• During the past decade it became increasingly clear that the

  2019-07-22

  

  During the past decade, it became increasingly clear that the affinity and efficacy of small agonists acting on the orthosteric binding site of a GPCR can be modulated by ligands that bind to a topographically distinct (allosteric) binding site on the same GPCR molecule 33, 39, 40, 41, 42. This allo

• br Conflict of interest statement br Acknowledgement The res

  2019-07-19

  

  Conflict of interest statement Acknowledgement The research leading to these results has received funding from the European Union Seventh Framework Programme (FP7/2007-2013) under grant agreement n° 278742 (Eurosarc) Introduction Pseudomyogenic hemangioendothelioma/epithelioid sarcoma-like

• br Conclusions We can conclude that Arg is important

  2019-07-19

  

  Conclusions We can conclude that Arg293 is important but not indispensable for MeGlcA recognition by EcXyn30A since the R293A variant still retains activity and preference for MeGlcA-substituted substrates. The substrate specificity of GH30_8 glucuronoxylanases is most probably determined by an o

• br Conclusion The past few years

  2019-07-19

  

  Conclusion The past few years have witnessed substantial progress in understanding the structural mechanisms of substrate recognition and the reactions catalyzed by the O-GlcNAc-cycling enzymes, but more work remains. In particular, future research will be needed to establish how OGT and OGA inte

• Introduction Excessive exposure to ultraviolet UV

  2019-07-19

  

  Introduction Excessive exposure to ultraviolet (UV) irradiation from the sun injures human skin, which might lead to premature aging and skin pathologies [1], [2]. Chronic exposure to UV (especially ultraviolet-B, UVB) irradiation could profoundly affect the skin epidermis, interfering with the ker

• The expression of EBI has been found to be

  2019-07-19

  

  The expression of EBI2 has been found to be dysregulated in several types of B cell malignancies and is thus reduced in e.g. diffuse large B-cell lymphomas [12] and chronic lymphocytic leukemia [13] and increased in post-transplantation lymphoproliferative disorders (PTLDs) [14]. EBI2 is also highly

• br Results and discussion br Conclusion We have

  2019-07-19

  

  Results and discussion Conclusion We have constructed a series of potent and greatly selective DPP-4 inhibitors with pyrazolo[1,5-a]pyrimidin-7(4H)-one core surrogates. The modification of the core led us to b2 which has IC50 of 80 nM and > 1000 fold selectivity over DPP-8 and DPP-9. We utiliz

• CHAPS Further indirect evidence supporting an

  2019-07-19

  

  Further indirect evidence supporting an important role of DPP-4 in the modulating the actions of both incretins comes from the observations that analogues of GLP-1 and GIP, modified to be resistant to DPP-4 cleavage, were subsequently shown to have greater metabolic stability in vivo which was assoc

• Lately using receptor TM peptides

  2019-07-19

  

  Lately, using receptor TM peptides, BiFC and PLA experiments, we have also obtained experimental evidence for the tetrameric structure of A1R–D1R, which explains the canonical interaction on Gi and Gs, respectively (Fig. 2). We have demonstrated for the first time the presence of this heterotetramer

• In order to gain further insights

  2019-07-19

  

  In order to gain further insights into the role of peptidases in B. xylophilus, four cysteine proteases highly secreted by B. xylophilus (Cardoso et al., 2016) were selected four further characterisation. Materials and methods Results and discussion Structural prediction and analysis The i

• Materials and methods Cell culture and receptor gene transfe

  2019-07-19

  

  Materials and methods Cell culture and receptor gene transfection. PC12 Fmoc-Lys(Boc)-OH were purchased from the Institute of Cell Biology, Chinese Academy of Sciences, Shanghai, China. The cDNA for mouse CysLT1 or CysLT2 receptor (mCysLT1 and mCysLT2, subcloned into pcDNA3.0) was kindly gifted by

• Compound was advanced to a chronic efficacy study in db

  2019-07-18

  

  Compound 52 was advanced to a chronic efficacy study in db/db mice maintained on a high fat diet. Animals were dosed with 0.5% methylcellulose vehicle, Simeprevir chemical 52 (1, 3 or 15mg/kg, po, Q.D.) or 1 (0.3mg/kg) for 14days. Over the course of the study body weight and food intake were measure

• In vitro study indicated the cell

  2019-07-18

  

  In vitro study indicated the cell death of hippocampal neurons was mediated by DAPK1 following ceramide-3 treatment (Pelled et al., 2002). the same study showed that DAPK1-deficient mice treated by acyl ceramide exhibit a less sensitivity to apoptosis, this proposed that DAPK1 plays a central role i

• The CysLT receptor antagonist BayCysLT RA significantly supp

  2019-07-18

  

  The CysLT2 receptor antagonist BayCysLT2RA significantly suppressed multiple antigen challenge-induced infiltration of eosinophils and mononuclear Angiotensin 1/2 (1-5) into the lung, indicating that CysLT2 receptor activation is involved in leukocyte migration. In contrast to the present finding, B

• Prostaglandins PGs are lipid mediators

  2019-07-18

  

  Prostaglandins (PGs) are lipid mediators that exhibit a variety of physiological properties by interacting specific G protein-coupled receptors (GPCRs) [10]. PGD2 is synthesized from PGH2 through two distinct PGD synthases; lipocalin-type PGD synthase (L-PGDS) and hematopoietic PGD synthase (H-PGDS)

15429 records 983/1029 page Previous Next First page 上5页 981982983984985 下5页 Last page