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The first and the best characterized mechanism of receptor d
2023-04-17
The first and the best-characterized mechanism of receptor-dependent internalization of Aβ is mediated via the α7-nicotinic MDL800 receptor [82]. Lipoprotein receptor protein represents the second best-studied route that facilitates the uptake of Aβ by neurons, involving additional molecules such as
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A central question that arises
2023-04-17
A central question that arises in this discussion is whether enhanced neurobehavioral responses to food cues emerge as a consequence of weight gain, or whether there are intrinsic differences in the motivational responses to food cues that precede weight gain. In support of pre-existing differences,
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Due to metabolic variations it is important to consider
2023-04-17
Due to metabolic variations, it is important to consider arginine metabolism and dependency in specific contexts to identify precise patterns. This is best illustrated for ASS: while ASS deficiency correlates with worse prognosis in sarcomas, ASS levels positively correlate with a poor prognosis in
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Overexpression of AR in a transgenic mouse model leads
2023-04-17
Overexpression of AR in a transgenic mouse model leads to a capsular cataract phenotype involving proliferation and formation of a fibrotic plaque of cells reminiscent of cells at the posterior lpa receptor in PCO [17]. To investigate the molecular mechanism that could link AR expression to this ph
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The present study determined the effect
2023-04-17
The present study determined the effect of DCA on VSMC calcification in vitro and in atherosclerotic ApoE-/- mice in vivo. We found that Lidocaine non-toxic concentrations of DCA, did not affect VSMC viability, induced calcification of VSMC in culture and increased atherosclerotic vascular calcific
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In recent years there have been further significant developm
2023-04-17
In recent years, there have been further significant developments that enhance an understanding of the role of adenosine in nociception. Thus, novel methods of recruiting adenosine A1Rs have been developed, and the role of adenosine A2A- and A3Rs in nociception has been further elaborated. Furthermo
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Tacrine an aminoacridine derivative Fig A was the first
2023-04-17
Tacrine, an aminoacridine derivative (Fig. 1, A), was the first AChE inhibitor approved for treatment of AD [12], [13]. This compound was withdrawn from the market due to its hepatotoxicity [14]. In spite of tacrine's side effects, it is still an attractive lead compound for medicinal chemists due t
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Because LTs are proved to mediate
2023-04-17
Because LTs are proved to mediate multiple biological and pathological responses in various disease states, the 5-LO biosynthetic pathway producing LTs from AA have been the target of drug discovery efforts for over two decades. As observed from literature, a pile of research efforts has been direct
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Song et al reported series of triazolylsalicylamide derivati
2023-04-17
Song et al. reported series of 1,2,3-triazolylsalicylamide derivatives and screened over kinase panel and found compound 31 as most potent which inhibited Aurora-A, specifically with IC50 of 0.37 μM. Compound 31 was about 10-fold more active for Aurora-A than for Aurora-B (IC50 = 3.58 μM reported se
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The evidence points toward a role for LO activity
2023-04-17
The evidence points toward a role for 12/15-LO activity in WAT in modulating chronic local inflammation and subsequent systemic metabolic decline in the obese state. However, little is known as to the role of 12- and 15-LOs in BAT. Indeed, in addition to WAT, platelet- and leukocyte-type 12-LO are e
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Receptors containing an x y subunit interface where x
2023-04-17
Receptors containing an αx/γy subunit interface, where x=1, 2, 3, 5 and y=1–3, form a high-affinity binding site for benzodiazepines (Figure 1A), for the later developed Z-drugs of different chemotypes, and for a large number of chemically distinct research compounds 17, 18 (Box 1 for examples). For
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Moreover mice exposed to high
2023-04-14
Moreover, mice exposed to high-cholesterol diet have mildly activated astrocytes, increased expression of ApoE and aquaporin-4 in the hippocampus, and altered levels of proteins associated with Aβ metabolism (Chen et al., 2016), which is related to a higher demand for cholesterol transport and the n
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ADOR immunoreactivity was high in parasympathetically innerv
2023-04-14
ADOR immunoreactivity was high in parasympathetically-innervated smooth muscle, namely the iris sphincter muscle and the ciliary muscle. No ADOR immunoreactivity was noted in the sympathetically-innervated iris dilator muscle. Immunoreactivity against all four ADORs was noted in the ciliary epitheli
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br Acknowledgements MC and PD were funded by the
2023-04-14
Acknowledgements MC and PD were funded by the Michael J Fox Foundation (Grant ID 9969). We would like to thank Pierluigi Saba, Francesco Traccis and Barbara Tuveri for their technical assistance. Introduction In the prostate, androgens play a crucial role in normal, BPH and cancerous growth b
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During myeloid cell maturation expression of
2023-04-14
During myeloid cell maturation, expression of 5-LO mRNA and protein is strongly induced (60–130-fold) by calcitriol (1,25(OH)2D3) and transforming growth factor-β (TGFβ) [6,7]. The upregulation of 5-LO mRNA transcription is mainly due to transcript elongation and mRNA maturation [8,9]. Interestingly
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