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br Conclusions Several lines of evidence have
2024-03-06
Conclusions Several lines of evidence have been established, which support the adenosine kinase hypothesis of epileptogenesis, which is based on a sequence of events leading from acute SKF38393 HCl injury to initial downregulation of ADK, rise in extracellular adenosine, changes in astrocytic ade
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Wnt agonist 1 During the course of our ACK
2024-03-06
During the course of our ACK1 inhibitor program, a high-throughput screening (HTS) campaign of our internal sample collection was conducted. A series of -aryl pyrimidine-5-carboxamides of the general structure () was identified. Earlier studies of the structure–activity relationship (SAR) of identif
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In terms of the ring B C position while C
2024-03-06
In terms of the ring B C5′ position, while C5′-F (compound ) was tolerated, C5′-Me (compound ) and C5′-Cl (compound ) substitutions resulted in a loss in potency. However, the C5′-OMe substitution (compound ) resulted in a ∼3-fold increase in potency compared to . Modeling suggested a pseudo hydroge
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For both the hydroxylation and lyase
2024-03-05
For both, the 17α-hydroxylation and 17, 20-lyase reactions, the heme iron center of P450 17A1 receives electron reducing equivalents from CPR. Both reactions require one pair of electrons and molecular oxygen for the conversion of the substrate into product in each catalytic cycle. However, the 17,2
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In this report we introduce
2024-02-23
In this report, we introduce a new method for identifying aminopeptidases. Because single substrates can be insufficient for enzyme identification, we used an entire library of substrates to obtain more information about enzyme activity and to directly detect aminopeptidases. Moreover, substrates ca
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br Polymorphic variation ERAP is polymorphic and
2024-02-23
Polymorphic variation ERAP1 is polymorphic and several single nucleotide polymorphisms (SNPs) in its gene that encode amino OTX-015 changes have been associated with predisposition to a variety of diseases, ranging from viral infections to cancer and autoimmunity (Alvarez-Navarro and Lopez de Cas
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We recently identified a G A dependent epigenetic
2024-02-23
We recently identified a G9A-dependent epigenetic mechanism for transcriptional activation of the serine pathway in cancer cells (Ding et al., 2013). G9A, also known as EHMT2 and KMT1C, is a H3K9 methyltransferase that has a primary role in catalyzing H3K9me1 and H3K9me2 in euchromatin (Shinkai and
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br Materials and method br Result
2024-02-23
Materials and method Result and discussion Conclusion Acknowledgments This work is partly supported by the University Research Committee (URC) of the Senate of The Federal University of Technology, Akure. The authors thanked IFS for the funds (F/4449 1F and F/4449-2F) used to purchase th
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APN accounts for of total plasma proteins
2024-02-23
APN accounts for 0.01% of total plasma proteins in humans; this proportion increases with age to a small extent (Barb et al., 2007). Normal APN levels in the circulation range 3–30μg/mL (Aprahamian and Sam, 2011). APN levels are lower in men than women due to the presence of testosterone and even mo
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The disease stimulatory effects of hyperadiponectinemia
2024-02-23
The disease-stimulatory effects of hyperadiponectinemia in patients contradict a previous view based on studies of preclinical models showing that APN might be beneficial for AD [8]. Indeed, despite the action of APN as a risk factor in patients with AD, APN is protective against oxidative stress-in
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Fencilli et al reported derivatives
2024-02-23
Fencilli et al. reported derivatives of PHA-680626 (15) which demonstrated strong anti-proliferative activity against large group of leukaemia cell lines including IM-resistant BAF3 cells expressing mutants like T315I, M351T and E255K. Decrease in Histone H3 phosphorylation led to induction of endo-
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br Ataxia telangiectasia and Rad related
2024-02-23
Ataxia–telangiectasia and Rad3 related as a therapeutic target Several concerns revolving around functional inhibition of ATR have hindered the exploitation of ATR as therapeutic target in cancer therapy and delayed the development of specific ATR kinase inhibitors. It was anticipated that pharma
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Findings of the present study
2024-02-23
Findings of the present study provide a molecular mechanism for the elevated ASK1 expression in obesity and how it may be functionally linked to whole-body insulin resistance. The role our findings assign to increased E2F1 in upregulating ASK1 parallels the capacity of this transcription factor to r
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However one should keep in mind that these results
2024-02-23
However, one should keep in mind that these results may not reflect exactly in vivo antioxidant activity. Many other issues such as absorption, metabolism and physicochemical properties of different antioxidants must also be considered (Prior et al., 2007, Wu et al., 2004). Some research groups are
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The most common grade AEs associated
2024-02-22
The most common grade 3/4 AEs associated with the soluble fusion protein ziv-aflibercept are neutropenia, hypertension, and diarrhea [63]. In general, medical oncologists associate ziv-aflibercept with worse toxicity than BV, and meta-analyses of clinical trial data with ziv-aflibercept or BV suppor
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