• Emerging evidence has shown that pharmacological FXR

  2022-03-14

  

  Emerging evidence has shown that pharmacological FXR agonism attenuates chronic alcohol treatment-induced liver injury and steatosis [18], [19], while whole-body FXR knockout worsens alcohol-induced liver injury [19]. This suggests that FXR plays an important role in ALD development. However, defici

• dca to sdf Pharmacological inhibition of PKR seems to be an

  2022-03-14

  

  Pharmacological inhibition of PKR seems to be an interesting strategy for revealing the role of PKR in oxytosis and ferroptosis. The oxindole/imidazole derivative C16 was identified by screening a library of 26 different ATP-binding site-directed inhibitors of varying structure that is more selectiv

• Mitochondrial is the main source for ROS and

  2022-03-14

  

  Mitochondrial is the main source for ROS and ATP generation, and the loss of mitochondrial membrane potential is involved in the alteration of mitochondrial metabolism and mitochondrial failure-induced cell death [33,34]. In this study, we showed that upregulated ZNF32 sustained mitochondrial membra

• This SAR work led to

  2022-03-14

  

  This SAR work led to the identification of compound 10r ((±)-2-[3-fluoro-4-[3-(hexylcarbamoyloxy)phenyl]phenyl]propanoic acid, ARN2508) [51] as a potent in vivo active inhibitor of intracellular FAAH and COX activities, which exerts profound anti-inflammatory effects in mouse models of IBD without c

• Cyclic Pifithrin-α hydrobromide Previous study demonstrated

  2022-03-14

  

  Previous study demonstrated that Hcy elevated organ culture-induced up-regulation of ETB receptor in VSMCs (Chen et al., 2016a; Chen et al., 2016b). Many signaling pathways were involved in Hcy-induced up-regulation of ETB receptor in VSMCs, such as ERK1/2/NF-κB signaling pathway, Sirt1/NF-κB signal

• A pyrimidine class of compounds is of

  2022-03-14

  

  A pyrimidine class of compounds is of enormous interest within anti-HIV drug discovery process for several decades, as pyrimidine based DABOs class [7], DAPYs class [8] are well known as NNRTIs as well as NRTIs. However, the overall role of a pyrimidine class of heterocycles in anti-HIV drug discove

• Introduction Protein tyrosine phosphorylation plays key

  2022-03-14

  

  Introduction Protein-tyrosine phosphorylation plays key roles in a variety of intracellular signaling pathways involved in cell proliferation, differentiation, gene expression, cell adhesion, and metabolic changes [1]. While receptor-type tyrosine kinases localize to the plasma membrane, most of no

• The more important effect of pitolisant

  2022-03-14

  

  The more important effect of pitolisant is related to its wake-promoting and arousal activities as a result of enhanced ap1 release in animal models (Ligneau, Perrin, et al., 2007). Moreover, its potential in the treatment of severe excessive daytime sleepiness (EDS) in narcoleptic teenagers refrac

• We have previously reported on

  2022-03-14

  

  We have previously reported on the effects of replacing the isoquinoline P2∗ moiety with a naphthalene ring and modifying the connectivity for this element to the P2 proline ring, as demonstrated by compounds – (). Therein, it was hypothesized that the reduced potency observed with – when compared

• Long non coding RNAs lncRNAs are mRNA like transcripts

  2022-03-12

  

  Long non-coding RNAs (lncRNAs) are mRNA-like transcripts of greater than 200 nucleotides (nt), with little or no protein-coding potential [13,14]. LncRNAs have been suggested to participate in transcription and post-transcription regulation as scaffolds, guides, decoys or repressors, activators, and

• In conclusion atorvastatin but not pravastatin

  2022-03-12

  

  In conclusion, atorvastatin but not pravastatin impaired glucose utilization in C2C12 cells and glucose tolerance in HFD mice, which may be partly due to the inhibition of GLUT4 translocation in muscle cells. The decrease in the cholesterol level induced by atorvastatin may partly account for the in

• br Glucocorticosteroid receptor structure and function

  2022-03-12

  

  Glucocorticosteroid receptor structure and function The gene encoding for the human GR is composed of 9 exons (Oakley and Cidlowski, 2011) and the translated protein is described as having 4 functional regions. The protein contains a highly conserved central DNA-binding domain (DBD) or C-domain,

• Clinical trials of all GSIs

  2022-03-12

  

  Clinical trials of all GSIs have ended prematurely, raising the question on our understanding of their target, the γ-secretase/presenilin. Development of compounds to target γ-secretase and reduce Aβ production is complicated by the fact that γ-secretase/presenilin has critical biological function,

• An advantage of photolabeling with tritiated photoprobes fol

  2022-03-12

  

  An advantage of photolabeling with tritiated photoprobes followed by microsequencing with Edman degradation is the ability to both identify the photolabeled caspase pathway and to quantify photoincorporation which enables assessment of pharmacological specificity and allosteric interactions with oth

• c75 Studies have indicated that formylated peptides FPRs and

  2022-03-12

  

  Studies have indicated that formylated peptides, FPRs, and in particular FPR-1 may be principal conductors in inflammatory processes in sterile-24, 26 and infection-related diseases. FPR-1 and formylated peptides, which are active components of CS, have been involved in smoking-induced lung damage,

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