• The knowledge on the structure of CYP including

  2024-12-06

  

  The knowledge on the structure of CYP17, including its active site, provides a rationale for understanding many mutations that are found in enzyme dysfunction in clinical disease as well as the enzyme's dual hydroxylase and lyase catalytic capabilities. This knowledge will assist rational drug desig

• br Conflicts of interest br Financial support This work

  2024-12-06

  

  Conflicts of interest Financial support This work was supported by grants from the Fondazione Cariplo [Grant number 2011-0463] (Carini); and by Funds for Original Research of the Università del Piemonte Orientale (2016, Project: Carini-Boldorini). The sponsors had no involvement in study desig

• 22 9 Among steroid saponins ginsenosides are the active

  2024-12-06

  

  Among steroid saponins, ginsenosides are the active components of ginseng, a well-known chinese medicinal plant. More than hundreds of different ginsenosides have been isolated from ginseng and have shown in the past to be membrane active substances and to influence the membrane by modulating lipid

• AP was originally described as a heterodimer of the bZIP

  2024-12-06

  

  AP-1 was originally described as a heterodimer of the bZIP proteins c-Jun and c-Fos. The experiments described here showed that stimulation of TRPV1 channels induced the expression of both of these classical constituents of AP-1. The essential role of both proteins was analyzed in a series of experi

• br Duality of interest br

  2024-12-06

  

  Duality of interest Contribution statement Acknowledgments Introduction Rapid, cell surface-initiated steroid actions have been reported for all major groups of steroid hormones and our understanding of membrane-mediated steroid actions has progressed rapidly over the last two decades. M

• Since the publication of the guidelines data have continued

  2024-12-05

  

  Since the publication of the 2011 guidelines, data have continued to accumulate indicating that the cognitive decline in AD occurs continuously over a long period [6–8], and that progression of biomarker measures is also a continuous process that begins before symptoms [9–14]. Thus, the disease is n

• Kinase inhibitor profiling Through systematic deletion of Ah

  2024-12-05

  

  Through systematic Kinase inhibitor profiling of AhR in specific cell types, Di Meglio et al. (2014) revealed that AhR in keratinocytes and fibroblasts are key to the exacerbated psoriatic phenotype induced by IMQ in AhR-deficient mice. This emphasizes the crosstalk between keratinocytes and the im

• br Concluding remarks Following the disappointing

  2024-12-05

  

  Concluding remarks Following the disappointing outcomes of Aβ immunotherapy trials for AD [62], the current prevailing concept is that disease-modifying therapy must be initiated from the presymptomatic stage of the disease because of the presumed incurability of chronic diseases once they become

• As we previously observed in the NSFT Fukumoto

  2024-12-05

  

  As we previously observed in the NSFT (Fukumoto et al., 2014), the effect of LY341495 in the FST was also inhibited by a 5-HT1A receptor antagonist, indicating the role of the 5-HT1A receptor in the actions of LY341495. Among the 5-HT1A receptors, which exist both presynaptically and postsynapticall

• br STAR Methods br Author Contributions br Acknowledgments T

  2024-12-03

  

  STAR★Methods Author Contributions Acknowledgments This study is funded by National Institutes of Health (NIH) Grants NS028901 and DC004450 (to L.O.T.); N.L. Tartar Trust Fellowship (to H.-W.L.); DC014878 to T.S.B. We thank members of the Trussell lab for helpful discussions, Dr. Stephen Dav

• HhAntag Bioinformatics tools are becoming more powerful and

  2024-12-03

  

  Bioinformatics tools are becoming more powerful and reliable due to the growing number and availability of experimentally determined protein structures (Arnold et al., 2006, Suplatov et al., 2015, Wiltgen and Tilz, 2009). The SWISS-MODEL and MODELLER programs are most frequently used for homology or

• The finding that OCT is expressed

  2024-12-03

  

  The finding that OCT3 is expressed in the nucleus accumbens (Gasser et al., 2009) suggests that inhibition of this transporter may underlie previously described effects of glucocorticoids on extracellular DA concentrations and indicates that DA clearance in this region is not mediated exclusively by

• The most widely recognized effects of adenosine are operated

  2024-12-02

  

  The most widely recognized effects of adenosine are operated through inhibiting A1R, one of the most abundant G protein-coupled receptors in Bromoenol lactone receptor tissue [53]. A1R are located presynaptically, postsynaptically and nonsynaptically [54]. Effect of adenosine in neuronal circuits o

• The inhibition of the exacerbated inflammatory response

  2024-12-02

  

  The inhibition of the exacerbated inflammatory response that follows injury may be an alternative approach to induce a more efficient repair [17,83]. In line with that, 5-LO is one of the most consolidated targets for dampening inflammation, mainly through the therapeutic effects of 5-LO inhibitors

• TC 14012 br Regulation and pharmacology of mPGES mPGES kDa

  2024-12-02

  

  Regulation and pharmacology of mPGES-1 mPGES-1 (16 kDa, 152 amino acids) is a trimeric integral membrane protein of the endoplasmic reticulum with each monomer containing four transmembrane domains (Samuelsson et al., 2007; Sjogren et al., 2013). The three active site cavities are located at the

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