• Pregnane X receptor PXR is a nuclear receptor that plays

  2023-01-02

  

  Pregnane X receptor (PXR) is a nuclear receptor that plays an important role in regulation of metabolism and disposition of structurally diverse xenobiotics as well as endogenous steroids and bile acids (Bertilsson et al., 1998, Kliewer et al., 1998, Lehmann et al., 1998). PXR regulates the metaboli

• Aberrant or a sustained activation of

  2023-01-02

  

  Aberrant or a sustained activation of AhR signaling pathway, triggered by exogenous toxic ligands such as dioxins, PAHs or polychlorinated biphenyls (PCBs), is a well-described biological process engaged during tumor initiation and/or promotion in various tissues (e.g. liver, lung, skin)(reviewed in

• Blockers will reduce perioperative myocardial ischemia and s

  2023-01-02

  

  β-Blockers will reduce perioperative myocardial ischemia and studies published in the 1990s suggested that their routine administration before surgery provided protection against perioperative CV complications.31., 32., 33. Based on these early studies, several national organizations endorsed the pe

• GMF was later localized to the cytosol of primary

  2023-01-02

  

  GMFβ was later localized to the cytosol of primary astrocytes and glioma cell lines [67], prompting investigations into its involvement in intracellular signaling. It was found that PKA phosphorylation of GMFβ inhibits the ERK1/2 branch of the MAP kinase pathway [73], yet activates the stress-respo

• In conclusion we have demonstrated that diaryl pyrazolo

  2023-01-02

  

  In conclusion, we have demonstrated that ,-diaryl-1-pyrazolo[3,4-]pyrimidine-3,6-diamines represent a novel class of ACK1 inhibitors. The presence of a polar substituent at C-4 of the N-6 aryl ring was shown to be unnecessary for maintaining high levels of inhibitory activity. Furthermore, selectivi

• br Results br Discussion The present study

  2023-01-02

  

  Results Discussion The present study uncovers a role of calpain, a family of calcium-dependent protease, in regulating postsynaptic differentiation at the NMJ. Cholinergic activation stimulates calpain, whose inhibition stabilizes AChR clusters in cultured muscle Go 6983 and in agrin mutant m

• LPA binds to six specific

  2023-01-02

  

  LPA binds to six specific cell surface GPCR receptors. The receptors LPA1 (lysophosphatidic receptor 1, formerly, Edg2), LPA2 (Edg4) and LPA3 (Edg7) belong to the endothelial differentiation gene family (EDG) and share sequence homology (50–60% amino KN-62 homology) An et al., 1997, An et al., 1998,

• br Acknowledgements We would like to thank Dr

  2022-12-29

  

  Acknowledgements We would like to thank Dr. Thomas Blanpied, Sai Sachin Divakaruni, Dr. Helmut Kessels, Feline Lindhout, Dieudonnée van de Willige, and all members of the MacGillavry lab for discussions and critical reading of the manuscript. This work was supported by NWO (ALW-VENI 863.13.020, A

• Current treatment options for corneal neovascularization inc

  2022-12-23

  

  Current treatment options for corneal neovascularization include topical application of steroids220, 25, 35, 43 or surgical interventions: laser ablation,14, 203, 234, 48 photodynamic therapy (PDT),4, 93 and fine-needle diathermy.221, 238, 240, 261 Targeting proangiogenic molecules with topical or s

• Perhaps the first evidence of

  2022-12-23

  

  Perhaps the first evidence of AMPKs therapeutic ability in DM1 came from Thomas Cooper’s laboratory where they demonstrated that insulin-independent glucose uptake was unaffected in human DM1 muscle bapta treated with MET, an AMPK activator and first-line therapy for type 2 diabetes mellitus [76].

• br Discussion Elevated blood BCAA levels are a common featur

  2022-12-23

  

  Discussion Elevated blood BCAA levels are a common feature of a developed pathophysiological state characterized by obesity and IR [4]. It has been suggested that this profile is part of a panel of biomarkers able to predict the onset of more severe complications like diabetes in humans [14]. In

• The excellent potencies selectivities and improved PK associ

  2022-12-21

  

  The excellent potencies, selectivities and improved PK associated with the piperazine class triggered more extensive off-target screenings of the highlighted compounds. A screen of more than 100 enzymes, receptors, and ion channels resulted in activity at the norepinephrine transporter (NET). This

• br Synthetic lethal approaches In

  2022-12-17

  

  Synthetic lethal approaches In addition to the potential utility of ATM and ATR as chemo- or radiosensitisers, recent studies suggest that such compounds may have single agent activity in certain subsets of patients through induction of synthetic lethality. Two genes are considered synthetically

• br Acknowledgements We would like to thank

  2022-12-17

  

  Acknowledgements We would like to thank Dr. Thomas Blanpied, Sai Sachin Divakaruni, Dr. Helmut Kessels, Feline Lindhout, Dieudonnée van de Willige, and all members of the MacGillavry lab for discussions and critical reading of the manuscript. This work was supported by NWO (ALW-VENI 863.13.020, A

• Molecular docking quantitative structure activity relationsh

  2022-12-17

  

  Molecular docking, quantitative structure–activity relationship (QSAR) and high-throughput virtual screening (HTVS) studies have a very widespread use in computer-assisted drug design.25, 26, 27, 28 Suvannang et al. used the published X-ray crystallographic data to examine known aromatase inhibitors

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