• br Materials and methods br Results br

  2022-01-28

  

  Materials and methods Results Discussion Several histamine H3 receptor antagonists have progressed into clinical development for indications including Alzheimer's disease, schizophrenia, pain and narcolepsy. Each of the compounds studied herein has been extensively characterized in its own

• Compared to the other histamine

  2022-01-28

  

  Compared to the other DMH-1 receptor subtypes, the H3 receptor exhibits rather complex pharmacology, being subject to extensive splicing, leading to two major (H3-445 and H3-365) and possibly more functional human receptor isoforms; for a comprehensive review please see Leurs et al. (2005) and Bong

• br Histamine attenuates the cognitive impairing effects

  2022-01-28

  

  Histamine attenuates the cognitive impairing effects of early postnatal maternal deprivation Histamine acting on H2 receptors in the hippocampal CA1 region is able to reverse the deleterious effect of the exposure of rats to partial postnatal maternal deprivation on their memory consolidation of

• Cy3-UTP br Future perspectives sGC signaling is important in

  2022-01-28

  

  Future perspectives sGC signaling is important in the maintenance of multiple physiological functions. sGC is localized to cell membranes with both sGC Cys modifications and heme regulation identified as the crucial components in regulating sGC activity. Specifically, S-nitrosation of several com

• Conflict of Interest The authors

  2022-01-28

  

  Conflict of Interest: The authors have no conflicts of interest to declare. Acknowledgments Understanding Pulmonary Remodeling The effects of serotonin (5-hydroxytryptamine, 5-HT) class 2 receptors (5-HT2) on airway function and remodeling in respiratory disorders are unclear. Using murine pr

• We have previously established the pharmacokinetic profile a

  2022-01-28

  

  We have previously established the pharmacokinetic profile and effective dose of MNF in the rat [43] and demonstrated the effectiveness of MNF as an anticancer drug in PRL-3 Inhibitor and xenograft models [44]. Moreover, MNF was found to effectively block GPR55 signaling in tumor cells [21]. The co

• However even if immunological tests with the NQ

  2022-01-28

  

  However, even if immunological tests with the NQ21 peptide are mostly positive [8], it doesn't mean that the structure of the NQ21 peptide is the same as that of the corresponding gp120 region characterized by a long alpha helix. Therefore, the aim of the current work was to check whether the NQ21 p

• Even though for almost years GnRH was considered

  2022-01-28

  

  Even though for almost 30 years GnRH was considered the main neuropeptide regulating gonadotropin release in vertebrates, Tsutsui et al. (2000) discovered, in the Japanese quail, Coturnix japonica, a hypothalamic neuropeptide that directly inhibits gonadotropin release, and thus named as gonadotropi

• Our exploration of Domain focused on the

  2022-01-28

  

  Our exploration of Domain 1 focused on the role of the carbonyl linker in (). We found that replacement of this group by a methylene unit as in or direct attachment of the thiophene ring to the central aromatic core as in did not significantly impact potency. The thiophene ring in could be repla

• The two competitive bivalent GlxI inhibitors polyBHG nM

  2022-01-28

  

  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

• br Materials and methods br Results br Discussion The glucos

  2022-01-28

  

  Materials and methods Results Discussion The glucose transporter GLUT1 can be acutely activated or inhibited in L929 fibroblast DiscoveryProbe™ Inhibitor Library by a wide variety of reagents or nutrient conditions [[9], [10], [11], [12],36,50]. This abrupt change in the activity of GLUT1 o

• Our own search towards aryl imidazole derived GSMs led

  2022-01-27

  

  Our own search towards aryl-imidazole derived GSMs led to the discovery of the benzimidazole derivative (). It is one of the most potent GSMs to date, suffering however from sub-optimal drug-like properties. More recently, we have described the design and synthesis of bicyclic triazolo-derivatives,

• br STAR Methods br Acknowledgments We would

  2022-01-27

  

  STAR★Methods Acknowledgments We would like to thank V. Gladyshev (Harvard), H. Kornblum (UCLA), L. Greene (Columbia), and J. Baraban (Johns Hopkins) for constructive comments to the project and manuscript. We thank L. Gross and A. Kumar for assistance with editing. We thank L.M. Gerber and Z.

• The F P concentration reported for a

  2022-01-27

  

  The F6-P concentration reported for a resting rabbit muscle [20] reduced the KAapp for aldolase–FBPase complex more than 50 times compared to KAapp for aldolase–FBPase in the absence of effectors (Fig. 1b and Table 1). A standard assay for determination of FBPase activity in a complex with aldolase

• br Materials and methods br

  2022-01-27

  

  Materials and methods Results and discussion To analyze the dependence of lysosomal exocytosis on Cu we exposed HeLa Physcion mg to fresh buffer containing normal levels of free Ca (1mM) and measured β-hex levels in the extracellular medium, followed by measuring β-hex content in the total ce

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