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The synthesis of compounds and were achieved according to
2022-04-19

The synthesis of compounds and were achieved according to standard procedures. As shown in , The compound 4-methyl-1-(4-sulfobutyl)quinolonium () was prepared by alkylation reaction. Compounds and were synthesized by substitution reactions between 4-fluorobenzaldehyde and , , '-trimethylethanedi
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To understand the impact of alterations
2022-04-19

To understand the impact of alterations in neurokinin 1 receptor zinc homeostasis, the role of Zn2+ as a neurotransmitter has to be appreciated. Certain regions of the brain including the neocortex and hippocampus harbour so-called “zincergic” (or “gluzinergic”) neurons, where Zn2+ is co-released wi
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The recent identification of new mechanisms for triggering f
2022-04-19

The recent identification of new mechanisms for triggering ferroptosis, by compounds termed FIN56 and FINO2, provided new insights into regulation of ferroptosis. FINO2 acts through a distinct mechanism: it promotes lipid peroxidation by oxidizing iron and indirectly inactivating GPX4 [180]. FIN56 w
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It raises a question about origin of
2022-04-19

It raises a question about origin of the sensitivity to Ca of both FBPase isozymes. Was the ancestral vertebrate FBPase inhibited by calcium similarly to the liver isozyme? And is the high sensitivity of FBP2 a new evolutionary feature of warm-blooded vertebrates? Additionally, since subcellular lo
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Neither E nor Z FPP
2022-04-19

Neither E- nor Z-FPP synthase catalyzed the reaction between 8-THPOGPP and IPP. However, a mutant E-FPP synthase (Y81S) produced 12-THPOFPP from the substrates 8-THPOGPP and IPP, and wild-type E-FPP synthase catalyzed the reaction betweeen 8-AcOGPP and IPP producing 12-AcOFPP. Mutant E-FPP synthase
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br Materials and methods br Results br Conclusions In
2022-04-19

Materials and methods Results Conclusions In general, the drug design process is very laborious, expensive and prone to errors. Various computational methods including docking and algorithms based on molecular dynamics and/or quantum chemistry can help considerably at the early stage of str
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Compound a substituted phenyl H
2022-04-19

Compound 6, a 5-(4-substituted-phenyl)-5H-pyrano[2,3-d:-6,5-d′]dipyrimidine derivative was invented previously to have significant efficacy to inhibit HIV integrase enzyme with 0.9 ± 0.4 μM of IC50 against 3′-processing and 16.1 ± 10.7 μM of IC50 against strand transfer suppression. The compound ind
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Genome wide binding and transcriptome analyses demonstrate t
2022-04-19

Genome-wide binding and transcriptome analyses demonstrate that Fbxl10 directly binds the Areg, Mdk, Lmnb1, Thbs1, Mgp and Cxcl12 locus and thereby might influences the expression of these migration associated genes. The expression of epidermal growth factor (EGF)-like molecule Amphiregulin (Areg)
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Based on the in vitro findings summarized here we
2022-04-19

Based on the in vitro findings summarized here, we posited that, in the intact brain, release of ROS from iron-laden astrocytes to the local neuropil elicits oxidative damage and degeneration of indigent dopaminergic projections and other vulnerable neuronal elements (Schipper, 2001). Of particular
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HBV is an enveloped double stranded DNA virus which is
2022-04-19

HBV is an enveloped, double-stranded DNA virus, which is transcripted into four major transcripts [6]. Among them, the 3.5 kb pregenomic RNA (pgRNA) directs the translation of HBV polymerase, core protein and acts as template for reverse transcription. So viral transcription is a key step of virus l
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PBI is an agonist of GPR and acts
2022-04-18

PBI-4050 is an agonist of GPR40 and acts as an antagonist or inverse agonist of GPR84. It cannot be excluded that other targets besides GPR40 and GPR84 could be implicated in the mechanism of action of PBI-4050 and could be explored in future studies. However, the present study, and in particular th
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While the specific set of
2022-04-18

While the specific set of challenges associated with deorphanization and transforming each poorly characterized GPCR into a useful drug target will be unique, much can be learned by considering how these issues have been addressed for other receptors. One group of poorly characterized GPCRs that hav
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Human GPR hGPR was originally isolated in as
2022-04-18

Human GPR55 (hGPR55) was originally isolated in 1999 as an orphan GPCR with high levels of expression in human striatum (Sawzdargo et al., 1999) (Genbank accession # NM_005683.3). hGPR55 was mapped to human chromosome 2q37, and in the human CNS it is predominantly localized to the caudate, putamen,
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Introduction Non alcoholic hepatic steatosis is characterize
2022-04-18

Introduction Non-alcoholic hepatic steatosis is characterized by the presence of steatosis in hepatocytes [1], which leads to the development of fatty liver [2]. It is strongly associated with obesity, insulin resistance, and type II diabetes [3]. They are major risk factors of non-alcoholic hepati
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In this study three potential Otx binding sites
2022-04-18

In this study, three potential Otx-2 IL-2, human recombinant sale were found in the promoter region of the sheep GnRH gene: −1786 bp to −1770 bp, −825 bp to −819 bp, and − 529 bp to −523 bp. Combined with the results of the double-luciferase assay, it could be inferred that the binding site of Otx-
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