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The allosteric site of class C receptors
2024-10-31
The allosteric site of class C receptors is generally located on the extracellular side of the TM domain (Brauner-Osborne et al., 2007, Christopher et al., 2015, Dore et al., 2014, Gregory et al., 2011, Harpsoe et al., 2017, Kniazeff et al., 2011, Pin and Prezeau, 2007, Urwyler, 2011, Wu et al., 201
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Phenolic compounds show reciprocal relationship with
2024-10-30
Phenolic compounds show reciprocal relationship with colonic microflora. Phenolic compounds are able to improve colonic health and modulate microbiota diversity with prebiotic and antimicrobial functions, while colonic bacterial enzymes catalyze deconjugation, dehydroxylation, and convert phenolic c
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While we chose to divide
2024-10-30
While we chose to divide our etiologies into three categories, it should be noted that such division has certain limitations. Even though URIs and the common cold are considered mainly viral in origin and rhinosinusitis mainly bacterial in origin,26, 27 there is considerable overlap between these co
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The association of male gender with increased atherosclerosi
2024-10-30
The association of male gender with increased atherosclerosis has stimulated interest in the role of androgen signalling in this condition. Androgens act (Fig. 2) by direct activation of androgen receptor (AR), a nuclear receptor that acts as a ligand-regulated transcription factor (Gao et al., 2005
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br Author contributions br Financial disclosures br
2024-10-30
Author contributions Financial disclosures Acknowledgements We thank Ms. Eva So for the editorial assistance. This work was supported by grants from the National Natural Science Foundation of China (No. 81622015, 81571042 and 81501143) and the National Basic Research Program of China (No. 2
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ERAP has been crystallized in two
2024-10-30
ERAP1 has been crystallized in two different conformations, wherein the C-terminal domain IV is either closely interacting with domains I/II and enclosing the active site (termed ‘closed’), or is rotated away in a hinge motion which exposes the active site (‘open’). This large motion correlates with
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Clinical observations of individuals with a decrease in LOX
2024-10-30
Clinical observations of individuals with a decrease in 12-LOX CGP 35348 are consistent with 12-LOX potentiating platelet activation and thrombus formation [40]. However, the relative contribution of 12-LOX to these complex disorders cannot be fully elucidated in the absence of a biochemical assess
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Nrf br AhR br Nrf and AhR friends or foes
2024-10-30
Nrf2 AhR Nrf2 and AhR: friends or foes for energetic metabolism? Perspectives in carcinogenesis upon xenobiotic exposure Acknowledgements Introduction Integration of endogenous and exogenous signals via appropriate receptors is at the core of biological differentiation and adaptive r
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The only psychostimulant treatment option in Turkey
2024-10-30
The only psychostimulant treatment option in Turkey is methylphenidate (Çetin et al., 2015). It is broken down by carboxylase enzyme (CES1) (Sun et al., 2004). From the point of pharmacokinetics, it may be suggested that CES1 gene polymorphisms may be the key responsible factors in patients resistan
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Since the cloning of ARs in the beginning
2024-10-30
Since the cloning of ARs in the beginning of the 1990s, the efforts to characterize them have led to the accumulation of a substantial amount of experimental data. Decades of site-directed mutagenesis (SDM; Box 1) studies, in combination with pharmacological data and computational modeling, have pav
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Encouraged by this observation a systematic SAR
2024-10-30
Encouraged by this observation, a systematic SAR study on the A ring -alkoxy was conducted as summarized in . The A ring methoxy-containing KRCA-0008 was proven an optimal substituent in terms of potency after all and its bigger size derivatives were detrimental in both biochemical and H3122 cellula
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There is also a literature on the impact
2024-10-29
There is also a literature on the impact of commodity (consumption) taxation under imperfect competition. Besley (1989) applies a Cournot model, in which production takes place under IRS and in which free entry leads to an excessive number of firms in the market. Introducing a distortive specific co
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Conclusion Twenty compounds with dinitrobenzoate scaffold we
2024-10-29
Conclusion Twenty compounds with 3,5-dinitrobenzoate scaffold were synthesized and evaluated using cell-free and HWB assays for their 5-LOX inhibition activities. Compared to the parent compound, six compounds show significantly increased enzyme inhibition activities. The best compound, 3-tolyl 3,5
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br Conclusion To conclude it would be
2024-10-29
Conclusion To conclude, it would be fair to say that the research efforts on FLAP inhibitors for intervening with LT biosynthesis have reached to a considerably advanced state during the last decade as a result of growing interest from both pharmaceutical industry and academia [4], [37], [38]. Du
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The present study has several limitations First the results
2024-10-29
The present study has several limitations. First, the results were obtained using RAW264.7 cells, which are derived from BALB/c mice infected with the Abelson leukemia virus (Raschke et al., 1978). However, these cells, which are a commonly used mouse macrophage cell line, show properties similar to
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