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Recently a lot of synthetic FFA agonists
2022-09-21
Recently, a lot of synthetic FFA1 agonists containing acidic moieties have been reported (Fig. 1) [13], [14], [15], [16], [17], [18], [19], [20], [21]. Notably, most of FFA1 agonists usually have the common biphenyl scaffold, which resulted in a relative deprivation in structure types of agonists [2
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Because AM had limited efficacy on rodent
2022-09-21
Because (AM-3189) had limited efficacy on rodent GPR40, we used two rodent models expressing human GPR40 to demonstrate efficacy of (AM-3189). First, we used human islet transplanted nude mice. In this model, endogenous pancreatic β-cells were ablated using streptozotocin, and mice were rescued to
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Magtanong et al observed that
2022-09-21
Magtanong et al. (2019) observed that caspase-dependent apoptotic lipotoxicity of saturated fatty acids is suppressed by exogenous MUFAs. This may explain the ability of MUFAs to prevent atherosclerosis, in contrast to the pathogenicity of saturated fatty acids. Moreover, MUFAs may promote while PUF
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Thus far it is reported that the histone methyltransferase a
2022-09-20
Thus far, it is reported that the histone methyltransferase activity of SUV39H1 is regulated through some posttranslational modifications. For example, deacetylation of SUV39H1 at Lys-266 by SIRT1 deacetylase increases SUV39H1 activity [31], and methylation of SUV39H1 at Lys-105 and Lys-123 by SET7
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The analytical approach for the
2022-09-20
The analytical approach for the simultaneous determination of HA and its metabolites is complex. There are commercial kits that allow the determination of HA through ELISA and of its metabolites through radioimmunoassay (RIA) techniques. However, these immunological-based techniques do not allow sim
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Our data indicate that curcumin reduced MDA and LOOH formati
2022-09-20
Our data indicate that curcumin reduced MDA and LOOH formation in plasma and kidney induced by gentamicin treatment. The results demonstrate the protective effect of this compound against oxidative damage to these membranes. Moreover, the ability of curcumin to reduce the formation of LOOH induced b
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In the Toc Regulator Mode Fig recognition
2022-09-20
In the “Toc34 Regulator Mode” (Fig. 6), recognition of the transit peptide by Toc159 monomer (step 4) leads to heterodimer-formation [18]. Subsequently, preprotein interaction with the Toc34G homodimer (step 1) regulates the Toc34G homodimer (step 2, 3). However, this mode requires a parallel induct
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br Conclusion The following is the supplementary data relate
2022-09-20
Conclusion The following is the supplementary data related to this article. Conflict of interest Funding Acknowledgements Peroxiredoxin VI (Prdx6) is a dual-functioning antioxidant enzyme that acts to protect biological membranes against damage caused by lipid peroxidation , . The enz
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GSTs have been originally named ligandins because of their c
2022-09-20
GSTs have been originally named ‘ligandins’ because of their capacity to bind large ligand molecules (of molecular weight >400 Da) (Oakley et al., 1999). At least three separate Mirin have been reported for xenobiotics within the H-site; only one is for CDNB (Ralat and Colman, 2004). Usually, the n
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G protein coupled receptors GPCRs
2022-09-20
G-protein coupled receptors (GPCRs) constitute a large family of 7 trans-membrane-spanning proteins that activate internal signal transduction cascades through binding to different ligands including neurotransmitters, peptides, and lipids [7]. This family of receptors has therapeutic potentials in t
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Z-YVAD-FMK As a part of our continuing efforts
2022-09-19
As a part of our continuing efforts towards discovery of new class of compounds against different therapeutic areas and based on the literature reports, we designed a dual pharmacophore which possess a long aliphatic chain of free fatty acids and a phenyl propanoid part of known GPR40 agonists. Here
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br Conclusion In summary a
2022-09-17
Conclusion In summary, a series of novel GPR40 agonists bearing phenylpropiolic casein kinase 2 inhibitor motif with favorable metabolic stability were prepared and evaluated for their activities as GPR40 agonists. Among them, compound 9 was identified as a structurally distinct GPR40 agonist po
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There has been conflicting evidence on
2022-09-17
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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SR3335 CDX is also a tumor suppressor gene
2022-09-17
CDX1 is also a tumor suppressor gene; the ablation of CDX1 and CDX2 results in a significant increase in tumor formation in the colon. CDX1 is regulated by epigenetic modification; the hypermethylation of the CpG island at the promoter is positively associated with severe clinical phenotypes. In add
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The cortical actin filaments are arranged in a network
2022-09-17
The cortical cyproheptadine hcl filaments are arranged in a network abuting the plasma membrane with a thickness of ∼190nm in living cells, that displays highly dynamic behaviors 15, 16, 17. Technical challenges, however, have hampered investigation of the detailed function dynamic interactions bet
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