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br AD and COX LOX pharmacology Early studies on the
2023-02-01
AD and COX/5-LOX pharmacology Early studies on the role of cyclooxygenases in AD were inspired by epidemiological data suggesting that COX inhibitors such as nonsteroidal anti-inflammatory drugs (NSAIDs) could be beneficial in AD patients (Lucca et al., 1994, McGeer et al., 1990). This line of re
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Another significant group of reductase inhibitors is the ste
2023-02-01
Another significant group of 5α-reductase inhibitors is the steroidal 3-carboxylic biotin-LC-LC-tyramide derivatives (relevant examples in Fig. 5), which were designed to mimic the putative enzyme-bound enolate intermediate. This was achieved by introducing sp2-hybridized centers at C3 and C4 and a
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Over the past decade extensive research has
2023-02-01
Over the past decade, extensive research has been directed toward the discovery of Aurora-selective small-molecule inhibitors. As a result, a handful of Aurora inhibitors has been identified. Among them, 1 (VX-680) and 2 (SNS-314) have entered human clinical trials as pan-Aurora kinase inhibitors (F
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It has been well established that shortly
2023-01-31
It has been well established that shortly after systemic inflammation, NADPH oxidase and iNOS activity were increased in the Fungicidin and lead to overproduction of reactive oxygen species (ROS) and NO [66]. Moreover, previous studies indicated that Ang II induced an increased level of NADPH oxidas
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Inhibition of autophagy has been
2023-01-31
Inhibition of autophagy has been shown to alleviate neuronal damage after cerebral ischemia, both in cell culture and rodent models (Koike et al., 2008, Li et al., 2015, Wang et al., 2016, Zhang et al., 2014, Zheng et al., 2014). Therefore, blockage of autophagy is a potential target for prevention
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br Pathophysiology of Alzheimer disease
2023-01-31
Pathophysiology of Alzheimer disease Alzheimer disease is characterized by severe neurodegeneration, neuroinflammation, and progressive loss of cognitive abilities. The diagnostic criteria for dementia released by the National Institute on Aging-Alzheimer's Association define dementia as the deve
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A straightforward synthetic pathway was adopted to
2023-01-31
A straightforward synthetic pathway was adopted to synthesize the target compounds as outlined in . The starting chloromethylquinazolinones (–) were synthesized from anthranilic mps1 kinase in two steps following reported procedures., , , The first step involves chloroacetylation of anthranilic ac
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To our knowledge BAY has not
2023-01-31
To our knowledge, BAY 60-6583 has not progressed to clinical development and remains to be the only ADORA2B agonist that has been developed.33, 34 Further development of similar compounds would be beneficial in future fibrosis research. One of the limitations of our study is being limited to in vit
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br Conclusions The present data suggest
2023-01-31
Conclusions The present data suggest that homeostatic balance of the cortical/hippocampal adenosinergic tone is necessary for normal working memory function and any deviation appears to impair performance – either as a consequence of A2AR under-activation when adenosine levels are reduced or due
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Although the role of apelin and APJ receptor
2023-01-30
Although the role of apelin and APJ receptor in cardiovascular functions has been well-elucidated, little is known for the effect of the central apelinergic system on gastrointestinal (GI) functions. In mice, it has been found previously that central exogenous apelin-13 decreased gastric emptying (G
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Based upon these findings the S
2023-01-30
Based upon these findings, the 12S-lipoxygenase seems to increase membrane excitability by specifically inhibiting M-type K+ channels. The 12S-lipoxygenase is expressed in many parts of mammalian Amyloid Beta-Peptide (1-40) including the cerebrum, cerebellum, hypothalamus, basal ganglia, hippocampus
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br Conclusion br Conflict of
2023-01-30
Conclusion Conflict of interest Acknowledgements Introduction Human salivary aldehyde dehydrogenase (hsALDH) (E.C. 1.2.1.5) is the first line of defence against toxic aldehydes in the oral cavity. HsALDH is primarily a dimeric, class 3 ALDH (ALDH3A1) specific for aromatic and long/medium
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Atypically BcALDH has a minor reducing activity
2023-01-30
Atypically, BcALDH has a minor reducing activity for all-trans-retinal, which requires the binding of the reduced form of the NADP+ (NADPH) cofactor that is a side-product of the canonical oxidation activity of BcALDH. The reduction activity that converts all-trans-retinal to all-trans-retinol was r
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PC is considered as a cancer of
2023-01-30
PC is considered as a cancer of the epigenome (Grasso et al., 2012, Robinson et al., 2015). Our results demonstrate that the interaction of AR with ACK1 drives the positive feedback epigenetic circuitry that is ultimately conducive to promote AR transcription. Further, this circuitry subjugates AR t
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br Results br Discussion Autophagy is considered as
2023-01-30
Results Discussion Autophagy is considered as an important process in physiological and pathological ovarian function. It is related mainly to follicular atresia and CL regression (for review see [20]). However, an involvement in luteal cell survival is also proposed [21], [22]. The present st
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