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The typical pharmacophore for GPR agonists contains
2021-12-17

The typical pharmacophore for GPR40 agonists contains four parts: head (acid moiety), central (phenyl ring), linker and tail (aromatic carbocyclic or heterocyclic ring) [20]. On the other hand, the chemical features that are required for the PPARγ agonists include hydrogen bond donors and acceptors
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Epidemiological studies revealed that vitamin D deficiency w
2021-12-17

Epidemiological studies revealed that vitamin D deficiency was associated with a wide range of neuropsychiatric disorders and neurodegenerative diseases, in particular, Alzheimer's and Parkinson's disease (Annweiler et al., 2013; Knekt et al., 2010), dementia and cognitive function impairment (Balio
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There are human genes in the SLC A family
2021-12-17

There are 12 human genes in the SLC5A family, and 6 of these are expressed in human heart (Table 2). Little is known about SGLT proteins in the heart. Zhou et al. [56] reported the presence of SGLT1 mRNA in the human heart. Researchers have found that levels of SGLT1 mRNA in heart are approximately
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Work in the Ruiz i Altaba lab was funded by
2021-12-17

Work in the Ruiz i Altaba lab was funded by grants from the Swiss National Science Foundation, the Ligue Suisse Contre le Cancer, the European FP7 Marie-Curie Initial Training Network HEALING, a James McDonnell Foundation 21st Century Science Initiative in Brain Cancer-Research Award and funds from
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The waiting time for first arrival of cells into
2021-12-17

The waiting time for first arrival of SANT-1 into the dense fraction of 3–4 min at the normal chloride conductance, and about 30 min with inhibition to about 10% of the normal value, signifies that the Gardos channels in the activated cells become maximally or near maximally activated, corresponding
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In perimenstrual catamenial epilepsy there is emerging
2021-12-16

In perimenstrual catamenial epilepsy, there is emerging evidence to suggest that P withdrawal plays a key role in seizure exacerbations occurring around the time of menstruation (Backstrom et al., 1984, Bonuccelli et al., 1989, Scharfman and MacLusky, 2006). The mechanisms underlying ovarian cycle-r
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LXRs are physiological regulators of
2021-12-16

LXRs are physiological regulators of cholesterol and lipid metabolism and influence glucose metabolism. In addition, they have been shown to repress transcription of certain pro-inflammatory genes (Jakobsson et al., 2012; Ogawa et al., 2005; Terasaka et al., 2005). Thus, LXRs can either activate or
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The PK and the tissue distribution
2021-12-16

The PK and the tissue distribution profiles of 15k, 15j, 14d and 2 (Table 8) in male ICR mice were assessed. 15k, 15j, 14d all exhibited prolonged half-lives and improved plasma exposure. 15k achieved the highest concentration (15.45 μg/mL) in plasma among four compounds. The observation that 15j (S
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So what makes a FFAR agonist
2021-12-16

So what makes a FFAR1 agonist different and interesting? As shown in the , the cellular mechanism is different from those of present insulin-releasing pharmacotherapies—namely the secretion initiators (sulphonylureas and meglitinides) and the incretin-based secretion potentiators (glucagon-like pept
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The NGS of six Southern
2021-12-16

The NGS of six Southern Brazil patients revealed three different variants: c.472C > T (p.Arg158Trp); c.958G>A (p.Gly320Arg) and c.986T>C (p.Leu329Pro) (Table 2). The amino acids involved in these substitutions were evolutionarily conserved in different species (Fig. 1B). The amino caspofungin invol
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br Experimental procedures br Conflicts of interests br
2021-12-16

Experimental procedures Conflicts of interests Introduction Here we investigate differences in growth properties and short-term morphological changes in response to ET-1 in Chinese hamster ovary (CHO) cells stably and separately expressing ETA or ETB receptors. A stably transfected CHO syst
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While IN inhibitors are a relatively new
2021-12-16

While IN inhibitors are a relatively new addition to the clinician's palette of drugs to formulate HAART regimes, resistance to both INSTIs and LEDGINs has been observed. For example, even within Australia where it is estimated that 25,313 people are currently living with HIV and the infection rate
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On the other hand G a GLP could also alter
2021-12-16

On the other hand, G9a/GLP could also alter neuronal function without directly altering the transcription level of particular plasticity-related protein: the consolidation of early-LTP to late-LTP, as well as the reversal of mGluR-LTD by G9a/GLP inhibition required PKMζ translation and its downstrea
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br Results and Discussion The Set
2021-12-16

Results and Discussion The Set7 sequence is homologous to the other identified histone methyltransferases in S. pombe (Figure S1) and also shares similarity with human HMTases, H3K9 GLP/Ga9, and H4K20 SUV420H1 (Figure S1). Set7 fused with the GFP (Set7-GFP) localized in the nucleus and cytoplasm
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AGN 194310 mg The first suggestion that histamine may
2021-12-16

The first suggestion that histamine may play a role in memory consolidation was from Almeida and Izquierdo (de Almeida & Izquierdo, 1986) who showed that the immediate posttraining intracerebroventricular (i.c.v.) administration of 1–10ng of the drug were found to enhance the retention of one-trial
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