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Several highly potent CysLT receptor antagonists with large
2021-08-09

Several highly potent CysLT1 receptor antagonists with large structural β-Tocotrienol have been developed. Beyond antagonists with structures analogous to cysteinyl leukotrienes, other subclasses comprise: (a) hydroxyacetophenones, (b) indoles and indazoles, (c) quinolines, benzothiazoles, and thia
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Naringenin is the one of
2021-08-09

Naringenin is the one of the many components in grapefruit juice. It was assumed that administration of 20mL grapefruit juice per kilogram of body weight is completely glucuronidated in the hepatic or gut wall for first pass metabolism [38]. It has been detected that one liter of grapefruit juice co
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As compared with the broad
2021-08-09

As compared with the broad spectrum of chemicals known to serve as the ligands for PXR and CAR, the ligands of VDR are previously restricted to VD3 as well as its hydroxylated metabolites and the secondary bile eg5 LCA. Recently, the VDR-binding capacities of more compounds have been discovered, wh
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br Financial Support We would like to
2021-08-09

Financial Support We would like to acknowledge financial support by the National Natural Science Foundation of China (grant numbers 81672778 and 81372165) and Natural Science Foundation of Beijing Municipality (grant number 5142009). Acknowledgements Introduction The process of spermatogen
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Another option is to use the thiol groups
2021-08-09

Another option is to use the thiol groups of cysteine residues, which can be modified by use of PEG-maleimide and vinyl sulfone. However, changes in PEGylation interactions or reaction conditions can result in changes in the functional properties of the therapeutic proteins [[50], [51], [52]]. A st
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MAPK Inhibitor Library The crystal structure of LiCoO is pre
2021-08-09

The crystal structure of LiCoO2 is presented in Fig. 1. We can notice that the Li and Co atoms occupy the centers of two different edge-sharing [CoO6]-octahedra, which results in formation of separate Li and Co layers. Hence, the layered structure of LiMO2 is able to intercalate lithium into transit
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Several highly selective COX inhibitors coxibs have
2021-08-09

Several highly selective COX-2 inhibitors (coxibs) have been reported and marketed [6], including celecoxib [7] and etoricoxib [8] (Fig. 1). Even though these drugs produce less ulceration than conventional NSAIDs, coxibs still produce significant gastric and cardiovascular side effects due to the d
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The two SNPs rs rs
2021-08-09

The two SNPs rs4818-rs4680 presented above are part of the haploblock (rs6269, rs4633, rs4818, rs4680) presenting the 3 major haplotypes which influence the enzymatic activity of COMT. This activity is inversely related to the sensitivity of pain in a chronic pain syndrome; so the haplotype (GCGG) h
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No orthologs could be found in our
2021-08-09

No orthologs could be found in our B. oleracea BAC library for AtCk1/2, which could mean that it is unique to Arabidopsis, or that we failed to detect it in our library. However, the second possibility is unlikely considering that Southern blotting analysis with four restriction enzymes disclosed fr
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Not all of the biological activities exhibited by progestoge
2021-08-09

Not all of the biological activities exhibited by progestogens (Table 1) are mediated via binding to SRs. For example, the anti-estrogenic action of progestogens in the tazemetostat is due to the progestogen-bound PR suppressing ER gene expression, and consequently the ability of the cell to respond
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Bioinformatics analysis for genes encoding proteins ESR
2021-08-09

Bioinformatics analysis for genes encoding proteins (ESR1, IL6, TERT, DNMT3B) showed that NF-kB is one of the transcription factors that might be regulating their expression, especially for IL6, TERT and DNMT3B genes. Previous studies have demonstrated that PA induces NF-kB activation, thus increasi
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Formoterol Hemifumarate In our former work our interest was
2021-08-06

In our former work, our interest was in discovery of novel VEGFR-2 inhibitors as anti-angiogenesis agents. Along this line, with natural alkaloid taspine as the lead compound, rounds of structure optimization were performed to develop novel VEGFR-2 inhibitors [[13], [14], [15]]. Among them, BPS-7, b
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In conclusion we designed novel E inhibitors based on
2021-08-06

In conclusion, we designed novel E1 inhibitors based on the three-dimensional structure of E1 in complex with ubiquitin. Following an enzymatic assay evaluating synthetic compounds , , and , we identified compound as a novel E1 inhibitor. Comparing the inhibitory activity of compound with and ,
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The liposomes as a FDA approved drug
2021-08-06

The liposomes, as a FDA-approved drug delivery carrier, have been widely utilized for drug delivery [32], [33], [34]. Liposomes are defined as self-assembled vesicles, which are composed of one or multiple concentric lipid bilayers and enclose an aqueous core. The advantages of utilizing liposomes a
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The glycolytic pathway is a catabolic route that ends
2021-08-06

The glycolytic pathway is a catabolic route that ends with the synthesis of pyruvate (Pyr). In Arabidopsis embryos, the conversion of phosphoenolpyruvate (PEP) to Pyr, catalyzed by pyruvate kinase (PK), is mainly located in the plastids [10], [11]. The preceding reaction is catalyzed by enolase (ENO
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