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C prevents the glutamate and erastin induced ROS
2022-08-13
C16 prevents the glutamate- and erastin-induced ROS accumulation but does not affect the decrease in GSH, indicating that prevention of ROS accumulation by C16 is not due to the restoration of GSH levels. Instead, C16 itself possessed superoxide anion scavenging activity in vitro at similar concentr
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The primary or in transit site of
2022-08-13
The primary or in-transit site of metastasis for many cancers, including melanoma, are nearby sentinel lymph nodes (LNs) [6]. As such, sentinel LN biopsy is a common procedure to diagnose and stage melanoma progression [7,8]. Sentinel LNs are often the primary site of metastasis due to tumor cell-st
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While histone modifications can alter inter nucleosomal inte
2022-08-13
While histone modifications can alter inter-nucleosomal interactions that govern the compaction state of a chromatin fiber (Francis et al., 2004, Kalashnikova et al., 2013, Lu et al., 2008), the potential impact of histone modifications on higher-order chromosome organization beyond chromatin-fiber
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The structures of KDM A revealed a Cys
2022-08-13
The structures of KDM4A revealed a Cys-His Zn(II) binding site that is close to the substrate binding spot, which bioinformatic analyses indicated was not present in any other histone demethylase subfamily. Therefore, an alternative method to inhibit the KDM4 family (95) would be to use compounds th
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br Materials and methods br Results br Discussion
2022-08-13
Materials and methods Results Discussion Several histamine H3 receptor antagonists have progressed into clinical development for indications including Alzheimer's disease, schizophrenia, pain and narcolepsy. Each of the compounds studied herein has been extensively characterized in its own
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Unfortunately the approved drugs suffer from
2022-08-12
Unfortunately, the approved drugs suffer from failure in many cases [5,6]. Several mutations occur in the binding site of NS3/4A protease, which affect drug binding and cause drug resistance [13]. It is a big challenge and needs more efforts to be done. This is the reason why research is still conce
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GSTP is a class Glutathione S transferase GST enzyme
2022-08-12
GSTP1 is a π-class Glutathione S-transferase (GST-π) enzyme involved in tumor suppression by protecting 46619 against genomic damage mediated by various oxidants. Although the loss of GSTP1 function by hypermethylation has been reported as a common epigenetic alteration in prostate carcinogenesis (
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The number of small molecule GSK inhibitors is continuously
2022-08-12
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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br Expression profile of GPR As noted
2022-08-12
Expression profile of GPR35 As noted above, initial studies indicated expression of GPR35 in rat intestine [1] and stomach [2]. Subsequent studies have confirmed significant expression levels in the small intestine, colon and stomach, and this might be relevant in the association between a GPR35
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Molecular modeling studies also revealed insignificant diffe
2022-08-12
Molecular modeling studies also revealed insignificant differences in ligand-receptor interaction energies between R and S enantiomers of LPCs or their 2-OMe-analogues, suggesting that enantiomers of a particular structure should exert similar GPR119-mediated biological effect. Indeed, when studied
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To effectively evaluate prospective mechanisms by which chro
2022-08-12
To effectively evaluate prospective mechanisms by which chronic HIV infection induces pulmonary fibrotic changes in humans, we confirmed that predisposition to fibrotic change in older individuals could be mimicked in a mouse model. Hydroxyproline is a nonessential amino pacap required for the synt
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hydroxylase Through a large scale phylogenetic analysis of
2022-08-12
Through a large-scale phylogenetic analysis of UDG superfamily in more than 1000 completely sequenced genomes, it is shown that family 3 hydroxylase can be separated into two clades with the traditional family 3 SMUG1 as one of them (Fig. 1) [31]. UDG enzymes in another clade are present in eubacter
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Phylogenetic trees of receptors for peptides similar
2022-08-12
Phylogenetic trees of receptors for peptides similar to glucagon from diverse vertebrate species typically are similar to the tree presented in Fig. 3 (Sivarajah et al., 2001, Chow et al., 2004, Irwin and Wong, 2005, Cardoso et al., 2005, Cardoso et al., 2006, Ng et al., 2010, Park et al., 2013, Hwa
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br Introduction HH GLI signaling is one of
2022-08-12
Introduction HH-GLI signaling is one of the major pathways involved in both normal and neoplastic development [[1], [2], [3], [4]]. Inappropriate activation of this pathway has been linked to cancer, including medulloblastoma, rhabdomyosarcoma, basal cell carcinoma and cancers of the lung, stomac
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Two excellent GSMs with clear pharmacological effect across
2022-08-12
Two excellent GSMs with clear pharmacological effect across rats, dogs, monkeys, and human subjects are BMS-932481 and BMS-986133 with IC50 at 6.6 and 3.5 nM to reduce Aβ42, respectively. Both GSMs exhibit dose- and time-dependent activity in vivo by decreasing Aβ1-42 and Aβ1-40 levels while increas
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