• We notice that previous reports

  2021-12-01

  

  We notice that previous reports of arsenic exposure are not completely consistent with each other, in terms of exposure-changed histone acetylations. In an early investigation, As exposure (7.5 μM) of HepG2 ddhUTP increased H3K9ac after 24 h, when analyzed by methods of immunofluorescence and Weste

• br ABT aR aR methyl hexahydropyrrolo b

  2021-12-01

  

  ABT-288 (2-[4'-((3aR,6aR)-5-methyl-hexahydropyrrolo[3,4-b]pyrrol-1-yl)-biphenyl-4-yl]2H-pyridazine-3-one) is a selective H3R antagonist/inverse agonist developed by Abbott. Structurally, it is a compound with molecular weight (MW) 372.46 g/mol, three H-bond acceptors (HBA), and Moriguchi LogP (MLo

• Taken together this study provides the proof of concept that

  2021-12-01

  

  Taken together, this study provides the proof of concept that our novel heterologous human/rat HER2-specific T cell vaccine HuRt-TEXO, which is capable of stimulating both humoral and CTL responses leading to potent antitumor immunity through the circumvention of HER2 tolerance in double transgenic

• br Structural Homology and Functional Implications Amino aci

  2021-12-01

  

  Structural Homology and Functional Implications Amino Erlotinib receptor sequence analyses of Disp and the Shh receptor Ptch indicate that both proteins share structural homology with a family of bacterial efflux pumps that function in resistance, nodulation, and division (RND) transporter compl

• In summary we have designed and explored

  2021-12-01

  

  In summary, we have designed and explored synthetic routes towards novel acylsulfamoyl benzoxaborole-based HCV NS3 protease inhibitors. Interestingly, the resulting, unoptimized P1–P3 and P2–P4 macrocyclic inhibitors were equipotent in an enzyme assay and somewhat less potent in replicon assays, com

• br Methods br Results and discussion br

  2021-12-01

  

  Methods Results and discussion Conclusions In this work, 100-ns MDSs were applied on the WT and on the R155K and D168A single point mutations of the NS3/4A protease in the apo form and in complex with ASV, a current drug in phase III clinical trials. According to the PCA, these two mutation

• br Materials and methods br Results br Discussion I have

  2021-12-01

  

  Materials and methods Results Discussion I have identified an alternative transcript of the integrin αE gene that is abundantly expressed in testis. In humans, this transcript (hAED) includes part of intron 26 and exons 27, 29, 30, and 31 of the conventional αE gene and Northern analysis in

• The characterization of Da CTSL shows that it preferentially

  2021-12-01

  

  The characterization of Da-CTSL1 shows that it preferentially cleaves Z-FR-AFC (Fig. 8), which has a herpes simplex virus phenylalanine at P2 and Da-proCTSL1 is autocatalyzed at pH 8.0 releasing an activated Da-CTSL1 that exhibits optimal activity at pH 8 indicating that the enzyme when secreted by

• The absence of direct oxidation of Fe by

  2021-12-01

  

  The absence of direct oxidation of Fe2+ by L1 in experiments in solution would be consistent with the recognized low O2 affinity of sGC. It is known that, in KU-0063794 with other hemoproteins, such as globins and heme-containing oxygenases with a Fe2+-proximal histidine linkage, sGC prevents oxida

• Over the last few years experimental evidence for

  2021-12-01

  

  Over the last few years, experimental evidence for the involvement of Epac1 in cancer progression is beginning to emerge (Almahariq et al., 2015, Banerjee and Cheng, 2015, Parnell et al., 2015, Parnell et al., 2015, Schmidt et al., 2013). For example in melanoma cells, silencing of Epac1 attenuates

• Pharmacologic approaches of inhibiting GSNOR activity have r

  2021-12-01

  

  Pharmacologic approaches of inhibiting GSNOR activity have reached the point of clinical development with the recent announcement of the first cystic fibrosis patients treated with the first-in-class GSNOR inhibitor, N6022 (N30 Pharmaceuticals). Clinical development is ongoing for other indications

• br Manganese based imaging probes br Imaging of

  2021-12-01

  

  Manganese-based imaging probes Imaging of vesicular monoamine transporter 2 (VMAT2) Imaging of sulfonylurea receptor 1 (SUR1) In mammals, insulin secretion is mediated by the membrane potential of pancreatic β-cells. Increases in glucose levels lead to blocking of ATP-sensitive potassium ch

• br Results and discussion br Conclusion In

  2021-12-01

  

  Results and discussion Conclusion In summary, starting from our previous lead Protease Inhibitor Library 1, we replaced the 5-nitropyrimidine core with pyrimidopyrimidine to obtain a series of novel compounds as drug candidates of GPR119 agonist for treatment of type 2 diabetes. Some derivati

• No compounds in this series showed

  2021-12-01

  

  No compounds in this series showed any appreciable activity at GlyT2 and can thus be considered GlyT1-selective. For the GlyT2 IC was >20μM. To determine CNS penetration of -(2-(azepan-1-yl)-2-phenylethyl)-benzenesulfonamides, select compounds were evaluated in a cassette CNS exposure screen in ma

• An alternative approach to improving pharmacokinetic profile

  2021-12-01

  

  An alternative approach to improving pharmacokinetic profile while retaining high GlyT1 potency was also pursued. Libraries were prepared in which potency enhancing piperidine C4 substituents were combined with clearance lowering truncated alkyl sulfonamides. The result was the discovery of (). Unl

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