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br Results and discussion br Conclusion
2021-06-22
Results and discussion Conclusion In this investigation, pharmacophore models of CK1 inhibitors were developed using a pharmacophore modeling protocol proposed by us. The optimal pharmacophore hypothesis, Hypo2, was adopted to retrieve potential CK1 inhibitors from the commercial chemical data
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mt t It is of interest to
2021-06-22
It is of interest to point out that curcumin in this study reduced body weight gain; the underlying mechanism may be due to a decrease in general mt t of fat, which was associated with a significantly reduced NPC1L1 expression in small intestine. Labonte et al revealed that NPC1L1 deficiency or ezet
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MdHCLB channels expressed in Xenopus oocytes
2021-06-22
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
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Currently phosphodiesterase type PDE inhibitors are used
2021-06-22
Currently, phosphodiesterase type 5 (PDE-5) inhibitors are used widely as the first- line oral treatment for erectile dysfunction of varying causes. Radical prostatectomy for the treatment of prostate cancer is frequently associated with erectile dysfunction, and this type of erectile dysfunction is
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PI K Akt signaling pathway is
2021-06-22
PI3K/Akt signaling pathway is known in modulating cell apoptotic process (Saurus et al., 2015). To study the contribution of PI3K/Akt signaling pathway in ERRγ-mediated anti-apoptotic effect in podocytes, we examined phosphorylation of Akt and expression of PI3K subunits p110α and p85α via qRT-PCR
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There may be an interplay
2021-06-22
There may be an interplay of EP2, EP3, EP4 alone, or in combination, with EP1 for the onset of TCDD-induced neonatal hydronephrosis. EP2 and EP4 have been reported to increase AQP2 phosphorylation and membrane trafficking (Li et al., 2009; Olesen et al., 2011). The EP2 and EP4 mRNA concentrations we
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Compared to ET all agonists tested showed a fold
2021-06-21
Compared to ET-1, all agonists tested showed a 2–4 fold bias for the G protein constrictor assay compared to the β-arrestin assay (Table 1). This preliminary analysis indicated that at least modest pathway bias for endogenous ET peptides is possible, however the physiological significance of this, i
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Recent studies support the concept that dietary metabolites
2021-06-21
Recent studies support the concept that dietary metabolites, such as retinoids and AHR ligands, regulate ILC3 function. These metabolites act through intracellular nuclear receptors that function as transcription factors, thereby controlling ILC activity through the stimulation of specific transcrip
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While a number of studies have helped elucidate the
2021-06-21
While a number of studies have helped elucidate the principles of target amino group specificity, UBL selectivity, and Ub dpn specificity [3], [4], [9], [10], [14], [19], [20], [23], [24], [33], [34], [37], [38], [39], [40], [41], the role of the canonical E2-RING interface in governing substrate u
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The structure of the HOIP RBR LDD module bound
2021-06-21
The structure of the HOIP RBR–LDD module bound to UbcH5~Ub reveals insights into an activated HOIP component [47]. Contacts between the E2~Ub and the non-cognate RBR module in the crystal suggest how a structure in which the active sites of the E2 and the E3 are in close proximity might look. In thi
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Dipeptidyl peptidase inhibitors DPP is or gliptins stimulate
2021-06-21
Dipeptidyl peptidase-4 inhibitors (DPP-4is or gliptins) stimulate both post-meal insulin secretion and inhibit xanthine oxidase secretion in a glucose-dependent manner, rendering the risk of hypoglycaemia minimal [10]. They are weight-neutral or may even induce slight weight loss. Their good efficac
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br GPCRs form heterotetramers In addition to homodimers and
2021-06-21
GPCRs form heterotetramers In addition to homodimers and heterodimers, for several family A receptor heteromers, experimental evidence supports the presence of higher order rearrangements as tetrameric structures, comprised of two different homodimers, each able to signal with its preferred G pro
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Cyclin D inhibits the transcriptional activity
2021-06-21
Cyclin D1 inhibits the transcriptional activity of the transcription factors myogenin and MEF2 [39,40]. In addition, myogenin activates MEF2 expression, which feeds back to amplify the myogenin promoter [38]. In this study, DGKδ suppression, in addition to the increase of cyclin D1, inhibited myogen
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br Introduction Localized degenerative and progressive enlar
2021-06-21
Introduction Localized, degenerative and progressive enlargement of the aortic diameter involves all layers of the vessel wall may ultimately rupture creating a catastrophic cardiovascular event [1,2]. An aneurysm may be located in the thoracic or abdominal aortic wall with different clinical app
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Confidence with which data of animal safety toxicity
2021-06-21
Confidence with which data of animal safety/toxicity studies can be translated to human depends upon the knowledge that whether humans would be exposed to similar chemical entities (parent and its metabolites) as the animals exposed during toxicity studies. In this regard, in vitro qualitative evalu
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