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Molecular properties as well as metabolic stability
2021-09-27

Molecular properties as well as metabolic stability in rat and human liver microsomes for the most active nitro (), nitrile (), methylsulfone (), and sulfonamides () analogues were measured (). All these derivatives possessed excellent membrane permeability as measured in the Pampa assay and further
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Although it is mainly a glial protein
2021-09-27

Although it is mainly a glial protein, 5–10% of total GLT-1 represents a neuronal form located at presynaptic terminals, but its physiological role remains elusive (for discussion, see (Rimmele and Rosenberg, 2016)). Nevertheless, this amount might be significant since GLT-1 has been estimated to be
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br Acknowledgements This work was supported by the Science a
2021-09-27

Acknowledgements This work was supported by the Science and Technology Department of Hubei Province (No.2016CFB368) and the National Natural Science Foundation of China (No. 81201053). Introduction L-Glutamate (glutamate) is the most important excitatory neurotransmitter of the central nervou
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Regulation of pancreatic and cell mass has been
2021-09-26

Regulation of pancreatic α and β cell mass has been extensively studied and hotly debated, due to potential therapeutic implications. Early claims of Angptl8 as “betatrophin” and Angptl4 as a regulator of glucagon secretion and α cell proliferation (Yi et al., 2013, Ben-Zvi et al., 2015) have not st
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The significance of A and tau as therapeutic
2021-09-26

The significance of Aβ and tau as therapeutic targets is not only derived from pathological evidence of postmortem brain but also from biochemical analysis of cultured human neurons. This is largely based on the induced pluripotent stem cell (iPSC) technology that has been established to study Aβ, t
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br Acknowledgment br Introduction Non steroidal anti
2021-09-26

Acknowledgment Introduction Non-steroidal anti-inflammatory drugs (NSAIDs) are widely utilized to treat pain and inflammation [1], but their chronic use is hindered by a variety of potentially serious adverse events that include gastrointestinal (GI) mucosal lesions, bleeding and perforations
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Notwithstanding the functioning of galaninergic system may b
2021-09-26

Notwithstanding, the functioning of galaninergic system may be even more complex (Fuxe et al., 2012). Some studies present evidence that GAL2 receptors might form heteroreceptor complexes with neuropeptide Y1 receptors in lxr agonist of amygdala (Narváez et al., 2015a), DRN (Díaz-Cabiale et al., 20
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In order to establish proper folding
2021-09-26

In order to establish proper folding and enzymatic activity, G9a and GLP methyltransferases each contain four structural zinc ions. Both sta 90 contain two distinguishable types of zinc fingers; three Zn(II) ions are chelated in a triangular cluster by 9 cysteines (b, top left), whereas one Zn(II)
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Introduction Hedgehog HH signaling regulates development
2021-09-26

Introduction Hedgehog (HH) signaling regulates development, cell proliferation, and tissue repair [1], [2], [3]. In mammals, HH signaling is activated by 3 ligands: Sonic hedgehog (SHH), Indian hedgehog (IHH), or Desert hedgehog; SHH is the most widely expressed in adult tissues [3]. The primary re
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The treatment target which aims at diagnosing of HIV infecte
2021-09-24

The “90-90-90 treatment target” which aims at diagnosing 90% of HIV-infected individuals, treating 90% of those diagnosed and achieve viral suppression for 90% of treated individuals, is a key strategy to achieve one of the sustainable development goals (SDG) of ending AIDS as a public health threat
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Nevertheless in the brain we found that
2021-09-24

Nevertheless, in the brain, we found that trehalose phosphorylates AMPK, which is a metabolic sensor. AMPK is known to be transiently activated in muscle by acute exercise [21,22]. Bayod et al. also reported that AMPK was significantly activated in both the cerebral cortex and hippocampus in exercis
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PU-H71 To synthesize the azaindole based compound Suzuki cou
2021-09-24

To synthesize the 7-azaindole based compound , Suzuki coupling of 6-chloro-7-azaindole with 4-CFO-phenylboronic PU-H71 was carried out in the presence of Pd(dppf)Cl·CHCl to supply biaryl in quantitative yield (). Iodination at the C-3 position resulted 3-iodo-7-azaindazole . Alkylation of the -1 pos
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Besides the described effects on gross locomotor function im
2021-09-24

Besides the described effects on gross locomotor function, impairment of visuo-motor coordination and fine-motor skills like resting tremors, bradykinesia and rigidity were also investigated, reflecting on the symptomatology of Parkinson's disease in humans (Inzelberg et al., 2008). Preclinically, t
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gpr55 agonist The modulation of the activity of the Gardos
2021-09-24

The modulation of the activity of the Gardos channel by the chemokines IL-8 and RANTES was observed in the Duffy-positive but not in the Duffy-negative SSRBCs. This finding is consistent with the previous observation on normal red blood gpr55 agonist (AARBCs) described by Rivera et al. [10]. Altoge
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Together the epigenetic interplay revealed in this
2021-09-24

Together, the epigenetic interplay revealed in this study enabled us to expand the therapeutic potential of EZH2is from hematological malignances to solid tumors. In solid tumors, EZH2i-driven transcriptional changes are shown to be dispensable of H3K27me-regulated transcriptional network. Instead,
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