• Pregnane X receptor PXR is a nuclear receptor that plays

  2023-11-07

  

  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

• We found that several anticancer

  2023-11-07

  

  We found that several anticancer drugs inhibit 5-HT3 chk1 current in vitro. Several studies have suggested that 5-HT3 receptor antagonists have anti-mitogenic and apoptotic effects on colorectal and breast cancer cell lines (Ataee et al., 2010, Hejazi et al., 2015). Irinotecan is used frequently to

• br Conclusions and clinical relevance Astrogliosis and an

  2023-11-07

  

  Conclusions and clinical relevance Astrogliosis and an increase in ADK is a pathologcial hallmark of epilepsy. The consequence of increased ADK in the epileptic Biotin-azide is a decrease in the ambient adenosine tone and A1R activity. As a result, systemic administration of A1R agonists or ADK

• G actin has a molecular weight of kD and dimensions

  2023-11-07

  

  G-actin has a molecular weight of 42 kD and dimensions about 55 × 55 × 35 Å3. It consists of 375 amino acids arranged into two individual domains (Alberts et al., 2014). A central cleft bisects the protein into two aforementioned domains which surround a deep cleft containing ATP or ADP and a tightl

• br ACK inhibitors Since ACK activation is correlated with po

  2023-11-07

  

  ACK1 inhibitors Since ACK1 activation is correlated with poor prognosis in various cancers, strong efforts are being directed by multiple groups towards developing highly potent and specific small molecule inhibitors targeting the ACK1 kinase. At least eight small molecule kinase inhibitors have

• br Experimental section br Results and discussion

  2023-11-07

  

  Experimental section Results and discussion Conclusion Acknowledgements This work was financially supported by Recruitment Program of Global Experts, and the Director Foundation of XTIPC, CAS, Grant No. 2015RC011. This work was also financially supported by Natural Science Foundation of

• Concerning asthma in a study evaluating the

  2023-11-07

  

  Concerning asthma, in a study evaluating the effect of tiotropium in severe asthma, the sputum eosinophil count and exhaled nitric oxide were also assessed. However, evaluation of the anti-inflammatory effect of tiotropium was difficult because these markers were low at baseline and thereafter. In a

• The present in vitro pharmacological experiments revealed th

  2023-11-07

  

  The present in vitro pharmacological experiments revealed that the cholinergic up-regulation of VEGF expression in neurons and astrocytes was mainly mediated by nicotinic AChR and muscarinic AChR, respectively. In addition, neuronal VEGF expression was elevated by endogenous ACh in a manner that was

• Regarding the HT B receptors they act as terminal receptors

  2023-11-07

  

  Regarding the 5-HT1B receptors, they act as terminal receptors and are involved in the presynaptic regulation of the release of 5-HT. But at spinal level these receptors are principally situated post-synaptically (Sari, 2004). The ability of autoreceptors to regulate extracellular levels of 5-HT dur

• br Dihydrotestosterone in adult fish and frogs

  2023-11-07

  

  Dihydrotestosterone in adult fish and frogs New perspectives and next directions Similar to other androgens, DHT can modulate reproductive endpoints in both fish and amphibians. However, predicting the effects of DHT can be challenging, as reproductive homeostasis is dependent upon the balanc

• br The embryological and physiological roles of ATX ATX is

  2023-11-07

  

  The embryological and physiological roles of ATX ATX is a vital enzyme that is needed for early embryological development. ATX knockout (KO) (ENPP2−/−) embryos die in utero on average at day 9.5 with vascular and neural tube defects [30], [73], [74], [75]. In these mice, malformations in the alla

• In this report the natural compound deguelin potently

  2023-11-07

  

  In this report, the natural compound deguelin potently and dose-dependently suppressed Aurora B kinase activity in vitro, indicating that this compound is an effective Aurora B inhibitor. The docking study indicated that deguelin was docked into the ATP-binding pocket of Aurora B and formed hydropho

• In addition to pH regulation by ion counter

  2023-11-06

  

  In addition to pH regulation by ion (counter-) fluxes, acidification is regulated by the abundance of V-ATPase on organelles, by the pumping activity of the complex and by proton leakage. In yeast, the V-ATPase VO subunit a is the only subunit expressed in two isoforms termed Stv1p and Vph1p. V-ATPa

• Suspecting that ACL might regulate

  2023-11-06

  

  Suspecting that ACL might regulate the expression or activity of myogenic transcription factors, Das knocked down MyoD and found that such intervention abolished the effect of ACL on fast MyHC expression and that, conversely, MyoD overexpression partially rescued reduced fast MyHC expression caused

• From an historical perspective ligands

  2023-11-06

  

  From an historical perspective, ligands for GPCRs (adrenaline, serotonin, AS-605240 australia or morphine, to name a few) have been identified before their receptor counterparts, at a time when the concept of receptor itself was controversial [15]. Although many cognate receptors for endogenous lig

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