• Main Text FFAR GPR is a long

  2022-08-18

  

  Main Text FFAR1 (GPR40) is a long-chain fatty Pimasertib (LCFA) receptor highly expressed and enriched in enteroendocrine cells, where it senses LCFAs generated from dietary triglycerides, and in pancreatic islet cells, where it acts as a powerful stimulator of insulin secretion. However, the physi

• Following the discovery of diketo

  2022-08-18

  

  Following the discovery of β-diketo compounds S-1360 [31] and L-731988 [32] as anti-HIV integrase inhibitors, a group of researchers discovered a potent perifosine based derivative (1) as the inhibitor of HIV integrase functioning at the 3′-processing and strand transfer steps of HIV integrase. Bioa

• Spatial localization of zGC and zGCAP transcripts

  2022-08-17

  

  Spatial localization of zGC and zGCAP transcripts by in situ hybridization was detected in the ONL. No transcripts were detected in the outermost periphery of the photoreceptor cell layer adjacent to the marginal zone. This region is described as the area of cone genesis and maturation [29], which f

• Targeting MCTs is likely to have

  2022-08-17

  

  Targeting MCTs is likely to have dramatic effects on lactate-dependent metabolic symbiosis described in the previous paragraphs. A plethora of MCT inhibitors have been described, including α-cyano-4-hydroxycinnamate (CHC) [59], organomercurials [60], stilbene disulfonates [60], and other second-gene

• Sorafenib Our aim was to gain insight into mechanisms that

  2022-08-17

  

  Our aim was to gain insight into mechanisms that underlie the contribution of thrombospondin-1 (TSP1) to progression of CKD. TSP1 is the most-studied member of the thrombospondin family of matricellular proteins. Previous studies have demonstrated that pharmacological suppression or genetic depletio

• GPR is present primarily in

  2022-08-17

  

  GPR119 is present primarily in the pancreas and the intestine. Activation of GPR119 increases insulin, GLP-1, GIP and PYY secretion. GPR119 agonists stimulate insulin release in a glucose-dependent manner. The glucose dependent insulin secretion (GIDS) mechanism makes GPR119 an attractive target for

• SGCs tightly ensheath the soma of DRG neurons Costa and

  2022-08-17

  

  SGCs tightly ensheath the soma of DRG neurons (Costa and Moreira, 2015, Hanani, 2005, Takeda et al., 2009). Intimate associations between SGCs and neurons facilitate bidirectional regulation of SGC function and neuronal excitability. After nerve injury, neuronal hyperexcitability can result in SGC a

• Obestatin increased GnRH mRNA expression in the POA being

  2022-08-17

  

  Obestatin increased GnRH mRNA expression in the POA, being the main place of GnRH synthesis (Goodman, 2015). Simultaneously, obestatin also caused a decrease in the GnRH mRNA expression in ME, without affecting the level of this peptide mRNA in AHA. A lack of differences observed in the mRNA level i

• br Materials and methods br

  2022-08-17

  

  Materials and methods Results In this study we re-examined the kinetics of ET transport and tested the ability of various suggested substrates of OCNT1 to inhibit ET uptake. Using a native ET transporter expressed in the human HeLa cell line ET was found to be taken up with a Km of 51 μM and V

• Human Glucocorticoid Receptor hGR was first

  2022-08-17

  

  Human Glucocorticoid Receptor (hGR) was first cloned in 1985 (Hollenburg et al., 1985). It is a modular protein comprised of an N-terminal trans-activating domain (NTD), a C-terminal ligand-binding domain (LBD) and a central DNA- binding domain (DBD). The DBD is highly conserved and has two zinc fin

• br Acknowledgements This work was

  2022-08-17

  

  Acknowledgements This work was supported by a fellowship to C.H. under the ‘100 Foreign Expert’ scheme of the Shanxi province government(R100456). Conflict of interest: Dr. Holscher is a named inventor on a patent submitted by Lancaster University on the use of dual GLP-1/GIP analogues in neurode

• Two excellent GSMs with clear pharmacological effect across

  2022-08-16

  

  Two excellent GSMs with clear pharmacological effect across rats, dogs, monkeys, and human subjects are BMS-932481 and BMS-986133 with IC50 at 6.6 and 3.5 nM to reduce Aβ42, respectively. Both GSMs exhibit dose- and time-dependent activity in vivo by decreasing Aβ1-42 and Aβ1-40 levels while increas

• We next determined the selectivity profile of the most

  2022-08-16

  

  We next determined the selectivity profile of the most potent GPR40 agonists (4k–n) against other free fatty Pyoluteorin receptors (FFA3/GPR41, FFA2/GPR43 and FFA4/GPR120). FFA2 and FFA3 agonists have a preference in binding short-chain fatty acids while FFA1 and FFA4 have a higher affinity to medi

• Although unexpected based on our predictions

  2022-08-16

  

  Although unexpected based on our predictions, low baseline and post-stress cortisol being associated with high anxiety has been previously documented in both clinical and healthy populations of humans (Beaton et al., 2006; Jezova et al., 2004; Shirotsuki et al., 2009; Vingerhoets et al., 1996), and

• Here we show in contrast to previous

  2022-08-16

  

  Here we show, in contrast to previous work, that several phenotypes associated with Orb6 inactivation, including increased cell width, are independent of Gef1. We further find that Orb6 positively regulates exocytosis, also independently of Gef1. To identify novel targets of Orb6, we performed quant

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