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Introduction High mobility group box HMGB is a nuclear
2022-01-21
Introduction High mobility group box 1 (HMGB1) is a nuclear protein that plays a fundamental role in the regulation of DNA-associated events such as DNA repair, transcription, and replication. HMGB1 can be translocated to the cytosol, plasma membrane, and extracellular space in response to various
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zilpaterol In the previous paper we described
2022-01-21
In the previous paper, we described the design and synthesis of tricyclic thiazoles as FBPase inhibitors, and a series of SAR studies led to the identification of phosphate 3 and difluoromethylenephosphonate 4 exhibiting potent FBPase inhibitory activities (IC50=13, 47nM, respectively) (Fig. 2). In
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Recently considerable effort has been invested in developing
2022-01-21
Recently, considerable effort has been invested in developing FDPS inhibitors based on alternative scaffolds (including nonbisphosphonates) that allow other tissue types and parasite-derived forms of FDPS , to be targeted. There are several limits in analyzing inhibitors of FDPS activity: the most
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Our data demonstrate that cobas HCV s
2022-01-21
Our data demonstrate that cobas HCV’s performance characteristics meet these requirements, making the assay useful in the management of therapy for chronic hepatitis C. We documented that cobas HCV has the requisite LOD, measureable range (15 − 1.0E + 08 IU/mL) and precision allowing for baseline HC
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HCC is one of the most prevalent malignant tumors
2022-01-21
HCC is one of the most prevalent malignant tumors and a leading cause of cancer-related death, globally [[11], [12], [13]]. Hepatitis B virus (HBV) infection is closely related to the development of liver diseases [[14], [15], [16], [17]]. More than 350 million people are chronically infected with H
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Several compounds have been described in the literature
2022-01-21
Several compounds have been described in the literature as inhibitors of the sGC. Among them, methylene blue and LY83583 () are not direct sGC inhibitors, but rather block cGMP formation by generating superoxide anion radicals that deactivate NO. Despite their extensive use in plethora of research s
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The present study chose the fdh gene the homolog of
2022-01-21
The present study chose the fdh gene, the homolog of mammalian GSNOR, to generate UAS-fdh and fdh double-stranded RNA interference (ds-RNAi) transgenic Drosophila. These transgenic models were used to study the effect of GSNOR activity modulation on visual learning and memory and to explore the poss
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We first set out to identify the minimum pharmacophore
2022-01-20
We first set out to identify the minimum pharmacophore. Early structure activity relationships (SAR) indicated that the chloro substituents were not required and that the benzisoxazole moiety could be replaced by a number of other groups. A broad survey of “left-hand” hydrophobic moieties was conduc
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Based on work from our labs with mGlu
2022-01-20
Based on work from our labs with mGlu NAMs, and the ability of [3.3.0] systems, such as the octahydropyrrolo[3,4-]pyrrole, to effectively mimic piperazines, we focused our attention on the potential bioisoteric replacement of the [3.1.0] system of and , as well as the piperidine of , with a [3.3.0]
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Uracil DNA glycosylase UDG is a highly conserved damage
2022-01-20
Uracil-DNA glycosylase (UDG) is a highly conserved damage repair enzyme which can specifically recognize and excise uracil residue within the DNA sequences and actuate the DNA Bezafibrate excision repair (BER) pathway which keeps the maintenance of genomic integrity and stability [[21], [22], [23]]
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br Regulation of Glu transporters The pivotal role
2022-01-20
Regulation of Glu transporters The pivotal role of Glu transporters in the fine tuning and turnover of this excitatory amino Bikinin synthesis calls for a detailed characterization of its regulation. Several general mechanisms that modify Glu uptake activity have been described. These include tr
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The biological actions of ghrelin are mainly due to
2022-01-20
The biological actions of ghrelin are mainly due to its interaction with GHSR-1a (Howard et al., 1996). The pharmacological properties of D-Lys3-GHRP-6, a selective antagonist of GHSR-1a, have been extensively studied (Beck et al., 2004, Benso et al., 2007, Sibilia et al., 2006). To study the recept
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br Secretase in inflammatory diseases Secretase appears to
2022-01-20
γ-Secretase in inflammatory diseases γ-Secretase appears to play a more important role than previously recognized in inflammatory diseases. Studies have shown that mice partially deficient in PS genes (PS1+/− PS2−/−) develop an immune system deficit in late adulthood, such as ulcerated skin or a
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br Materials and methods br Results
2022-01-20
Materials and methods Results Discussion G-quadruplex structures are extensively studied for its role in central dogma of molecular biology viz. replication problems leading to chromosomal translocations [20], [21], transcriptional inhibition [32] and alternative splicing and translational
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VS strategies have been building momentum in G drug
2022-01-20
VS strategies have been building momentum in G4 drug discovery both as a low-cost enrichment step and as a lead development step in the discovery pipeline, which our laboratory has previously discussed [31]. Whereas traditional HTS methods rely on obtaining and screening hundreds or thousands of com
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