• br FXR FGF in the

  2021-10-06

  

  FXR–FGF15/19 in the control of BAs synthesis The nuclear receptor FXR is the master regulator of BAs homeostasis, modulating their synthesis, SAG supplier and uptake [15]. FXR decreases BA de novo hepatic biosynthesis by reducing the expression of CYP7A1. At the canalicular membrane, newly-synth

• Growing evidence supporting the anti inflammatory and tissue

  2021-10-04

  

  Growing evidence supporting the anti-inflammatory and tissue-protective effects of FPR antagonists led to the screening of commercial libraries for novel small-molecule FPR antagonists. As result of these screening efforts and/or structure–activity relationship (SAR)-directed design and synthesis, a

• Our paper also contributes to the

  2021-10-03

  

  Our paper also contributes to the large, but hitherto inconclusive literature that studies the effects of option-based compensation or convexity in compensation on corporate risk-taking policies. On the one hand, some studies document a positive relationship by showing that convexity increases lever

• The proposed contributory role of endogenous histamine via

  2021-10-03

  

  The proposed contributory role of endogenous histamine via activation of H1 receptor in the locomotor sensitization induced by caffeine was further ratified by H1 receptor antagonism during the induction phase and subsequently its effect on expression to locomotor sensitization induced by caffeine.

• br Discussion The aim of the

  2021-10-03

  

  Discussion The aim of the present study was to extend the list of ASIC ligands and to check if histamine receptors ligands can also affect ASICs. The novel finding is that not only histamine but also thioperamide, 1-metylhistamine and Nα-methylhistamine are active ASIC1a potentiators, while other

• br Results and discussion br Conclusions In summary we

  2021-10-02

  

  Results and discussion Conclusions In summary, we generated analogues of the hit compounds 1–3, studied their structure–activity relationships, and created a series of highly potent GPR55 agonists. The most potent agonists among the series were 17a-b, 17e, 17g and 17l with EC50 values below 10

• br Conclusions br Introduction G protein coupled receptors G

  2021-10-02

  

  Conclusions Introduction G protein-coupled receptors (GPRs) share common structural motifs, including seven transmembrane helices, and the ability to activate heterotrimeric G proteins such as Gs, Gi, Gq and G12/13. A variety of GPR cellular functions are mediated by second messengers such as

• A number of experimental data declare a tight interdependenc

  2021-10-02

  

  A number of experimental data declare a tight interdependence between the pathological changes of glutamate transport in cyp450 inducers and consequent alterations in glutamate transport and activity/expression of glutamate metabolizing enzymes in platelets (Aliprandi et al., 2005, Behari and Shriv

• The identification of distinct expression domains

  2021-10-02

  

  The identification of distinct expression domains in the limb suggested that these domains might have specific biological functions. We explored this possibility by determining enriched biological processes for each category using GO ontology term analysis (WebGestalt) (Zhang et al., 2005). Category

• In the small intestine digestion and

  2021-10-02

  

  In the small intestine, digestion and ataluren of the nutrients are the next processes with an impact on the resulting plasma profile. Normally, neither carbohydrate digestion nor absorption are limiting factors, which is illustrated by the rapid and extensive absorption of glucose in conditions wit

• br Contributions br Acknowledgements This

  2021-10-02

  

  Contributions Acknowledgements This research was supported by Natural Sciences and Engineering Research Council (NSERC) Discovery grant No. 341538 and Ontario Graduate Scholarships to HM and VS. Introduction Sexual size dimorphism describes size difference between male and female individua

• FXR agonists represent an attractive class of drugs

  2021-10-01

  

  FXR agonists represent an attractive class of drugs for patients with PFIC. Synthetic and semi-synthetic FXR agonists, with higher affinity and potency to activate FXR, have been successfully tested in animal models of cholestasis. In these murine models, the semi-synthetic steroidal FXR ligand obet

• Reducing the molecular weight According

  2021-10-01

  

  Reducing the molecular weight: According to a thorough analysis of a large, structurally diverse Caco-2 permeability dataset using a variety of statistical techniques by AstraZeneca researchers, logD and molecular weight are suggested the most important factors in determining the permeability of dru

• Another TKI used in cancer therapy is the

  2021-10-01

  

  Another TKI used in cancer therapy is the Abl inhibitor imatinib mesilate which has also a beneficial effect on glucose homeostasis in diabetic humans [39], [40], [41]. Imatinib has a clear impact on NFκB activation and anti-apoptotic preconditioning of β-cells [39], attenuating islet inflammation

• The Hippo pathway has been

  2021-10-01

  

  The Hippo pathway has been well established as a tumor suppressor pathway and is involved in many diverse biologic processes including cell growth, cell death, and organ size control in organisms, ranging from Drosophila to mammals [4]. Central to this pathway is a kinase cascade in which the Ste20-

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