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During the course of our research on mGlu PAMs
2020-05-27
During the course of our research on mGlu PAMs,, the hydroxyacetophenone scaffold was found to possess dual mGlu PAM and CysLT1 antagonism activity, presumably as orthosteric antagonist (). There is currently an increasing interest in drug discovery to explore multitarget drugs or polypharmacology
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Taking into account that a PFOS inhibits CRF
2020-05-27
Taking into account that: (a) PFOS inhibits CRF gene expression as well as CRF and corticosterone secretion (Pereiro et al., 2014); (b) CRF1r mediates the stimulation of the pituitary ACTH secretion by this neuropeptide (Rivier et al., 2003); (c) corticosterone regulates its own synthesis by a negat
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Accurate equilibrium predictions of CO containing mixtures
2020-05-27
Accurate equilibrium predictions of CO2 containing mixtures, however, are challenging with traditional equations of state. The reason for this may be that CO2 has a large quadrupole moment. The large quadrupole moment of CO2, as well as size asymmetry, are for instance believed to be the reasons for
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br Introduction Abdominal aortic aneurysm AAA is
2020-05-26
Introduction Abdominal aortic aneurysm (AAA) is a daily concern in vascular surgery, as successful treatment is exclusively achieved by open or endovascular repair. Its prevalence is 2–11% among male smokers, and rupture the major complication, is associated with unacceptably high morbidity and m
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br Materials and methods br Results
2020-05-26
Materials and methods Results Discussion UPP components including the proteasome, E1s, E2s, E3s and DUBs may become one the most important Fidaxomicin of therapeutic targets for the pharmaceutical industry in the near future and supersede those which are involved in the phosphorylation sys
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It has been reported about
2020-05-26
It has been reported about the synthesis of benzyl bromide in our previous reports, as shown in , , The synthetic route of compounds – is depicted in , Briefly, the synthesis of pyrimidinedione derivatives was started from commercially available gamma secretase inhibitors . After alkylation of ma
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Approximately of the etamicastat dose was recovered in urine
2020-05-26
Approximately 50% of the etamicastat dose was recovered in urine, 30% in the form of etamicastat and 20% in the form of BIA 5-961. These data agree with those from a study with [14C]-labeled etamicastat in healthy subjects, which showed that approximately 95% of the administered radioactivity had be
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br Significance Dysregulation of dopamine
2020-05-26
Significance Dysregulation of dopamine homeostasis contributes to Parkinson\'s disease (PD). The nuclear receptor Nurr1 plays a central role in dopamine homeostasis, regulating the transcription of Ginkgolic Acid C15:1 governing the synthesis, packaging, and reuptake of dopamine. Efforts to capit
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br Conclusion br Conflict of
2020-05-26
Conclusion Conflict of interest Acknowledgment The authors acknowledge the grant support of the Tehran University of Medical Sciences (94-02-49-29647). Introduction Earlier in vitro observations have also established that the human 5-HT2A, while very similar to the rat isoform, exhibits
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Herein we designed a strategy
2020-05-26
Herein, we designed a strategy utilizing the target-protection method to produce a signal in a system involving fluorescence CuNPs stabilized by dumbbell template DNA (DT DNA) through a locked circle consisting of two poly T loops and a poly (ATTA) stem. In the presence of MTase, DT DNA was modified
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ATP dependent DNA ligases in vertebrates are divided in
2020-05-26
ATP-dependent DNA ligases in vertebrates are divided in three families [7]. Family I DNA ligases are responsible for sealing the nicks during DNA replication and in long-patch base excision repair (BER). Family III DNA ligases are involved in short-patch BER. Lastly, family IV DNA ligases are involv
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Substituents at the C position
2020-05-26
Substituents at the C11 position — An oxygen-containing substituent at the C11 position also affects the catalytic activity of Δ1-KSTDs. The Δ1-KSTDs from the Gram-positive bacteria R. equi [29], N. simplex ATCC 6946 and IFO 12069 [48,49,52], and R. rhodochrous IFO 3338 [27] were able to 1(2)-dehydr
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br Materials and methods br Results br Discussion To our
2020-05-26
Materials and methods Results Discussion To our knowledge, this is the first large-scale longitudinal measurement of more than 20 cytokines in normal pregnancy. Simultaneous measurements of several cytokines with multiplex magnetic bead-based immunoassays are becoming increasingly common in
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Introduction Cytochrome P CYP A is the most important enzyme
2020-05-26
Introduction Cytochrome P450 (CYP)3A is the most important enzyme involved in the metabolism of 30–40% of currently prescribed drugs [1]. The CTPB level and activity of CYP3A show large intra- and inter-individual variability, which contributes to unpredictable drug response and toxicity. A multit
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The ability of TKIs in inducing CRTH expression could be
2020-05-26
The ability of TKIs in inducing CRTH2 expression could be related to the c-terminal of CRTH2 receptor that is important molecular determinant in the down-stream signaling cascade activation [20]. This requires further studies to prove it or disprove it. Additionally, further studies are needed to ex
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