• YAP TAZ nuclear function is

  2022-04-19

  

  YAP/TAZ nuclear function is also influenced by interaction with the TEAD family of transcription factors [96, 97, 98, 99, 100, 101]. The RAC1 Iohexol exchange factor protein TIAM1 has recently been linked to YAP/TAZ regulation in the nucleus and cytoplasm. Nuclear TIAM1 inhibits YAP/TAZ binding to

• The rationale for developing HDACi as anticancer agents was

  2022-04-19

  

  The rationale for developing HDACi as anticancer agents was based on their ability to induce the hyperacetylation of histones and nonhistone proteins, resulting in increased differentiation, apoptosis, and ascorbic acid sale arrest of cancer cells 1, 2, 3. HDACi have been used in the treatment of h

• In summary P P macrocyclization proved to

  2022-04-19

  

  In summary, P2-P4 macrocyclization proved to be an effective strategy to drive activity in this series of HCV NS3 protease inhibitors while microsomal stability was enhanced by the introduction of steric bulk along the tether. This modification augmented the previously-described tactic of improving

• A number of synthetic GPR agonists have been reported to

  2022-04-18

  

  A number of synthetic GPR119 agonists have been reported to date, several of which have advanced into clinical trials. Reported GPR119 agonists are often composed of three parts as depicted in : a piperidine or a piperazine ring -substituted with a carbamate or a heteroaryl group at the right side,

• br TGR Agonists br FXR TGR Dual

  2022-04-18

  

  TGR5 Agonists FXR/TGR5 Dual Agonists In 2010, a FXR/TGR5 dual agonist, 51 (INT-767), was reported [57]. Using an AlphaScreen coactivator recruitment assay, the potency of 51 at FXR was 30nM. In NCI-H716 cells, 51 stimulated intracellular cAMP secretion with an EC50 of 0.63μM. Its TGR5 potency

• To test this concept we

  2022-04-18

  

  To test this concept, we took advantage of our large supply of various 2-pyridyl containing [3.1.0] cores (inactive with alkyl or aryl sulfonamides) and prepared the -methylimidazole sulfonamide analogs and (), as work form Merck demonstrated that the 2-pyridyl moiety was superior to the original 4-

• br Materials and methods br Results br

  2022-04-18

  

  Materials and methods Results Discussion Although large-scale purification of homogeneous and functional membrane proteins is challenging, it is essential for biochemical, biophysical and structural characterization. This is particularly true for human P-gp, as its atomic structure has only

• br Materials and methods br Results br Discussion

  2022-04-18

  

  Materials and methods Results Discussion Heart hypertrophy is initially physiological to compensate for the loss of heart functions. However, sustained stresses lead to a pathological status, in which myocardium becomes stiffened by interstitial fibrosis and thereby diastolic dysfunction in

• In experiments using D to displace binding of specific high

  2022-04-18

  

  In experiments using D22 to displace binding of specific high-affinity radioligands for DAT, NET, and SERT in mouse Aprepitant tissue, we observed a ranking with D22 displacement efficiency in the order of DAT > SERT > NET (IC50 values being ~ 11 (DAT), 26 (SERT), and 101 (NET) µM; Fig. 1, Fig. 2,

• Excessive extracellular glutamate can be removed from brain

  2022-04-18

  

  Excessive extracellular glutamate can be removed from Z-DQMD-FMK interstitial fluids to the blood plasma for the maintenance of proper extracellular glutamate homeostasis in the mammalian central nervous system [[5], [6], [7]]. The glutamate concentration in the blood plasma increases in case of isc

• Glucagon was described as an insulin

  2022-04-18

  

  Glucagon was described as an insulin secretagogue as early as 1965 (Samols et al., 1965). Our studies extend these findings by demonstrating that this is a direct effect mediated by distinct receptors in the mouse pancreas. Previous experiments on isolated β FMK clearly show that glucagon is capable

• Another consistent observation in our studies was the lower

  2022-04-18

  

  Another consistent observation in our studies was the lower plasma catecholamine concentrations in the exercised GHSR-null mice, suggesting a diminished sympathoadrenal response. A proper sympathoadrenal response is essential for increasing substrate utilization during exercise [81]. Thus, the reduc

• Ghrelin readily crosses the blood brain barrier Banks et

  2022-04-18

  

  Ghrelin readily crosses the blood Protease Inhibitor Cocktail (EDTA-Free, 200X in DMSO) barrier (Banks et al., 2002, Banks et al., 2008), and recent studies have identified central nervous system sites of action for ghrelin-mediated appetite and hyperphagia (Alvarez-Crespo et al., 2012, King et al.

• In addition to the robust intracellular calcium mobilisation

  2022-04-18

  

  In addition to the robust intracellular calcium mobilisation, DHA and TUG-891 also induced MMP-9 granules release and superoxide production, supporting a key role of calcium in bovine neutrophil defense responses (Burgos et al., 2011). Pisani et al. (Pisani et al., 2009) described a reduction of bas

• br Conclusion We have demonstrated that ETB receptors negati

  2022-04-16

  

  Conclusion We have demonstrated that ETB receptors negatively regulate the expression of AT1 receptors in renal proximal tubule TDZD-8 from WKY rats but not in SHRs. Short-term activation of the ETB receptor increases AT1 receptor phosphorylation in WKY cells but decreases it in SHR cells. We con

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