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Having identified initial leads and further lead
2021-12-02

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 Actinonin derivatives – and () were evaluated for GSNOR potency. Among this, fluoro, methyl, chlor
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Finally a potentially effective therapeutic approach is to t
2021-12-02

Finally, a potentially effective therapeutic approach is to target the LDH enzymes that mediate bidirectional conversion of pyruvate into lactate. In particular, because LDHA is the predominant isoform expressed in glycolytic tumours, an array of LDHA-targeting compounds have been proposed and valid
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Several studies have sought a cross
2021-12-02

Several studies have sought a cross-relationship between commensal bacteria-derived metabolites and the Gprs (Blad et al., 2012). Gpr81 is expressed primarily in adipocytes, and hence, lactate-Gpr81 interaction inhibits lipolysis (Cai et al., 2008, Liu et al., 2009). Lactate reduced inflammation by
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T7 High Yield RNA Hepcidin expression was not affected
2021-12-02

Hepcidin expression was not affected under GlyT1 inhibition. Hepcidin downregulation is well documented in conditions of ineffective erythropoiesis and dyserythropoietic anemias, including sideroblastic anemia 33, 34. Systemic iron acquisition under these types of anemia is obviously independent fro
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AFB Fapy dG has been long recognized as a
2021-12-02

AFB1-Fapy-dG has been long recognized as a substrate for nucleotide excision repair [24,25]. However, we recently demonstrated that this lesion is removed by Heme Colorimetric Assay Kit synthesis excision repair. We showed that DNA glycosylase NEIL1, a member of the Fpg/Nei glycosylase family, coul
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br Conflict of interest br Acknowledgements br Introduction
2021-12-01

Conflict of interest Acknowledgements Introduction Second generation antipsychotic drugs (SGAs) such as olanzapine are widely used in treating individuals with schizophrenia and bi-polar disorder and are increasingly prescribed for other conditions such as anxiety (Pringsheim and Gardner, 2
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We found that silymarin induced more improvement
2021-12-01

We found that silymarin induced more improvement of renal functions compared to Rvs. Our results were in agreement with previous studies. The effect of silymarin has been tested in alloxan-induced diabetes mellitus models in rats. Alloxan produces reactive oxygen species which injure renal tissue. S
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br Conclusion br Author contributions br Ethics approval
2021-12-01

Conclusion Author contributions Ethics approval Competing interests Introduction VHL is a well-known tumor suppressor and works as a target recruitment subunit of an E3 ubiquitin ligase complex that recruits hydroxylated hypoxia inducible factor α (HIF-α) for proteasomal degradation u
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The glycolytic activator phosphofructo kinase fructose bisph
2021-12-01

The glycolytic activator 6-phosphofructo-2-kinase/fructose 2,6-bisphosphatase 3 (PFKFB3) is well-known as a downstream substrate of hypoxia-inducible factor 1α (HIF-1α) signaling pathway [5,6]. Tumor hypoxia has long been associated with increased malignancy, poor prognosis and drug resistance. HIF-
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The haspin gene is also unusual because it
2021-12-01

The haspin gene is also unusual because it lacks introns. This is more remarkable when one compares the mammalian genes to those of likely haspin orthologs that are present in the genomic sequences of other species. Such genes in Drosophilamelagonaster, Arabidopsisthaliana and Caenorhabditiselegans
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Trimidox australia Aspartame l aspartyl l phenylalanine meth
2021-12-01

Aspartame (l-aspartyl l-phenylalanine methylester) is a dipeptide artificial sweetener that is widely used as a non-nutritive sweetener in various food products [1]. The increased market of dietary products and the development of new synthetic sweetening compounds have not been sufficiently explored
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br Materials and methods br Results
2021-12-01

Materials and methods Results Discussion An HMC is a blinding type of cataract frequently observed in Asian countries due to the appallingly high incidence of high myopia in those areas [4], [5] and typically features earlier onset and more rapid progression of nuclear cataract [1], [2]. Th
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The saturated carbocyclic derivatives pyrazoles M and
2021-12-01

The saturated carbocyclic derivatives, pyrazoles (2.5μM and 5.2μM) and (9.0μM and 2.5μM), provided little improvement in potency when compared to the linear alkyl derivatives, whereas the C5-phenyl derivative (0.31μM and 0.43μM) showed promise as a scaffold for further structural modifications.
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Recently higher grade varicoceles have been reported to be
2021-12-01

Recently, higher-grade varicoceles have been reported to be associated with higher nocturia levels [20], and we observed an interesting phenomenon in which the urine volume/water intake ratio dramatically increased in the rat model of experimental left varicocele (ELV); the decreases in hypothalamic
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Next we investigated the accumulation of H ribavirin
2021-11-30

Next, we investigated the accumulation of [3H]-ribavirin in fresh villous fragments of human placenta, which provide a physiologically relevant, well-described and validated model for assessing drug interactions with ENTs [32], [35], [69], [70]. The uptake of [3H]-ribavirin was time-dependent and si
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