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GPR agonistic activity was evaluated for
2021-09-17

GPR119 agonistic activity was evaluated for the human GPR119 receptor in a cell-based cAMP assay. The results expressed the potency as EC values and the inherent activity (IA) as percentages which were compared to the test compound with oleoylethanolamide (OEA), an endogenous ligand of GPR119 (defin
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br Methods br Results br Discussion LPD in
2021-09-17

Methods Results Discussion LPD, in terms of insufficient secretion of progesterone by the CL, reflected by low serum progesterone levels can occur in IVF attempts using any kind of ovarian stimulation protocol (Fatemi et al., 2007, Garcia et al., 1981, Van der Linden et al., 2011). However,
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The LBD experiences a large scale conformational transition
2021-09-17

The LBD experiences a large-scale conformational transition between open and closed states upon agonist binding within the cleft separating the two lobes of the domain. The upper lobe (Lobe 1, also called D1) is connected to the ATD, and the lower lobe (Lobe 2, also called D2) is connected to the TM
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Since the isoflavone emerged as privileged scaffold in
2021-09-17

Since the isoflavone emerged as privileged scaffold in Hh inhibition, based on molecular modeling predictions and prior studies [17,22], here we designed a number of isoflavones able to interact preferentially with the Smo receptor or the Gli protein. Molecules were synthesized by means of a novel s
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The presence of ghrelin s mRNA
2021-09-17

The presence of ghrelin's mRNA in the eye and the presence of ghrelin in the aqueous humor, along with a decrease of its levels in glaucoma, suggest a local role for this peptide in the ocular tissue [8], [16], [18]. There is no available data regarding the presence of GHSR-1 in the anterior segment
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The GAL also modified HT
2021-09-17

The GAL(1–15) also modified 5-HT system (Millon et al., 2015). Using a rat medullary raphe-derived cell line RN33B, we observed that GAL(1–15) significantly decreased the 5-HT immunoreactivity in the RN33B LY 303511 (p Conclusion All these data emphasized the role of GAL and its N-Terminal fragme
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G quadruplex DNA structures may exist in either positive
2021-09-17

G-quadruplex DNA structures may exist in either positive or negative strand of a promoter to regulate gene expression. The positive strand of the HOXC10 promoter is overall C-rich in the 1000 bp upstream of the TSS (36.6% of C versus 24.1% of G) and contains many C-runs; thus, G-quadruplex structure
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br General features of FGFRs and inhibitors br Conclusion
2021-09-17

General features of FGFRs and inhibitors Conclusion Given the critical role of FGFRs in the progression of tumors, the co-crystal structures of these kinases in complex with inhibitors are determined in order to clarify the mechanism of actions and explore new efficient inhibitors. This manusc
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Finally the optimized leads and were tested
2021-09-17

Finally, the optimized leads (−)- and (−)- were tested in rat model of CIPN (3 and 30 mg/kg, po, qd, administered for 7 days) and the results have been shown in . Under acute set up, after single oral administration at 30 mg/kg, both the compounds exerted significant improvement of the NP condition
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br Heme and the HO system Heme a complex
2021-09-16

Heme and the HO system Heme, a complex of iron and protoporphyrin IX, has versatile functions, which are critical for the survival of all aerobic organisms including mammalians and bacteria [9]. The central iron in heme facilitates six ligand binding sites [10], four of which are occupied by nitr
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An important example of a frame is the lattice
2021-09-16

An important example of a frame is the lattice of open subsets of any topological space X. The correspondence is clearly functorial (by taking inverse images), and consequently one has a contravariant functor with the category of topological spaces and continuous maps as domain category. The fun
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br Epigenetic regulation of OA pathogenesis Although epigeno
2021-09-16

Epigenetic regulation of OA pathogenesis Although epigenome of each cell is unique but can undergo temporal and spatial changes in response to environmental stimuli such as diet, exercise, smoking and disease status. Aberrant epigenetic modifications due to environmental factors are associated wi
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In mammals meiotic maturation is
2021-09-16

In mammals, meiotic maturation is the process that couples completion of MI with the acquisition of developmental competence to support fertilization (Figure 1). In females there are several hallmark maturation events that are linked to the cell cycle. First, meiosis is not continuous, it is initia
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A nitric oxide donor glyceryl
2021-09-16

A nitric oxide donor, glyceryl-trinitrite, and the substrate for nitric oxide, l-arginine, have been used to treat preterm labor. However, these studies are preliminary. The beneficial effect of nitric oxide donors needs to be confirmed by more controlled studies. The probable pitfall of using nitri
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The relationship between increased GPR expression in
2021-09-16

The relationship between increased GPR120 expression in the EDL skeletal muscle and systemic glucose control is yet to be investigated. However, if the increased expression of GPR120 correlates with enhanced insulin-stimulated glucose uptake in skeletal muscle, particularly the EDL muscle, this migh
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