• In summary we have designed and explored

  2021-12-24

  

  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

• It is extremely difficult to predict a

  2021-12-24

  

  It is extremely difficult to predict a plausible conformer of hsGCαβ heterodimer with right orientation of multiple domains. Even though the template identities in case of dimeric domains were not high enough but still we modelled the entire heterodimeric structure of hsGCαβ with a reasonable and ju

• monoamine oxidase inhibitor Glutathione transferases EC also

  2021-12-24

  

  Glutathione transferases (EC 2.5.1.18; also referred to as glutathione S-transferases, GSTs) are ubiquitous and promiscuous enzymes that catalyze various kinds of reactions involving a wide variety of substrates that are toxic and chemically reactive (Angelucci et al., 2005). The primary function of

• Compound was synthesized in a racemic fashion

  2021-12-24

  

  Compound was synthesized in a racemic fashion with this study and plans for an enantioselective synthesis could be developed based on the activity of racemic . Synthesis of compound followed a slightly different synthetic route due to the ineffectuality of the S2 reaction on the secondary position (

• SAR around amino derivative revealed

  2021-12-24

  

  SAR around amino-derivative revealed a number of interesting trends related to the serum shift and in vitro activity (). A comparison of derivative , and its epimer , showed that the stereochemistry had little effect on the serum shift and the intrinsic affinity for the receptor. In contrast, re-po

• Uracil DNA glycosylase UDG is a highly conserved damage repa

  2021-12-24

  

  Uracil-DNA glycosylase (UDG) is a highly conserved damage repair enzyme which can specifically recognize and excise uracil residue within the DNA sequences and actuate the DNA 1-Oleoyl lysophosphatidic acid sodium salt excision repair (BER) pathway which keeps the maintenance of genomic integrity a

• The GlyR is pentameric with each subunit consisting

  2021-12-24

  

  The GlyR is pentameric, with each subunit consisting of an extracellular ligand binding domain (LBD), four transmembrane (TM) segments, and a large intracellular loop between TM3 and TM4. Binding of neurotransmitter produces conformational changes that are rapidly transmitted to the membrane-spanni

• To confirm the in vitro findings atorvastatin or

  2021-12-24

  

  To confirm the in vitro findings, atorvastatin or pravastatin was given to C57BL6/J mice fed with high fat diet. Doses of atorvastatin were set to be 6 mg/kg and 12 mg/kg, which were within clinical therapeutic doses. The results revealed that treatment of atorvastatin but not pravastatin impaired g

• Type diabetes mellitus is characterised by two major feature

  2021-12-24

  

  Type 2 diabetes mellitus is characterised by two major features: peripheral insulin resistance and impaired insulin secretion from pancreatic beta Desfuroylceftiofur synthesis [1]. The condition occurs when the pancreatic beta cells are unable to compensate for increased insulin demand due to insul

• Xenobiotic metabolizing enzymes are classified as being

  2021-12-24

  

  Xenobiotic metabolizing enzymes are classified as being phase I, phase II and transporter enzymes, with phase I enzymes metabolizing lipophyllic xenobiotics to make them more polar so that the phase II enzymes can perform the necessary conjugation reactions that afford elimination. Although the phas

• br Do the actions of GLP R agonists on the

  2021-12-24

  

  Do the actions of GLP-1R agonists on the vascular endothelium account for GLP-1R agonist-mediated cardioprotection? The previous section highlighted the recent clinical evidence from cardiovascular outcomes studies supporting the notion that GLP-1R agonists confer cardioprotective actions in pati

• Medulloblastoma predominantly occurs in infants

  2021-12-24

  

  Medulloblastoma predominantly occurs in infants and children, and is the most-common type of paediatric malignant HOAt tumour, accounting for about 20% of all childhood brain tumors [63]. According to cancer genomics, medulloblastoma consists of at least 4 distinct subgroups: Hh driven, Wnt driven,

• br Introduction G protein coupled receptors GPCRs

  2021-12-24

  

  Introduction G-protein coupled receptors (GPCRs) represent one of the largest family of receptors involved in cell membrane signal transduction and have become one of the leading therapeutic targets worldwide (Chakraborty and Chattopadhyay, 2015; Bouvier, 2001; Sriram and Insel, 2018). GPCRs sign

• The first GSM was identified from the discovery

  2021-12-24

  

  The first GSM was identified from the discovery of non-steroidal anti-inflammatory drugs (NSAIDs). An amyloid reducing GSM that also suppresses inflammation is desirable. Inflammatory response is an invariable characteristic of AD pathogenesis, in part triggered by Aβ. During AD onset and progressio

• Dehydroepiandrosterone The chemical structure of BAs consist

  2021-12-23

  

  The chemical structure of BAs consists of a steroid nucleus with an acidic side chain. They are amphipatic molecules characterized by a hydrophilic α-face and a hydrophobic β-face. The hydrophobic pocket of the FXR LBD interacts with BAs largely through the β-face. The α-face contains several hydrox

15876 records 512/1059 page Previous Next First page 上5页 511512513514515 下5页 Last page