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          With this goal in mind we proceeded2022-01-10  With this goal in mind, we proceeded to explore the C5-heteroaryl class of pyrazole-acids. Initial efforts, focused on a thiophene replacement, demonstrated little improvement. The 2-thiophene derivative (0.25μM and 0.24μM), a surrogate to the phenyl moiety, demonstrated only a modest boost in acti 
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          PD 169316 australia Compared to methadone or morphine bupren2022-01-10  Compared to methadone or morphine, buprenorphine is a partial mu-opioid agonist, which shows high affinity for, and slow dissociation from, mu-opioid receptors. This maintenance of homeostasis may help to counter the development of an overt withdrawal syndrome, and may explain the lower risk of deve 
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          br Introduction Opioids have long been used in pain manageme2022-01-07  Introduction Opioids have long been used in pain management [1]. However, their non-medical use has grown rapidly in the last few years. Hydrocodone (HYD) is one of the most widely used short-acting opioids; with over 136.7 million prescriptions in 2011 [2]. HYD is a semi-synthetic opioid used fo 
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          br Declaration of interest br Acknowledgments This work was2022-01-07  Declaration of interest Acknowledgments This work was financially supported by the National Natural Science Foundation of China (No. 31471615), the Introduction of Talent Research Start-up Fund of Anhui Polytechnic University (No. 2017YQQ017) and the Pre-research Project of National Natural Sc 
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          We report on four affected children2022-01-07  We report on four affected children from two unrelated consanguineous view more 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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          PF-06447475 br Materials and methods br Results and discussi2022-01-07  Materials and methods Results and discussion Conclusion Altogether, our data provide an unexpected insight into Cx26 trafficking pathway and gap junction assembly in the cochlea. Since many of the disease-causing mutations in GJB2 impair the trafficking and delivery of Cx26 to the cell surf 
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          The present study demonstrates that SNAP exhibits a toxic ef2022-01-07  The present study demonstrates that SNAP 37889 exhibits a toxic effect to these specific cell types, which is independent of endogenous expression of GAL receptor subtypes and leads to apoptosis. This conclusion is based on our findings that, although HMCB, HL-60 and SH-SY5Y cell lines differ in GAL 
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          br Materials and methods br2022-01-07  Materials and methods Results Bgal from Alteromonas sp. ML117 had an open reading frame of 3126 bp encoding 1042 amino Mercaptopurine residues with a predicted mass of 120 kDa and a theoretical pI (isoelectric point) of 5.44. The recombinant Bgal contained a His tag, as well as other addition 
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          In the FARM motifs of GGPPSs hydrophobic2022-01-07  In the FARM motifs of GGPPSs, hydrophobic KB-R7943 mesylate are replaced by aliphatic amino acids, which are more flexible residues and allow the entrance of longer substrates into the pocket (Wang and Ohnuma, 2000). It has been reported that the lepidopteran Manduca sexta CA possesses GGPP synthase 
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          1027 synthesis Depletion of PI P e g by knockout of PIPKI2022-01-07  Depletion of PI(4,5)P2, e.g. by knockout of PIPKIγ, also profoundly inhibits SV endocytosis (Di Paolo et al., 2004). Conversely, loss of the PI(4,5)P2-metabolizing PI-phosphatase synaptojanin or its recruitor endophilin stalls SV recycling at the level of clathrin-coated vesicles (Bai et al., 2010, 
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          Following nerve injury Shh expression is upregulated in2022-01-07  Following nerve injury, Shh expression is upregulated in neuronal cell bodies of the facial and sciatic nerves. Additionally, Shh appears to be required for normal regeneration in vivo, and promotes motor neuron survival in vitro (Martinez et al., 2015; Akazawa and Kohsaka, 2007). Based on these obs 
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          br Experimental br Acknowledgements This work was financiall2022-01-07  Experimental Acknowledgements This work was financially supported by Ministry of Knowledge and Economy (10032113) and Ministry of Education, Science and Technology (20100000297). Introduction To ensure accurate chromosome segregation, cohesion between sister chromatids must be maintained u 
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          Introduction Inorganic arsenic InAs species such2022-01-07  Introduction Inorganic arsenic (InAs) species such as arsenite (AsIII) and arsenate (AsV) are present in groundwater. Arsenic contaminated drinking water is a global public health issue because of its natural prevalence and toxicity. Long exposure to arsenic results in chronic effect in humans, inc 
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          br Materials and methods br2022-01-07  Materials and methods Results Discussion Metabolic abnormalities and systemic immune dysfunctions are common during HIV infection and/or antiretroviral therapy. Although some transcriptomic studies of HIV infection have revealed global changes in the mRNA and microRNA expression profiles (R 
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          While CART increased circulating levels2022-01-06  While CART increased circulating levels of GIP and GLP-1 in vivo, we were unable to detect any effect of exogenous CART on GIP and GLP-1 mRNA expression or GLP-1 secretion in vitro. There is no ready explanation for this discrepancy. The CART doses used (both in vivo and in vitro) have been shown to 
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