor Up to now the research about the effect of PAs
2022-06-29
Up to now, the research about the effect of PAs on inhibiting carbohydrase activity in vitro or reducing blood sugar level in vivo was mainly reported in PAs from grape seeds, Lepisanthes alata (Malay cherry) leaves, sorghum, pomegranate, cranberry and persimmon (Banerji and Banerjee, 2016, Barrett
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br Results br Discussion Our cardiomyocyte specific GR knock
2022-06-29
Results Discussion Our cardiomyocyte-specific GR knockout mice did not show spontaneous cardiac hypertrophy unless pressure overload was given to the heart. This finding is somewhat different from previous work of a cardiomyocyte-specific GR c14ɑ demethylase mouse model using GR-floxed mice w
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The development of metabolic stable non
2022-06-29
The development of metabolic stable, non-peptidergic galanin agonists could be the basis to clinical diagnosis and treatment of tumors with high levels of galanin receptor expression like gliomas and pituitary tumors. As for gliomas, penetration of the blood brain barrier by the compounds might be p
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Liver is the house for a
2022-06-29
Liver is the house for a variety of xenobiotic-metabolizing Birinapant that produce reactive oxygen species as well as reactive metabolites (Johansson et al., 2009; Noh et al., 2017; Puntarulo and Cederbaum, 1998). When the enzymes act upon pre- or pro-haptens, the chemicals would be activated to r
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Several classes of small molecule
2022-06-29
Several Ritonavir of small-molecule inhibitors of FBPase have been reported. These inhibitors can be structurally classified into two groups; non-phosphorus-based inhibitors and phosphorus-based inhibitors. In the former group, several chemotypes including anilinoquinazoline, indole dicarboxylic ac
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Here we dissect X chromosome dosage compensation DC in
2022-06-28
Here, we dissect X chromosome dosage compensation (DC) in C. elegans to determine the effect of chromatin modifications on higher-order chromosome structure during long-range gene regulation. DC is exemplary because it controls hundreds of genes simultaneously, it distinguishes X chromosomes from au
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This crosstalk may be responsible for
2022-06-28
This crosstalk may be responsible for the beneficial effects of histamine H2 receptor inverse agonists on Blebbistatin sale pathologies and may also explain unwanted effects of these drugs on other tissues. In this way, Allen et al. reported an anaphylactoid reaction following cessation of high-dos
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