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As comparators compounds and were made using
2022-02-08

As comparators, compounds and were made using the pyrazolopyridine core with the CF triazole attached. The 2-fluorophenyl group was replaced with the methylpyrimidine in compound . The potency of these compounds were very good and compound looks attractive from a physicochemical perspective as it
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br Conflict of interest br
2022-02-08

Conflict of interest Acknowledgement Exposure to tobacco smoke in early life has been found to increase the risk of developing asthma and lung function deficits in adolescence and adulthood., , , , However, not all children exposed to tobacco smoke in early life develop asthma, which sugges
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A motivation for this study is the ability of
2022-02-08

A motivation for this study is the ability of PGD2 to inhibit hair lengthening (). Here we demonstrate that PGD2 also inhibits hair regeneration after wounding. Thus, PGD2 and Gpr44 inhibition of the hair follicle occurs in multiple contexts and may be exploited in future therapies. Pharmaceutical c
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br Discovery of GPR A The murine
2022-02-07

Discovery of GPR109A The murine niacin receptor, protein upregulated in macrophages by interferon-γ (PUMA-G), was identified as a G-protein-coupled receptor (GPCR) expressed in adipocytes and spleen [22], [23]. This finding suggested a role of this receptor in macrophage function [24]. In 2003, t
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SGCs tightly ensheath the soma
2022-02-07

SGCs tightly ensheath the soma of DRG neurons (Costa and Moreira, 2015, Hanani, 2005, Takeda et al., 2009). Intimate associations between SGCs and neurons facilitate bidirectional regulation of SGC function and neuronal excitability. After nerve injury, neuronal hyperexcitability can result in SGC a
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In the spinal cord EAAT constitutes of all high
2022-02-07

In the spinal cord, EAAT1 constitutes 40% of all high-affinity EAATs, and it is abundantly present in lumbar dorsal horn (Queen et al., 2007). In physiological conditions, EAATs remove glutamate from the synaptic cleft by co-transporting glutamate and sodium into adjacent glial cells. The inefficien
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The usefulness of GIP R antagonism for the treatment of
2022-02-07

The usefulness of GIP-R antagonism for the treatment of obesity-diabetes has been revealed in numerous studies employing knockout or chemical blockade of GIP-R signalling.*88, 89, *90, 91, 92, 93, 94, 95, 96, *97 For example, sub-chronic daily administration of (Pro3)GIP to ob/ob mice results in sig
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Recent studies suggest that the
2022-02-07

Recent studies suggest that the biological importance of endogenous ghrelin becomes accentuated during exposure to more metabolically-constrained and stressful environments. Indeed, mice lacking either ghrelin or GHSR demonstrate impaired ability to adapt metabolically and/or behaviorally to caloric
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GSIs were shown to effectively decrease A levels
2022-02-07

GSIs were shown to effectively decrease Aβ levels at doses close to or higher than their IC50 values in cell culture models. Surprisingly, they also slightly increase Aβ levels at low doses, (significantly below the IC50) also known as “Aβ rise”, due to various mechanisms including inhibition of cel
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So far only few studies report about
2022-02-07

So far only few studies report about GAL in the visual system: GAL has been detected in the cornea of rat (Jones and Marfurt, 1998), mouse (Henken and Martin, 1992) and pig (Stone et al., 1988), and in the uvea of rat (Strömberg et al., 1987), pig (Stone et al., 1988) and cat (Grimes et al., 1994),
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HPK 56 australia Brain derived neurotrophic factor BDNF is t
2022-02-07

Brain-derived neurotrophic factor (BDNF) is the most abundant growth factor in the brain and is critical for neuronal development and synaptic plasticity (Bekinschtein et al., 2008; Lu et al., 2014). Besides playing an important role in mood and cognition, BDNF is also involved in the regulation of
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FBP ALDOA complex is located
2022-02-07

FBP2-ALDOA complex is located on both sides of Z-line in striated muscles (Rakus et al., 2003a; Gizak et al., 2003) and its stability is regulated by calcium ions (Mamczur et al., 2005; Rakus et al., 2013) (Fig. 3). An increasing titre of [Ca2+] which occurs during muscle contraction stimulates diss
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It has been demonstrated that RA regulates
2022-02-05

It has been demonstrated that RA regulates gene FG2216 through an epigenetic mechanism during stem cell and cancer cell differentiation. In neuroblastoma cells, RA induced neural maturation through RET gene transcriptional activation by increasing H3K4me3 levels at the promoter region and demethyla
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br Materials and methods br Results Estimations of OMP
2022-02-05

Materials and methods Results Estimations of OMP generated by the proposed mechanism (Fig. 1) were first performed for the range of 0.001–2 mM of Spermine NONOate concentration in the cytosol. It was assumed that only 5% of all VDACs in MOM form the ANT-VDAC1-HKI contact sites, and that the fr
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Sonidegib is currently under investigation for the treatment
2022-02-05

Sonidegib is currently under investigation for the treatment of relapsed/refractory acute leukemia (NCT01826214) [76]. All patients experienced at least 1 AE, including anemia, diarrhea, fatigue, nausea, muscle spasms, decreased appetite, and blood creatine phosphokinase increased. The ongoing phas
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