• As part of a program

  2020-04-30

  

  As part of a program to explore the key binding interactions between the core of 1 and DGAT-1 a systematic analysis of the aminopyrimidine subunit was initiated. A potential approach to improving passive permeability within this series would be to increase lipophilicity via incorporation of substitu

• Given the importance of cysteine cathepsin inhibitors as put

  2020-04-30

  

  Given the importance of cysteine cathepsin inhibitors as putative therapeutic molecules and microbial virulence factors, we chose to investigate whether Yersinia enterocolitica may be a potent producer of such inhibitors. Y. enterocolitica is the most heterogeneous species within the genus Yersinia.

• Flexible alignment of isopropylphenylaminobenzimidazole with

  2020-04-29

  

  Flexible alignment of 7-isopropylphenylaminobenzimidazole 16 with the lead 2578 australia 1 was performed using MOE. It was found that the aryl group of compound 16, exemplified as a yellow circle in Figure 2, overlapped well with the corresponding alkyl chain of compound 1 as well as the other key

• In our previous research we have focused on the discovery

  2020-04-29

  

  In our previous research, we have focused on the discovery of novel VEGFR-2 inhibitors as anti-angiogenesis agents. Numbers of biphenyl-aryl urea incorporated with salicylaldoxime including BPS-7 have been developed as potent and selective VEGFR-2 inhibitors (Fig. 3) [12], [13], [14], [15], [16], [1

• EPAC activation in VSMCs and ECs reverses several processes

  2020-04-29

  

  EPAC activation in VSMCs and ECs reverses several processes involved in the development of in-stent restenosis. Of particular relevance is the ability of EPAC1 to induce SOCS3 gene expression, as SOCS3 exerts multiple protective effects in both cell types, while immunohistochemical studies have show

• Notably we demonstrated that EP EP receptor

  2020-04-29

  

  Notably we demonstrated that EP2/EP4 receptor-coupled activation of the cAMP signaling pathway accounted for both up-regulation of COX-2 and down-regulation of LOX, which is consistent with the roles of the cAMP signaling pathway in regulation of COX-2 and LOX by PGE2 in a number of other tissues or

• Several studies highlighted the potential of EOCs to

  2020-04-29

  

  Several studies highlighted the potential of EOCs to promote adverse effects on aquatic organisms. It was reported the toxicity of BPA to invertebrates and fish, and the effect of lipophilicity on toxicity was analyzed (Mathieu-Denoncourt et al., 2016). There was reported the effects of PPCPs on aqu

• Enolase as a plasminogen receptor and activator localized on

  2020-04-29

  

  Enolase, as a plasminogen receptor and activator localized on the surface of several helminths, can interact with the host fibrinolytic system (Yang et al., 2010, Du et al., 2009, de la Torre-Escudero et al., 2010). The enzyme is also one of excretory/secretory (ES) products in some helminths, such

• br Coactivator Binding Sets APC C Catalytic Core in Motion

  2020-04-29

  

  Coactivator Binding Sets APC/C Catalytic Core in Motion A coactivator not only recruits substrates to APC/C [18] (Figure 3B), but also stimulates repositioning of the catalytic core 19, 24. High-resolution cryo-EM maps of apo forms of APC/C without a coactivator show the catalytic core and platfo

• Intriguingly one E residue may serve

  2020-04-29

  

  Intriguingly, one E2 residue may serve as a molecular ‘gate’ to allow the C-terminus of ubiquitin to access the closed E2~Ub conformations favorable for ubiquitin transfer. This residue, Asp87 in UbcH5 family members, resides on one side of the opening that leads to the active site Cys (Fig. 4D). In

• We also observed reduced insulinotropic effects after

  2020-04-29

  

  We also observed reduced insulinotropic effects after intravenous administration of both GLP-1 and GIP with atropine, whereas no inhibition was observed by atropine of the direct effects of GLP-1 and GIP action on beta-cells in the islet experiments. This suggests that the reduction in circulating i

• Initially the cause of hypoglycemia was not apparent There w

  2020-04-29

  

  Initially, the cause of hypoglycemia was not apparent. There was no detectable lesion in the pancreas on plain computed tomography, and anti-insulin antibody was negative. Eight hours after hospital admission, his son discovered that the patient had accidentally taken glimepiride 3mg/day for 3 days.

• In conclusion we have found

  2020-04-29

  

  In conclusion, we have found that Egr1 can play an inhibitory role on DBH promoter-driven transcription. This inhibition requires a newly identified Egr1 response mdm2 p53 at the −227/−224 region of DBH promoter. This inhibition appears to result from Egr1 directly bound to the DBH promoter. We spe

• br Fragment based drug discovery FBDD is a powerful

  2020-04-29

  

  Fragment-based drug discovery (FBDD) is a powerful method to discover drug leads and has been widely adopted in both academia and industry. FBDD can be used to explore chemical INCB28060 space with libraries which are smaller in size, producing drug leads with high ligand-binding efficiency. It al

• Similarly LTD concentration dependently enhanced AQP express

  2020-04-29

  

  Similarly, LTD4 concentration-dependently enhanced AQP4 expression in astrocytes (Fig. 3). The LTD4-enhanced AQP4 expression was not affected by pranlukast but inhibited by Bay u9773, a non-selective CysLT1/CysLT2 receptor antagonist [33]. Because no selective CysLT2 receptor antagonists are current

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