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GSK is a critical component of the Wnt signaling
2022-08-26
GSK-3 is a critical component of the Wnt signaling pathway. The Wnt/beta-catenin signal transduction pathway is important in normal growth and development and is also frequently dysregulated in cancer and other diseases. The Wnt/beta-catenin pathway is finely tuned by both positive and negative inte
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br GPR a G protein coupled receptor GPCR was
2022-08-26
GPR35, a G protein-coupled receptor (GPCR), was discovered and classified as an orphan GPCR in 1998 and deorphanized in 2006 by the discovery of kynurenic phalloidin mg as the endogenous agonist. Since its discovery, limited references on the GPR35 receptor have appeared, due in part to a scarcit
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In summary we discovered azaindole substituted hydroxypyrido
2022-08-26
In summary, we discovered 7-azaindole substituted -hydroxypyridone as a potent zinc-binding GLO1 inhibitor (IC=11nM) through lead generation from HTS and structure-based inhibitor design. The X-ray cocrystal structure and the comparison of binding energies with the indole counterpart revealed that b
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Finally the results in this article indicate that atomistic
2022-08-26
Finally, the results in this article indicate that atomistic MD in conjunction with computational electrophysiology and ion-permeation simulations provide a useful tool for the functional annotation of ion-channel structures. In particular, they exemplify how MD simulations in native lipid membranes
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It is notable that pharmacological or genetic
2022-08-25
It is notable that pharmacological or genetic inhibition of GCGR signaling results in the engagement of a number of compensatory mechanisms that potentially impact glucose control. These include alpha-cell hyperplasia [2], [11], [12], [13] and increased beta-cell proliferation under low insulin cond
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Given the estimated number of NSVDC channels in a red
2022-08-25
Given the estimated number of 150–300 NSVDC channels in a red cell [7] and a single channel conductance of 30 pS at physiological salt concentrations [6], the maximum conductance observed in intact red cck 1303 australia indicate either a very low open state probability, in the order of 10−3 or a f
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Conclusion By generating high quality hypocotyl transcriptom
2022-08-25
Conclusion By generating high-quality hypocotyl transcriptomes of a jute hypocotyl-defect mutant and its wild-type comprising the largest number of annotated unigenes (39,076), we identified a complete array of structurally and functionally diverse β-galactosidases. Our proposed domain-centric clas
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A mutation in stearoyl coenzyme A desaturase
2022-08-25
A mutation in stearoyl coenzyme A desaturase 1 gene was reported to reduce sebum production and monounsaturated fatty acids (MUFA) synthesis in mice, which was accompanied with impaired clearance of gram-positive bacteria-induced skin infection (Georgel et al., 2005). Interestingly, gram-positive ba
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In summary the SAR of a
2022-08-25
In summary, the SAR of a series of phenylpropanoic acid-free fatty iox receptor agonists is described which resulted in the identification of potent FFA4 agonists. The superior pharmacokinetic properties of compound led to its selection as an in vivo tool compound which afforded robust efficacy in
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In a follow up study
2022-08-25
In a follow up study, the same research group further characterized FFA4 involvement in DU145 and PC-3 cancer cell lines by demonstrating that the anti-proliferative and anti-migration activities of FFA4 require the presence of LPA1 receptor (LPA1R), suggesting a mechanism consistent with negative c
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N-acetyl D-galactosamine br Methods and materials br Conflic
2022-08-25
Methods and materials Conflict of interest statement Introduction Ferroptosis (ferro = “ferrous ion (Fe2+)”, ptosis = “fall”), implicating the crucial role of cellular iron played in cell death, is a new form of nonapoptotic programmed cell death characterized by iron-dependent accumulation
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If the manager channel dominates we
2022-08-25
If the manager channel dominates, we expect the increase in debt maturity of treated firms relative to control firms to be more evident in firms with weaker corporate governance where managers are less monitored and have more discretion in changing firm risks. We use the governance index (GINDEX) co
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There has been conflicting evidence on the possible receptor
2022-08-24
There has been conflicting evidence on the possible receptor mechanisms that mediate the neuro-immuno-modulatory effects of FAAH substrates. Evidence from in vitro studies indicates that AEA-mediated modulation of TLR4-induced neuroinflammation may be mediated by CB1/CB2 receptor dependent (Correa e
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N6-Methyl-ATP br Conclusions In summary our results demonstr
2022-08-24
Conclusions In summary, our results demonstrate that in short term effect, TBT induced concentration-dependent vasorelaxation of HUA rings. Regarding the long term effects, exposure to a concentration of 100 μM TBT the human umbilical N6-Methyl-ATP have a dual effect, and a decrease of the 5-HT2
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br Trifluoromethylketones This group of
2022-08-24
Trifluoromethylketones This group of compounds was demonstrated to bind the zinc Sodium 4-Aminosalicylate in the active site due to its easy hydration, forming the required chelating intermediate. Ontaria et al. [92] have proposed variations around the cap group of trifluoromethylthiophene as th
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