• ICH induced striatal lesion produced

  2022-02-26

  

  ICH-induced striatal lesion produced a reduction of EAAT1 expression analogous to the decreased glutamate uptake at 6 h. The combined reduction of excitatory amino Reutericyclin transporters and of glutamate uptake activity might explain the well-known glutamate excitotoxicity following brain ischem

• Discrepancies in the reported results and conclusions from

  2022-02-26

  

  Discrepancies in the reported results and conclusions from different groups regarding studies in ghrelin−/− and ghsr−/− mice are likely explained by the mixed background of the mutant mice used in the different studies [35]; although in the case of mice exposed to HFD, exposure to a HFD immediately

• br Structures of human secretase Before the

  2022-02-26

  

  Structures of human γ-secretase Before the near-atomic resolution structures, the highest resolutions achieved for γ-secretase were 15 and 12Å [19, 21]. The 15-Å structure revealed a Prednisone chamber in the transmembrane domain and two pores at the top and bottom of γ-secretase, which were spec

• Compounds were tested for GPR activity in a functional assay

  2022-02-26

  

  Compounds , were tested for GPR40 activity in a functional assay monitoring calcium flux in CHO ampk pathway transiently transfected with human GPR40 gene. As shown in , compound was found to be a nanomolar GPR40 agonist, while compound was much less potent than . To explore the structure activit

• br Conclusion br Conflict of interest br Acknowledgements

  2022-02-26

  

  Conclusion Conflict of interest Acknowledgements Introduction The brain contains abundant fatty acids, which serve as constituents of membranes and as an energy source. In addition, fatty acids and their metabolites contribute to signal transduction between neurons or neurons and glial c

• This study introduces a mouse model carrying the point

  2022-02-26

  

  This study introduces a mouse model carrying the point mutation R258W in Ffar1, which abolishes the stimulation of insulin secretion in response to long chain fatty acids. The minimal genetic alteration mirrors the human situation and has the advantage over conventional knockout/congenic mouse model

• br Experimental procedures br Results br Discussion This

  2022-02-26

  

  Experimental procedures Results Discussion This study demonstrates that the genetic disruption or pharmacological inhibition of FAAH completely prevented all manifestations of pain symptoms in an NTG-induced migraine animal model. Thus, FAAH disruption or blockade abolished the activation o

• br Formation of secretory vesicles and trafficking toward pl

  2022-02-26

  

  Formation of secretory vesicles and trafficking toward plasma membrane Insulin and other components of the secretory granules are sorting and providing certain cues for BAMB-4 off the adjacent TGN membrane, forming immature secretory clathrin coated vesicles (Gehart and Ricci, 2013). Bin/Amphiph

• The lysine K specific demethylase KDM family

  2022-02-26

  

  The lysine (K)-specific demethylase 4 (KDM4) family is comprised of 4 isoforms, KDM4A to -D, also known as JMJD2A to -D. KDM4A, B, and C encode proteins consisting of a JmjC, a JmjN, two PHD, and two Tudor domains. KDM4D is unique within the KDM4 family in that it has neither PHD nor Tudor domains,

• Cy3 hydrazide br Acknowledgements This work was supported by

  2022-02-26

  

  Acknowledgements This work was supported by grants from the Agencia Nacional de Promoción Científica y Tecnológica (PICT2013-0495, PICT2016-1821), and from CONICET (PIP 2013-562), as well as from Fundación René Barón and Fundación Williams. Introduction Histamine poisoning, also known as scom

• Rigosertib The involvement of prostaglandins on the effects

  2022-02-25

  

  The involvement of prostaglandins on the effects induced by 1-nitro-2-phenylethane is similarly unlikely because vasorelaxation was not changed by indomethacin [20]. The inhibition of adenylyl cyclase with MDL-12330A [21] or cAMP-dependent protein kinase A with KT-5720 [22] also did not interfere wi

• br Conclusions br Acknowledgements The authors thank

  2022-02-25

  

  Conclusions Acknowledgements The authors thank Matt JM Wood and colleagues (AstraZeneca, UK) for permission to use logD and protein binding data presented in Sup. Table S2. Introduction The number of people suffering from type 2 diabetes mellitus (T2DM) has escalated worldwide as a consequ

• br FXR Agonists Azepinol b indole hEC nM

  2022-02-25

  

  FXR Agonists Azepinol[4,5-b]indole 1 (hEC50=600nM, efficacy (eff)=100%) was identified as a FXR agonist lead from a high-throughput screening effort. Structure–activity relationship (SAR) studies around the azepine ring demonstrated that dialkyl substitution at C-1 led to a 30-fold improvement in

• adenosine deaminase Due to the therapeutic potential

  2022-02-25

  

  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

• In silico analysis revealed structural similarities between

  2022-02-25

  

  In silico analysis revealed structural similarities between the CpMutY and the EcMutY which share typical domains and structural motifs (Fig. 5), common to a wide range of structurally related DNA repair enzymes. These include an endonuclease III domain, involved in excision of damaged pyrimidines,

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