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peptide receptors It appears that not all GPR agonists requi
2021-10-19

It appears that not all GPR119 agonists require a high dose to elicit acceptable peptide receptors control. According to preclinical data presented at the GTCbio Diabetes Summit, a 3mg/kg dose of AR-7947 was enough to induce similar blood glucose-lowering effects compared to those achieved by 30mg/k
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The two competitive bivalent GlxI inhibitors polyBHG nM and
2021-10-19

The two competitive bivalent GlxI inhibitors polyBHG2-62 (=1nM) and polyBHG2-54 (=0.3nM) () were designed based on the transition-state analog -(-bromophenyl--hydroxycarbamoyl) glutathione (BHG) by an examination of the X-ray crystal structure of human GlxI in complex with one CHG at each active sit
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Nuclear/Cytosol Fractionation Kit br Perspectives br Contrib
2021-10-19

Perspectives Contributors BP: study concept & design, literature review, data analysis & synthesis & presentation, primary draft of the manuscript; JDR: data analysis, Fig. 1 illustration, manuscript review & revision; ZP: study concept & design, manuscript review & edit; MI: manuscript review
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br A myriad of receptors in WM To
2021-10-19

A myriad of receptors in WM To complicate the picture, WM glia express numerous non-glutamatergic neurotransmitter receptors, a fact that is often underappreciated when considering pathophysiology. When examined in isolated optic nerve, a central WM tract completely devoid of neuronal synapses, r
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In a series of experiments the clotrimazole concentration
2021-10-18

In a series of experiments, the clotrimazole concentration was varied and the NSVDC channel conductances were calculated from Eq. (1) to obtain the dose-response relation (Fig. 3). The data were fitted to the Michaelis–Menten-type activation curve (Eq. (3)) and gave an EC50 value of 14 μM and a dose
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br Therapeutic approaches exploiting Cx function Due to thei
2021-10-18

Therapeutic approaches exploiting Cx43 function Due to their potential role in cancer metastasis, attempts have been made to alter connexin function to inhibit cancer growth. Therapeutic approaches include Cx43 peptide mimetics, Cx43 inhibitors, chemical agents capable of enhancing Cx43 function,
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Galactosidase Gal EC is an enzyme exoglycosidase and
2021-10-18

α-Galactosidase (α-Gal, EC 3.2.1.22) is an enzyme exoglycosidase, and the main role of this enzyme is the enzymolysis of α-galactoside. After this hydrolysis, galactosylation of cyclodextrins by the α-galactosidase occurs, thus forming α-galactosyl-cyclodextrin. This branched CD is easy to dissolve
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ZLN005 Further research should indeed focus on understanding
2021-10-18

Further research should indeed focus on understanding the nutritional value of food and its effect on metabolism, overall activation of metabolic NRs network. Moreover, given the prominent role of microbiota in the modulation of the FXR signalling (Degirolamo et al., 2014), there is enough impetus t
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Binding of FGFs to FGFRs
2021-10-18

Binding of FGFs to FGFRs leads to receptor dimerization, resulting in the transphosphorylation of a tyrosine in the activation loop of the kinase domain. Subsequently, the activated FGFRs phosphorylate their intracellular receptor substrates, particularly FGFR substrate 2 (FRS2) and phospholipase Cγ
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It is known that microglial function
2021-10-18

It is known that microglial function and morphology are closely related [20], but no studies have addressed whether neuroinflammation induced by alcohol might modify microglial Cefepime Dihydrochloride Monohydrate (i.e. morphology, neuroimmunochemical phenotype) through an eCB-dependent mechanism.
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According to the World Health Organization WHO
2021-10-18

According to the World Health Organization (WHO) classification, oligodendrogliomas or anaplastic oligodendrogliomas are primary neoplasms of the central nervous system, which are predominantly composed of cells morphologically resembling oligodendrocytes [23]. These tumors are often estimated to re
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Synthesis of these hydrazide inhibitors is outlined
2021-10-18

Synthesis of these hydrazide inhibitors is outlined in , . Condensation of Boc-carbazate with desired aldehyde resulted in hydrazone of type which were reduced to alkylated hydrazides using NaBH and toluenesulfonic acid. The resulting alkylated hydrazides were acylated with phloridzin chlorides
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The different NO stimulated and ODQ inhibited cNMP patterns
2021-10-18

The different NO-stimulated and ODQ-inhibited cNMP patterns in terms of absolute and relative magnitude and time course reported herein suggest distinct functional roles of cGMP, cCMP and cUMP. Therefore, it will be necessary to dissect cellular effects of these cNMPs in numerous cell systems. For t
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br Experimental br Acknowledgments This research
2021-10-18

Experimental Acknowledgments This research was supported by the Korea Research Foundation (2013R1A1A2007509). The authors thank to Dr. Moon Ho Son (Dong-A Pharm. Co. Ltd) for hGPR119 agonist activity assay. We also thank to Pharmacal Research Institute and Central Laboratory of Kangwon Nation
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During pain signal transmission glutamate is released
2021-10-18

During pain signal transmission, glutamate is released into the synaptic cleft, which, in turn, causes activation of N-methyl-d-aspartate (NMDA) receptors and hence neurotransmission across the synapse occurs. The synaptic concentration and resultant activity of glutamate are controlled by excitator
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