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Based on pharmacophore modeling a good
2022-06-16
Based on pharmacophore modeling, a good HDAC inhibitor has at least three sides/regions: the attachment side of the Zn2+ cofactor/HDAC active site (Zn2+ binding group/ZBG), hydrophobic cap (CAP) and linker containing connecting unit (CU) with electronegative groups (Mohan et al., 2011, Rossi et al.,
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br STAR Methods br Acknowledgments Anthony Koleske is thanke
2022-06-16
STAR★Methods Acknowledgments Anthony Koleske is thanked for helpful discussions and for providing p190RhoGAP-A cDNA. Anatoly Kiyatkin and Mark Lemmon are thanked for use of the BioTek Synergy 2 plate reader for the MANT assays. Leena Kuruvilla is thanked for assistance with the thermal shift a
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The number of small molecule GSK inhibitors is continuously
2022-06-16
The number of small molecule GSK-3 inhibitors is continuously rising and many have been tested in animals. These studies have provided additional support for specific roles of GSK-3 in neuronal functions under both normal and pathological conditions. Inhibition of GSK-3 has profound effect on neurop
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Differentiation to either Th or Th
2022-06-16
Differentiation to either Th1 or Th2 Ro 5-3335 mg is significantly influenced by the relative expression of T-bet and GATA-3, respectively (Zhu et al., 2006, Jenner et al., 2009). T-bet acts as a key regulator of Th1 cell fate determination and directly activates IFN-γ and suppresses IL-4 (Szabo et
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The activation of the ERK pathway participates in the transm
2022-06-16
The activation of the ERK pathway participates in the transmission of pain signaling by sensitizing primary afferents (Ji et al., 2009, Lai et al., 2011). Thus, the blockade of ERK activation in the primary sensory imidazole can reduce the mechanical hypersensitivity and the thermal hypersensitivit
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The aim of our study
2022-06-16
The aim of our study was to investigate the polymorphisms of RAGE and glyoxalase I gene and sRAGE serum levels in patients with pathological pregnancy trying to describe the genetic background of pathological pregnancy or to find a new biochemical marker (sRAGE) of these pathological states in pregn
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br Acknowledgements br Introduction Benzodiazepine BZ treatm
2022-06-16
Acknowledgements Introduction Benzodiazepine (BZ) treatment is widely used for quick and efficient anxiolytic and sedative responses. However, when the use is extended to longer periods, adverse effects emerge. These include tolerance to the initial drug effect, dependence as revealed by withd
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br Materials and methods br Results br
2022-06-15
Materials and methods Results Discussion In this study, we discover that Sufu stabilizes Gli1 protein levels by antagonizing Numb/Itch-mediated protein degradation. Together with previous work that demonstrates control of Gli2/3 protein levels by Sufu (Chen et al., 2009, Jia et al., 2009, W
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One way to approach this unifying hypothesis
2022-06-15
One way to approach this unifying hypothesis will be to compare the effects of the PBR/VDAC ligands on these processes. Recent studies have demonstrated that the three ligands of peripheral-type benzodiazepine receptor, i.e. PK 11195, Ro5-4864 and diazepam reduce membrane transport and conductance i
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Following optimization chemicals which were
2022-06-15
Following optimization, 31 chemicals, which were considered as the skin sensitizers and non-sensitizers in LLNA studies, were studied for their potential of β-galactosidase suppression (Table 2). The detailed information on test chemicals used were given in Table 1. With optimum cell densities, E. c
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In a recent study Neelaveni et al revealed that
2022-06-15
In a recent study, Neelaveni et al. [47] revealed that new thiazolidinedione derivatives (Fig. 6 a and 6 b) produced dual PPARγ and FFAR1 agonistic activity at micromolar concentrations with insulin sensitizing effects and enhanced insulin secretion from the pancreas. These derivatives were reported
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chlorpromazine hydrochloride Introduction Type diabetes T D
2022-06-15
Introduction Type 2 diabetes (T2D) has been seriously affecting the health life of 415 million people and 193 million undiagnosed people [1]. Importantly, this disease was found to cause death at least 1.5 million annually, and has brought about an extensive health concern throughout the world [2,3
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The investigation in vitro revealed that aldolase as
2022-06-15
The investigation in vitro revealed that aldolase, as well as FBPase, has affinity to α-actinin, one of the structural protein of the Z-line (Rakus et al., 2003a, Mamczur et al., 2005). Therefore, the existence of in vivo heterologous complex, consisting of aldolase, FBPase and α-actinin has been po
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br Hydroxyfarnesyl diphosphate was synthesised in three
2022-06-15
12-Hydroxyfarnesyl diphosphate (6) was synthesised in three steps starting from commercially available (E,E)-farnesol (10) (Scheme 5). Chlorination of 10 gave farnesyl chloride (11) in a quantitative yield, which was carried forward without purification. The following step was a selenium dioxide-c
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Over the last decade intense efforts
2022-06-15
Over the last decade, intense efforts have been devoted toward identifying IN inhibitors as potential drugs against HIV. Raltegravir and elvitegravir are integrase strand transfer inhibitors (INSTIs) that have been approved for therapy and dolutegravir is another INSTI that is currently in advanced
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