• The physiological and pharmacological roles of GPR

  2022-05-31

  

  The physiological and pharmacological roles of GPR81 remain largely unclear because of several reasons. The low potency of lactate agonizing GPR81 in the millimolar range, together with its fast metabolic turnover, renders as a challenge in in vivo studies using lactate. Furthermore, there are no po

• Waldeck Weiermair et al demonstrated that in

  2022-05-31

  

  Waldeck-Weiermair et al. (2008) demonstrated that in endothelial cells, the activation of GPR55 by application of 10µM anandamide resulted in a marked increase of ERK1/2 phosphorylation that was evident 2min following drug activation and was sustained for up to 3h. Another example comes from our unp

• Erastin br GPR is a class A

  2022-05-31

  

  GPR119 is a class A GPCR expressed on pancreatic β-cells and certain enteroendocrine Erastin which upon activation with an agonist, increases insulin secretion in response to rising glucose levels. Mechanistically, this insulinotropic effect is bifurcated involving both GPR119-mediated β-cell sig

• In recent years several DPP IV inhibitors

  2022-05-31

  

  In recent years, several DPP-IV inhibitors have already been approved, such as sitagliptin, vildagliptin, saxagliptin, tenegliptin, alogliptin and linagliptin, etc. Among them, linagliptin (1, Fig. 1) is a non-peptide mimetic sr 75 with a unique xanthine scaffold developed through high-throughput s

• The action of niacin in upregulating cAMP is most likely

  2022-05-31

  

  The action of niacin in upregulating cAMP is most likely determined by the milieu of adenylyl cyclase isoforms expressed in macrophages that are responsive to GPR109A activation. Several adenylyl cyclase isoforms, namely AC2, AC4 and AC7, are responsive to the stimulatory action of Gβγ G-protein sub

• The importance of FXR FGF

  2022-05-31

  

  The importance of FXR-FGF15/19 signaling in BA homeostasis is illustrated by various BA malabsorption syndromes. Clinically, BA malabsorption causes diarrhea due to high BA concentrations in the colon that lead to secretion of water and electrolytes and stimulation of propulsive contractions [36]. P

• The results obtained through in vitro in

  2022-05-31

  

  The results obtained through in vitro, in vivo and in silico corroborated with those presented by other works and indicate that CpMutY is involved in oxidative damage repair in this organism. In this regard, MutY conservation in evolutionarily distant bacteria suggests that this protein plays an imp

• Crystal structure of CD LEL have revealed the head

  2022-05-31

  

  Crystal structure of CD81-LEL have revealed the head sub-domain to be implicated in binding to HCV (Kitadokoro et al., 2001). In a study using African green monkey CD81, T163A, F186 L, E188K and D196E mutations disrupted HCV E2 binding (Higginbottom et al., 2000). In our docking studies, T163 and D1

• In this study with the use of C N

  2022-05-31

  

  In this study, with the use of 13C515N2-labeled glutamine, we observed that 13C515N2-labeled glutamine produces a wide range of NAAG isotopologues and its precursors: NAA and glutamate. The NAAG production from glutamine is consistently more elevated in MYC-ON lymphoma and OVCAR4 compared to MYC-OFF

• The transport of glutamate by EAAT

  2022-05-31

  

  The transport of glutamate by EAAT2 from the extracellular fluid into either astrocytes or endothelial cells is an unfavorable and energy-consuming process. This energy is provided by a coupled co-transport of three sodium ions, one proton, and one glutamate molecule in the counter-transport of one

• To confirm the in vitro findings atorvastatin or

  2022-05-31

  

  To confirm the in vitro findings, atorvastatin or pravastatin was given to C57BL6/J mice fed with high fat diet. Doses of atorvastatin were set to be 6 mg/kg and 12 mg/kg, which were within clinical therapeutic doses. The results revealed that treatment of atorvastatin but not pravastatin impaired

• The in vivo biological activity

  2022-05-31

  

  The in vivo biological activity of the four novel analogues was then systematically assessed in three animal models including normal control, high fat fed and ob/ob mice. As expected from earlier in vitro studies, all four glucagon receptor antagonists had minor effects on glucose or insulin concent

• Since the isoflavone emerged as

  2022-05-31

  

  Since the isoflavone emerged as privileged scaffold in Hh inhibition, based on molecular modeling predictions and prior studies [17,22], here we designed a number of isoflavones able to interact preferentially with the Smo receptor or the Gli protein. Molecules were synthesized by means of a novel s

• Obatoclax mesylate Most of the tumors showed relatively high

  2022-05-31

  

  Most of the tumors showed relatively higher GalR1 mRNA levels than the controls (Fig. 1a, Table 3). However one patient with the lower GalR1 mRNA levels (#12) had, in fact, relatively lower levels of transcript for galanin and the other galanin receptors. Patient #10 and 4 who were also expressing l

• In the present studies we found that

  2022-05-30

  

  In the present studies, we found that genistein did not antagonize fMLF-induced Ca2+ mobilization in FPR1-HL60 CC-223 and human neutrophils. Thus, the previously reported inhibitory effect of genistein on fMLF-stimulated degranulation, aggregation, and reactive oxygen species (ROS) production in hu

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