• br Author contributions statement P N Y

  2022-01-03

  

  Author contributions statement P.N.Y. designed the study, analyzed the data and prepared the draft of the manuscript. C.S performed the experiments, analyzed the data and generated Fig. 1, Fig. 2, Fig. 3, Fig. 4, Fig. 5, Fig. 6, Fig. 7, Fig. 8. A.K. and S.D. made Supplementary Figs. S1 and S2. D.

• The RAS RAF MEK ERK pathway also

  2022-01-03

  

  The RAS/RAF/MEK/ERK pathway (also known as the MAPK/ERK pathway) is one of the most important signaling pathways in PDAC. Activation of the MAPK/ERK pathway promotes PDAC growth and apoptosis resistance in response to gemcitabine [43,44]. We previously demonstrated that inhibition of GPX4 can overco

• In summary we have discovered the

  2022-01-03

  

  In summary, we have discovered the first examples of movement of Asp189 upon binding to fXa inhibitors. A series of novel and potent fXa inhibitors with a phenyltriazolinone P moiety were identified. Although the general binding mode compared to our previously-reported fXa inhibitors was maintained,

• The FAAH inhibitor activity of the

  2022-01-03

  

  The FAAH inhibitor activity of the 3-(5-(ethoxycarbonyl)-1-phenyl-1H-pyrazol-3-yl)phenyl cyclohexylcarbamates was investigated by preparation of compounds (43–52, Table 3). These new compounds displayed an important loss of activity in comparison with the corresponding regioisomers 5-phenyl compound

• In various models histamine has been shown

  2022-01-03

  

  In various models, histamine has been shown to induce chemotaxis. This was first appreciated over 40 years’ ago in studies with eosinophils (Clark et al., 1977). At that time, only histamine H1 and histamine H2 receptors were recognized and studies with ligands to these receptors indicated that neit

• BLU9931 synthesis This study was supported by

  2022-01-03

  

  This study was supported by the Finance Department Foundation of Jilin Province (3D5178963428). Introduction Breast cancer is one of the leading cause of death in women worldwide [1,2]. Due to recent advances of combined therapies, survival rate of breast has improved significantly. However, bre

• br Acknowledgement The work was

  2022-01-03

  

  6. Acknowledgement The work was supported by the NSFC through Grant Nos. 11535016 and 11475232. It was also supported by CAS. The authors thank their collaborators for beneficial discussions and enthusiastic supports in the simulations and calculations. Introduction Hypoxia-inducible factors

• br Discussion The aminoglycoside antibiotic gentamicin

  2021-12-31

  

  Discussion The aminoglycoside antibiotic gentamicin continues to be an important agent against life threatening infections. However, nephrotoxicity is a major complication of the gentamicin administration. Thus amelioration of nephrotoxicity would enhance its clinical use. Several approaches invo

• br Introduction The Ras superfamily

  2021-12-31

  

  Introduction The Ras superfamily of small GTPases is composed of more than 150 protein members involved in a wide variety of biological processes, such as proliferation, differentiation, cytoskeletal organization, and protein trafficking [1]. The Ras superfamily proteins act as molecular switches

• Targeting MCTs is likely to

  2021-12-31

  

  Targeting MCTs is likely to have dramatic effects on lactate-dependent metabolic symbiosis described in the previous paragraphs. A plethora of MCT inhibitors have been described, including α-cyano-4-hydroxycinnamate (CHC) [59], organomercurials [60], stilbene disulfonates [60], and other second-gene

• br The glyoxalase system has not

  2021-12-31

  

  The glyoxalase system has not yet been studied in E. histolytica or G. lamblia. Searches in the G. lamblia genome (GiardiaDB.org) revealed two genes encoding hydroxyacylglutathione hydrolases (Morrison et al., 2007), but no glyoxalase I gene was found. The genome of E. histolytica does not have a

• In summary activated A AR exacerbated the reverse transport

  2021-12-31

  

  In summary, activated A2AR exacerbated the reverse transport function of endothelial EAATs through a direct or indirect pathway depending on PKA and glutamate levels in response to OGD in vitro, but A2AR inhibition quickly restored the normal transport function. Moreover, the key mechanisms by which

• In addition this study also showed

  2021-12-31

  

  In addition, this study also showed no obvious increase in apoptosis but obvious increase in necrosis after WZB117 treatment. The possible reason is that apoptosis is an ATP-utilizing process which is an active and programmed form of cell death. In contrast, necrosis is an uncontrolled or pathologic

• Further research should indeed focus

  2021-12-30

  

  Further research should indeed focus on understanding the nutritional value of food and its effect on metabolism, overall activation of metabolic NRs network. Moreover, given the prominent role of microbiota in the modulation of the FXR signalling (Degirolamo et al., 2014), there is enough impetus t

• This review is an overview on the ongoing trials involving

  2021-12-30

  

  This review is an overview on the ongoing trials involving anti-FGF-FGFR therapies (Wu et al., 2013). Pathway FGFR in cancer A recent study comparing more than 4800 tumor tissue samples has shown that 7.1% of all tumor types have genetic alterations in the FGF-FGFR axis. The aberrations perce

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