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The feasibility of using the Fas Fas ligand FasL system
2022-06-15
The feasibility of using the Fas/Fas ligand (FasL) system to target vascular progenitor E7080 contributing to intimal hyperplasia has been shown in many studies [[18], [19], [20], [21], [22], [23], [24]]. Fas receptor, a member of tissue necrosis factor family, is a death receptor that initiates ap
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Our understanding of the genetic basis of myeloid malignanci
2022-06-15
Our understanding of the genetic basis of myeloid malignancies has been profoundly improved in recent years. Studies have revealed new recurrent somatic mutations in myeloid malignancies, including myeloproliferative neoplasms (MPNs), myelodysplastic syndrome (MDS) and acute myeloid leukaemia (AML).
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This connection is supported by studies
2022-06-15
This connection is supported by studies in the SIV macaque model of HIV, where treatment with methamphetamine, which greatly enhances CNS dopamine levels (Truong, 2005); increased b catenin inhibitor viral load. Methamphetamine also increased expression of the HIV co-receptor CCR5 in CNS macrophage
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Treatment with histamine had no
2022-06-15
Treatment with histamine had no effect on histamine H1 receptor expression in HepG2 BINA (Fig. 1), while knockdown of histamine H1 receptor expression prevented histamine from repressing apo A-I gene expression (Fig. 2). Overexpression of the histamine H1 receptor regulated apo A-I promoter activit
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phosphocreatine Histamine modulates an attentional state whi
2022-06-15
Histamine modulates an attentional state, which might affect performances in the object recognition test. Indeed, systemic injection of H3 receptor inverse agonists enhances the attentional state (41). However, the memory recovery in our study is unlikely to be due to the enhanced attentional state.
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It is important to mention
2022-06-15
It is important to mention that the IC50 of cetirizine needed to achieve histamine H2 receptor desensitization was 0.43 µM or 170 ng/ml (Fig. 1B), becoming clinically relevant since pharmacokinetic studies after oral administration of the clinically used dose (10 mg/day) reported a maximal plasma co
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HO acted as an intracellular
2022-06-15
HO-1 acted as an intracellular defender against oxidative stress-induced cell damage. To elucidate the effects of HO-1 in ropivacaine-induced cytotoxicity in neuronal cells, HO-1 activity was inhibited using a specific HO-1 inhibitor zinc protoporphyrin, ZnPP. Our results indicate that ZnPP treatmen
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The zinc dependent HDACs are classified into four groups
2022-06-15
The zinc-dependent HDACs are classified into four groups based on their structure, complex formation, and expression pattern: class I (HDAC1, HDAC2, HDAC3, and HDAC8), class IIa (HDAC4, HDAC5, HDAC7, and HDAC9), class IIb (HDAC6 and HDAC10), and class IV (HDAC11) [16]. We recently reported on a cyto
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Currently the computational chemical biology has been applie
2022-06-15
Currently, the computational chemical biology has been applied in hepatitis B antiviral drug discovery research [18]. Tan et al. explored oxime ethers as HBV inhibitors by docking and screening [19]. Allen et al. clarified the resistance of HBV to the nucleoside drug lamivudine [20]. The results sug
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The characterization of Da CTSL shows
2022-06-15
The characterization of Da-CTSL1 shows that it preferentially cleaves Z-FR-AFC (Fig. 8), which has a HOSu synthesis phenylalanine at P2 and Da-proCTSL1 is autocatalyzed at pH 8.0 releasing an activated Da-CTSL1 that exhibits optimal activity at pH 8 indicating that the enzyme when secreted by the f
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It is important to note that the GC
2022-06-15
It is important to note that the GC-C expression is retained in colon tumours, and therefore GC-C expression can be used as a marker to diagnose metastatic colon cancer [42]. However, expression of uroguanylin and guanylin is often lost in colorectal cancer progression [43]. Therefore, the anti-prol
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SC 79 A nitric oxide donor glyceryl trinitrite and the
2022-06-15
A nitric oxide donor, glyceryl-trinitrite, and the substrate for nitric oxide, l-arginine, have been used to treat preterm labor. However, these studies are preliminary. The beneficial effect of nitric oxide donors needs to be confirmed by more controlled studies. The probable pitfall of using nitri
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Having identified initial leads and further lead
2022-06-15
Having identified initial leads and (), further lead optimization was initiated on B- and C-rings to afford compounds with improved potency. Initial set of substituted imidazole-biphenyl-carboxylic phosphocholine derivatives – and () were evaluated for GSNOR potency. Among this, fluoro, methyl,
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Initially the synthesized compounds from were evaluated for
2022-06-15
Initially, the synthesized compounds from were evaluated for human GSNOR potency before generating additional SAR in order to understand scaffold feasibility and required functionality as illustrated in . Commercially available 4′-hydroxy-[1,1′-biphenyl]-4-carboxylic CTX0294885 having similar termin
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On the other hand it is quite possible that
2022-06-14
On the other hand, it is quite possible that strychnine-sensitive glycine sites are responsible for mediating the anticonvulsant effects of GlyT1 inhibitors. Strychnine, which acts as an antagonist at these sites, is a well-known as a convulsant drug, and elevation of endogenous glycine levels at th
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