• The nuclear receptor NR superfamily of

  2019-11-28

  

  The nuclear receptor (NR) superfamily of ligand regulated transcription factors has proven to be a rich source of targets for the development of therapeutics for a wide range of human diseases. The NR3B subfamily known as the estrogen-related receptor (ERRα[NR3B1], ERRβ[NR3B2] and ERRγ[NR3B3]) regu

• The reduction of the calcium response

  2019-11-28

  

  The reduction of the calcium response to AVP could be also due to a PKA-mediated effect of desensitization of IP3R, as described in rat megakaryocytes [41]. Furthermore, PKA activation inhibits intracellular Ca release in mouse pancreatic acinar cells [42] or in rat cerebellum [43]. The phosphorylat

• Grapiprant is a selective antagonist

  2019-11-28

  

  Grapiprant () is a selective antagonist for prostaglandin E (PGE) receptor subtype 4 (EP4) identified as a clinical candidate for the treatment of inflammatory pain associated with osteoarthritis (OA). It is currently under development for use in humans and dogs. The projected dosing regimen of grap

• br Clinical potential of ET receptor

  2019-11-28

  

  Clinical potential of ET receptor biased ligands Is there a clinical need for ET receptor biased ligands? Evidence is strongest from research in epithelial ovarian cancer demonstrating that ET-1 stimulated ETA-mediated β-arrestin signalling leads to activation of the oncogenic mediator NF-κB [21]

• OHC is a potent regulator of LXR

  2019-11-28

  

  25-OHC is a potent regulator of LXR-mediated pathways, that impact on TAI-1 mg lipid homeostasis [8]. This oxysterol affects expression of the cholesterol efflux pumps ATP-binding cassette transporter (ABC)A1 [9] and ABCG1, and expression of apolipoprotein E [10], [11], [12]. 25-OHC is able to stim

• Previous in vitro studies have demonstrated

  2019-11-28

  

  Previous in vitro studies have demonstrated that DNA-PK-deficient cell line (MO59J) is approximately 30-fold more sensitive to radiation than DNA-PK-proficient cell line (MO59K) [31]. Moreover, specific DNA-PK inhibitors SU11752 and wortmannin have been shown to sensitize GBM momelotinib (MO59K) to

• In the present study we examined

  2019-11-27

  

  In the present study we examined whether the gene for estrogen receptor alpha, Esr1, plays a role in the expression of maternal memory in female rats. The approach utilized a newly developed rat Esr1 knockout (KO) rat model (Rumi et al., 2014) to evaluate whether deletion of the Esr1 melanin affecte

• Elevated DPP activity has been

  2019-11-27

  

  Elevated DPP-4 activity has been strongly associated with diabetes mellitus, IR (Röhrborn et al., 2015), metabolic syndrome (Lamers et al., 2011) and inflammation (Zhong et al., 2015). However, report has it that GC exposure increases DPP-4activity in thymocyte homogenates (Kraml et al., 2003) but t

• Initially the cause of hypoglycemia

  2019-11-27

  

  Initially, the cause of hypoglycemia was not apparent. There was no detectable lesion in the pancreas on plain computed tomography, and anti-insulin antibody was negative. Eight hours after hospital admission, his son discovered that the patient had accidentally taken glimepiride 3mg/day for 3 days.

• br Conclusion br Competing interests br Authors

  2019-11-27

  

  Conclusion Competing interests Authors\' contributions Acknowledgements The work was supported by Aurigene Discovery Technologies (M) Sdn. Bhd., Industrial Doctoral Program sponsorship by Ministry of Higher Education, Malaysia and research grants by the University of Malaya, grant number

• br Results and discussion br Conclusion Novel and selective

  2019-11-27

  

  Results and discussion Conclusion Novel and selective aziridine-based inhibitors for the Leishmania mexicana protease LmCBP2.8 were discovered. Compounds 7d (Ki = 0.8 μM), 9d (Ki = 1.36 μM), 12d (Ki = 0.77 μM), 14d (Ki = 0.9 μM) and 18 (Ki = 0.441 μM) showed the highest potency and selectivity

• PCI-32765 Moreover a ligand for fusin has recently been foun

  2019-11-27

  

  Moreover, a ligand for fusin has recently been found: the lymphocyte chemoattractant stromal-derived factor-1 (SDF-1) binds to CHO PCI-32765 transfected with fusin and promotes secondary messenger production (Bleul et al., 1996; Oberlin et al., 1996). A new name, CXCR-4, has been proposed for the r

• Under conditions of energy scarcity

  2019-11-27

  

  Under conditions of energy scarcity or nutritional restriction, AMPK, a critical energy sensor, is activated in response to the increased ratio of AMP to ATP. Various kinases may phosphorylate AMPK, leading to its activation. For example, AMPK phosphorylation by liver kinase B 1 (LKB1) at Thr172 re

• MdHCLB channels expressed in Xenopus oocytes

  2019-11-27

  

  MdHCLB channels expressed in Xenopus oocytes produced currents in response to HA and GABA (Fig. 1, Fig. 3). This is in agreement with the findings with Drosophila HCLB channels (Gisselmann et al., 2004). In the HA concentration-response curves, the effects of GABA were additive to those of HA only i

• br Discussion The use of

  2019-11-27

  

  Discussion The use of carp primary cell cultures proved to be a valuable approach to evaluate the piscine immune response. A. hydrophila was a more potent stimulator of NO formation by carp leukocytes compared to commercial LPS often used for leukocyte stimulation (Mustafa and Olson, 1998, Chao e

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