• Molecular docking study of compound was performed

  2021-01-20

  

  Molecular docking study of AMG-458 was performed using the Schrödinger Small-Molecule Drug Discovery Suite taking advantage of known X-ray crystal structures of activated EPAC2 protein. The model shows that compound occupies the CBD of EPAC2 and forms hydrogen bonds with Arg448 and the cyano-hydr

• As proof of principle the effect of selective

  2021-01-20

  

  As proof of principle, the effect of selective blockade was measured using TAK-044, a peptide antagonist with approximately 250-fold selectivity for the ETA subtype over ETB as measured by ligand binding in the human heart. A 30-mg infusion over 15 minutes of TAK-044 (providing a serum concentration

• br Materials and methods br Results br Discussion Anti

  2021-01-20

  

  Materials and methods Results Discussion Anti-EGFR therapy for epithelial carcinomas has important clinical significance, but widespread intrinsic or acquired resistance seriously affects efficacy. Mutation and heterodimerization of EGFR are the two main causes of resistance to anti-EGFR th

• br Acknowledgments br Introduction Ubiquitin ligases limit t

  2021-01-19

  

  Acknowledgments Introduction Ubiquitin ligases limit the stability and activity of substrates by targeting them for proteasomal-dependent degradation. Siah is a two-member family of ubiquitin ligases implicated in control of key cellular processes. Among those, Siah ligases control prolyl hydr

• In the context of E ligase drug

  2021-01-19

  

  In the context of E3 ligase drug discovery, it is critical to identify the appropriate E2/E3 substrate pairing to ensure the development and use of the most physiologically relevant screening assay. There have been many reports of limited E2/E3 activity profiling with a small number of E2 and E3 pkr

• The photocleaving properties of were studied by performing X

  2021-01-19

  

  The photocleaving properties of 1 were studied by performing ΦX174 photocleavage assays. Light irradiation of the mixtures of increasing amounts of 1 with supercoiled DNA caused>90% supercoiled form relaxation and approximately 5% of linearization for the higher concentrations of 1 (1:10bp and 1:2bp

• We next focused our design

  2021-01-19

  

  We next focused our design building into the ribose binding site, which had not been yet utilized in this effort. Compounds bearing a series of five-membered aromatic heterocycles (compound , ) showed reduced inhibition of the Gram-positive isozymes compared with compound , but a 20-fold improved po

• Cryptosporidium is a protist causing serious diarrhea in hum

  2021-01-19

  

  Cryptosporidium is a protist causing serious diarrhea in humans and other animals (Bouzid et al. 2013). In its mitosomes, the most reduced forms of mitochondria, it is assumed that the membrane potential is generated by a simple respiratory chain consisting of transhydrogenase, type II NADH dehydrog

• ubenimex DDR expression is upregulated in the glomeruli and

  2021-01-19

  

  DDR1 expression is upregulated in the glomeruli and tubules of injured kidneys [7], [8], [19]; however, what role this receptor plays in kidney resident ubenimex is unclear. A plausible hypothesis is that DDR1 might contribute to kidney injury by directly exerting a pro-fibrotic action. In favor to

• A growing body of data indicates that endothelial NOS

  2021-01-19

  

  A growing body of data indicates that endothelial NOS (eNOS) is a rate-limiting enzyme for the synthesis of nitric oxide (NO), its downstream leukotriene molecule. High pathological concentrations of NO produced from inducible NO synthase (iNOS) induce apoptosis, whereas a reduction in the concentr

• Materials and methods br Results Assay of botulinum toxin

  2021-01-19

  

  Materials and methods Results Assay of botulinum toxin activity is critical for the risk-assessment, diagnosis, and treatment of botulism cases. The frequently encountered active forms of the toxin are; L chain (inside intoxicated neuronal cells), BoNT (in the blood stream of a botulism patient,

• Cyclosporine NEORAL Oral Solution Novartis

  2021-01-19

  

  Cyclosporine (NEORAL® Oral Solution, Novartis) is an immunosuppressant widely used in organ transplantation and many other clinical conditions [12]. It undergoes extensive hepatic and intestinal biotransformation mainly via the metabolizing enzyme, CYP3A4 [[12], [13], [14], [15]]. Considering the na

• Although the reasons why viral RNA does not

  2021-01-19

  

  Although the reasons why viral RNA does not bind to and activate PKR in WNV-infected cells are not known, some of the known characteristics of flavivirus infections provide possible clues. The viral I-BET151 protein forms dimers that associate with ER membranes and viral RNA (Lindenbach et al., 200

• br Materials and methods br Results br Discussion Anti EGFR

  2021-01-19

  

  Materials and methods Results Discussion Anti-EGFR therapy for epithelial carcinomas has important clinical significance, but widespread intrinsic or acquired resistance seriously affects efficacy. Mutation and heterodimerization of EGFR are the two main causes of resistance to anti-EGFR th

• br Materials and methods br Results br

  2021-01-18

  

  Materials and methods Results Discussion To our knowledge, this is the first large-scale longitudinal measurement of more than 20 cytokines in normal pregnancy. Simultaneous measurements of several cytokines with multiplex magnetic bead-based immunoassays are becoming increasingly common in

15150 records 653/1010 page Previous Next First page 上5页 651652653654655 下5页 Last page