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CYP A is involved in the
2021-05-13
CYP3A is involved in the metabolism of approximately 50% of all drugs that are currently prescribed to patients [1], [15], [16]. Marked interindividual variabilitity of the catalytic function for metabolizing CYP3A substrates has been demonstrated with variability exceeding 20-fold [1]. Levonorgestr
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Substitutions on the benzene ring of
2021-05-13
Substitutions on the benzene ring of the phenyl acetic LY3039478 moiety were evaluated to study their effect on DP and CRTH2 selectivity (). Compound has strong affinity for CRTH2, but it only has moderate affinity for DP. Small substitutions such as methoxy () and fluorine () next to the aryloxy
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br Material and methods br Discussion First
2021-05-13
Material and methods Discussion First, we investigated cannabis use, and results showed that the lifetime prevalence of cannabis use in our sample was 29.63%, with a significant difference between males (73.8% of the abusers) and females (26.2%). Moreover, the mean age and age at onset were si
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Protein kinase casein kinase CK comprises a family of
2021-05-13
Protein kinase casein kinase 1 (CK1) comprises a family of highly related, constitutively active serine/threonine protein kinases (reviewed by [15]). CK1 is involved in controlling a wide variety of different cellular events including protein turnover [16], [17], nuclear import [18] and the cellular
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br Materials and methods br Results br Discussion Persimmon
2021-05-13
Materials and methods Results Discussion Persimmon tannin has been reported to have the bile acid binding ability in vitro (Matsumoto et al., 2011) and hypolipidaemic effects in animals (Matsumoto et al, 2008, Zou et al, 2012). Our previous study also proved that persimmon tannin promoted t
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Spinal cord injury leads to
2021-05-13
Spinal cord injury leads to an extensive inflammatory cascade on spinal cord and the release of pro-inflammatory cytokines can sensitize neurons, activating signaling pathways that will result in thermal and mechanical hypersensitivity [39]. In this regard, Guo and collaborators (2014) demonstrated
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In most cases the ligand affinity between
2021-05-13
In most cases, the ligand affinity between subtypes is similar, but their tissue distribution is different. In the case of the estrogen receptors (ER), two subtypes (ERα and ERβ) exist (Kuiper et al., 1996) and ERβ has several isoforms, designated ERβ1–5 (Moore et al., 1998) or ERβcx (Ogawa et al.,
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Although the mechanisms underlying the EP mediated
2021-05-13
Although the mechanisms underlying the EP4-mediated increase in the frequency of mEPSCs via PGE2 remain unclear, mechanisms similar to those driven by EP2 may be involved because activation of both these receptor subtypes increases the intracellular concentration of cAMP (Nishigaki et al., 1995, Sug
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br Materials and methods br Results discussion br Conclusion
2021-05-12
Materials and methods Results + discussion Conclusions We have demonstrated the systematic optimization of the functional folding of a CF synthesized GPCR. The approach addresses central issues relevant for many membrane proteins such as disulfide bridge formation, proper hydrophobic enviro
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The isomeric phenyloxazole not only exhibited increased
2021-05-12
The isomeric 5-phenyloxazole not only exhibited increased potency against NEP, but also a decreased ACE inhibition thus providing encouraging selectivity. Changing the P1 group from an -propyl to a more polar methoxyethyl at the left hand Imiloxan hydrochloride (as seen in compound pairs – and –)
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er alpha Immunomodulation effects of certain oxysterols were
2021-05-12
Immunomodulation effects of certain oxysterols were previously shown to depend on activation of oxysterol-binding liver X receptors (LXRs). Recent work from our labs as well as from others has shown additional receptors linking oxysterols and immunity. For example, we found that 7α,25-dihydroxychole
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The molecular mechanisms regulating the differentiation of T
2021-05-12
The molecular mechanisms regulating the differentiation of Th1 versus Tfh Donepezil HCl from IL-12-stimulated CD4+ T cells remain largely uncharacterized in humans. This topic has been extensively studied in mice (Weinmann, 2014), because IL-12 stimulation promotes mouse naive CD4+ T cells to expre
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br Conclusion br Conflict of interest br Author contribution
2021-05-12
Conclusion Conflict of interest Author contributions Acknowledgements Piyamas Kanokwongnuwut was supported by the Development and Promotion of Science and Technology Talent Project (DPST), Royal Thai Government Scholarship. Funding for the work was provided by the Attorney General’s Depa
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The unique property of mutant IDH in producing an
2021-05-12
The unique property of mutant IDH1/2 in producing an oncometabolite that has no known physiological function makes mutant IDH enzymes as obvious potential therapeutic targets for the treatment of IDH-mutated tumors (Rohle et al., 2013, Wang et al., 2013). Clinical studies have also suggested the pre
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Resistance to SP is linked to point mutations that
2021-05-12
Resistance to SP is linked to point mutations that accumulate at several sites in the dihydrofolate reductase (dhfr) and dihydropteroate synthase (dhps) BAY 41-2272 of P. falciparum (Roper et al., 2003). These mutations have been identified in codons 16, 51, 59, 108, and 164 in the dhfr gene and co
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