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The MeO CFO phen yl group was then selected for
2022-04-09
The 1-MeO-4-CFO-phen-2-yl group was then selected for the C-3 position when we investigated the aryl substituents at the C-6 position of indazole. As shown in , C-6 position seems to be more tolerant than the C-3 position, as all the aryl groups examined exhibited potent hGCGR activity. Interestingl
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In our reporter assay system C H T Gli Luc
2022-04-09
In our reporter assay system, C3H10T1/2-Gli1-Luc cells were incubated with Shh CM to induce Gli1-mediated luciferase activity (Fig. 1B). Z-Ajoene inhibited Shh CM-induced luciferase activity in a concentration-dependent manner as seen in Fig. 1C. Z-Ajoene also inhibited SAG (a Smo activator)-induced
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Here we used chemogenetic modulation of
2022-04-09
Here, we used chemogenetic modulation of MBH GHSR neurons to address the role of the endogenous ghrelin system in the normal, hyperphagic response to a short-term fast. Studies demonstrating the requirement of an intact ghrelin-GHSR system for the rebound food intake following fasting have been inco
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Amongst oxidants that we have studied
2022-04-09
Amongst oxidants that we have studied, PMS is unique in having a greater effect in deoxygenated cells. The resulting phenotype shows some similarities with the increased cation permeability shown by deoxygenated sickle a replacement [27]. It is interesting to consider why PMS has this effect. PMS f
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The sexual dimorphism in dlGALR a
2022-04-09
The sexual dimorphism in dlGALR1a and dlGALR1b receptors found in the gonads of adult fish led us to hypothesize that the gene expression difference between female and males might be attributed to the differences in steroid production between female and male gonads. Interestingly we have found that
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Acute lung injury is present in
2022-04-09
Acute lung injury is present in sepsis and SIRS and is associated with increased pulmonary levels of proinflammatory cytokines and neutrophil extravasation into the alveolar space [19], [24]. Hauser et al. [25] observed that fragmented mitochondria induced pulmonary inflammation via neutrophil activ
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Binding of FGFs to FGFRs leads
2022-04-09
Binding of FGFs to FGFRs leads to receptor dimerization, resulting in the transphosphorylation of a tyrosine in the activation loop of the kinase domain. Subsequently, the activated FGFRs phosphorylate their intracellular receptor substrates, particularly FGFR substrate 2 (FRS2) and phospholipase Cγ
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In patients with breast cancer ZRANB gene
2022-04-09
In patients with breast cancer, ZRANB1 gene amplification was found in a subset of cases, and ZRANB1 protein levels correlated with EZH2 protein levels and poor survival (both TNBC and non-TNBC). Moreover, unlike normal mammary epithelial cells, all human breast cancer cell lines examined (both TNBC
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Thus far it is reported that the histone methyltransferase a
2022-04-09
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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br Acknowledgements and disclosures This work was
2022-04-09
Acknowledgements and disclosures This work was supported in part by the National Institutes of Health (R01 HL-131673-01A1) and the Veterans Administration (BX-002539-01), United States. The authors have nothing to disclose concerning any conflict of interest. Introduction Adaptations are ofte
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Haploid germ cell specific nuclear protein kinase Haspin pro
2022-04-08
Haploid germ cell-specific nuclear protein kinase (Haspin) proteins are divergent members of the eukaryotic protein kinase family. Haspin (encoded by germ cell-specific gene 2: Gsg2) is found in many eukaryotic lineages (animal, fungi, and plants), and the protein and its mRNA were initially detecte
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The initial beta carboline derivatives used in
2022-04-08
The initial beta-carboline derivatives used in the in silico docking experiments were prepared using the procedure outlined in . Harmol, , was -alkylated with -Boc-protected alkylamines in the presence of cesium carbonate to give and . The carbamate protecting group was removed under acidic conditi
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br sGC cGMP PKG pathway
2022-04-08
sGC/cGMP/PKG pathway in regulation of platelet small GTPases All classical Rho family members of small GTPases including RhoA, Rac, Cdc42, some atypical Rho GTPases like RhoB, RhoF and RhoG, and also Ras family members N-Ras, K-Ras, Rap1A, Rap1B, Rap2A and Rap2B, and the Ras-related GTPases of th
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Further SAR was explored with the imidazole series to
2022-04-08
Further SAR was explored with the imidazole series to achieve better enzyme inhibition activity (). In comparison to published earlier, replacing the amide with sulfonamide and reverse sulfonamide maintained the GSNOR inhibitory activity. It is clear that exchanging the phenyl ring (, and ) by t
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There is sufficient evidence to indicate that kisspeptin
2022-04-08
There is sufficient evidence to indicate that kisspeptin plays a role in regulating sheep reproduction. However, the molecular mechanism by which kisspeptin regulates GnRH sgk inhibitor and reproduction has remained unclear. Therefore, in this study on GnRH in sheep, the promoter region of GnRH was
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