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Optimization of the tetrahydroindazole series
2021-09-17
Optimization of the tetrahydroindazole series led to the discovery of two moderately potent γ-secretase modulators, 2-cyclobutane and 2-hydroxy-2-methylpropane which were subsequently evaluated in a kinetic aqueous solubility assay. Unfortunately, neither analog demonstrated improved solubility ()
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Some previous findings indicate that GALP has
2021-09-17
Some previous findings indicate that GALP has an influence on AVP and OT secretion from the posterior pituitary gland. Cunningham et al. (2004) noted that the expression of GALP mRNA was increased in the neurohypophysis of lactating rats compared to non-lactating rats, whereas GALP mRNA expression i
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br Materials and methods br Results Bgal
2021-09-17
Materials and methods Results Bgal from Alteromonas sp. ML117 had an open reading frame of 3126 bp encoding 1042 amino A 967079 residues with a predicted mass of 120 kDa and a theoretical pI (isoelectric point) of 5.44. The recombinant Bgal contained a His tag, as well as other additional amin
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br Conflicts of interest br Significance
2021-09-16
Conflicts of interest Significance p53 is required for the induction of cell senescence to limit the proliferation of polyploid cells. We found that Hippo signal deficiency or Yap activation in mouse livers result in polyploid formation and polyploid cell growth. The combined loss of Hippo sig
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br Direct effect of HDACs on contractile function by
2021-09-16
Direct effect of HDACs on contractile function by deacetylating cytoskeletal and contractile proteins Role of HDACs in electropathology by transcriptional reprogramming Next to deacetylation of α-tubulin by HDAC6 in experimental and human AF, there is also evidence for transcriptional reprogra
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Several studies have reported that the genotype and allele f
2021-09-16
Several studies have reported that the genotype and allele frequencies of S267F vary considerably between different study groups and geographical regions (Ezzikouri et al., 2017, Hu et al., 2016, Lee et al., 2017, Li et al., 2014, Pan et al., 2011, Peng et al., 2015, Yang et al., 2016, Zhang et al.,
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Annexin A ANXA a member of annexin superfamily is
2021-09-16
Annexin A7 (ANXA7), a member of annexin superfamily, is a Ca2+- and phospholipid-binding protein and possesses GTPase activity [5,6]. The ANXA7 gene is located on human chromosome 10q21, where multiple potential tumor suppressor genes exist. Homozygous ANXA7 (−/−) knockout mice showed a lethal pheno
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br Materials and methods br Results br Discussion
2021-09-16
Materials and methods Results Discussion To understand the molecular basis for how ghrelin secretion is regulated at the cellular level, we identified the full repertoire of 7TM receptors and G proteins in gastric ghrelin Exo1 and functionally characterized the majority of the receptors wh
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lpa receptor Studies utilising GPR mice however report diffe
2021-09-16
Studies utilising GPR55−/− mice, however, report different effects of GPR55 on body weight and insulin sensitivity. Genetic deletion of GPR55 appears to have no effect on overall body weight 5, 6, 7. However, one of these studies found increased fat deposition and insulin resistance in GPR55−/− mice
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93 6 For molecules with potential for therapeutic use high
2021-09-16
For molecules with potential for therapeutic use, high potency is desired, preferably in the nM or lower concentration range. However, the glycine receptor specific peptides identified with the New England Biolabs Ph.D. libraries, both in this study (Fig. 3) and by Tipps et al. (2010), acted at low
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In the a first in
2021-09-15
In the 2003, a first in vitro indication of modulation of FXR expression in CRC showed that FXR expression was absent in undifferentiated colon carcinoma cell line SW480, while it was progressively increasing along with the degree of cell differentiation in Caco2 and HT29 cells, and its transcriptio
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br ACKNOWLEDGMENTS br Introduction Odorant receptors
2021-09-15
ACKNOWLEDGMENTS Introduction Odorant receptors (ORs) are the largest subfamily of G protein-coupled receptors (GPCRs) and are mainly expressed by olfactory sensory neurons in the nose for the detection of various odorants [1]. However, more recent reports suggest that ORs are also expressed an
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Polyunsaturated fatty acids PUFAs represent
2021-09-15
Polyunsaturated fatty acids (PUFAs) represent a class of lipids that contain two or more carbon double (unsaturated) bonds (CC) and classified as n-3, n-6 and n-9 fatty acids. PUFAs including n-3 such as docosahexaenoic Hypotaurine (DHA), eicosapentaenoic acid (EPA) and n-6 such as arachidonic acid
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The F P concentration reported for a resting rabbit muscle
2021-09-15
The F6-P concentration reported for a resting rabbit muscle [20] reduced the KAapp for aldolase–FBPase complex more than 50 times compared to KAapp for aldolase–FBPase in the absence of effectors (Fig. 1b and Table 1). A standard assay for determination of FBPase activity in a complex with aldolase
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FDP is considered as key intermediate
2021-09-15
FDP is considered as key intermediate in the isoprenoid biosynthetic pathway, since it is the common precursor of polyisoprene units and farnesylated proteins (Cao et al., 2012). In order to understand the role of FDP gene in rubber-producing plants it is of critical importance to ZD 7288 and chara
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