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Imaging QTL studies may have several
2024-11-23

Imaging QTL studies may have several potential advantages over case-control studies, including increased power . Imaging endophenotypes of disease in QTL studies can separate patients and normal subjects more accurately and therefore limit the confound of including asymptomatic subjects in the contr
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Lorlatinib is an orally active brain penetrant cyclic
2024-11-23

Lorlatinib is an orally active brain penetrant cyclic 2-aminopyridine derivative that is a type I½ B ALK inhibitor (Fig. 5F) [61]. This medicinal is an effective antagonist against the more common L1196M and G1269A crizotinib-resistant mutations as well as the less common T1151Ins, L1152R, C1156Y, F
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APPL is highly expressed in pancreatic cells but its
2024-11-22

APPL1 is highly expressed in pancreatic β cells, but its levels are significantly decreased in several mouse models of obesity and diabetes, including HFD-induced obese mice and db/db mice [6], [73], suggesting that the dysregulation of APPL1 may be associated with malfunction of the pancreas in obe
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The most widely recognized effects of adenosine are operated
2024-11-22

The most widely recognized effects of adenosine are operated through inhibiting A1R, one of the most abundant G protein-coupled receptors in ER 50891 tissue [53]. A1R are located presynaptically, postsynaptically and nonsynaptically [54]. Effect of adenosine in neuronal circuits of adult mammals is
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br Results br Discussion To
2024-11-22

Results Discussion To achieve quantitative understanding of chembridge turnover, we utilize rapidly moving lamellipodial fragments that are geometrically simple, structurally homogeneous, and persistent, and measure relevant rates and concentrations in this system. We find that the lamellipod
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In terms of the ring B C position
2024-11-22

In terms of the ring B C5′ position, while C5′-F (compound ) was tolerated, C5′-Me (compound ) and C5′-Cl (compound ) substitutions resulted in a loss in potency. However, the C5′-OMe substitution (compound ) resulted in a ∼3-fold increase in potency compared to . Modeling suggested a pseudo hydroge
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Although our data failed to reproduce the
2024-11-22

Although our data failed to reproduce the robust enhancement of LTP in the rat dentate with nicotine that was previously reported, our results with NS6740 suggest a more fundamental role for α7 receptor signaling in modulation of synaptic tone in the LTP pathway. The discovery of the cholinergic ant
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During myeloid cell maturation expression of LO mRNA and
2024-11-22

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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Regarding androgens it is known that they are also
2024-11-22

Regarding androgens, it is known that they are also essential for reproductive success (Walters et al., 2010). At the molecular level, their effects are produced mainly by dihydrotestosterone (DHT), arising from the conversion of testosterone by the enzyme 3-oxo-5-alpha-steroid-4-dehydrogenase (enco
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br Introduction The principal pathways of adrenal and gonada
2024-11-22

Introduction The principal pathways of adrenal and gonadal steroidogenesis have been known for over 50 years (reviewed by Miller and Auchus, 2011). Cholesterol is first converted to pregnenolone via three reactions, 20-hydroxylation, 22-hydroxylation and scission of the 20,22 carbon–carbon bond,
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Crystal structures were obtained of sulfonamide and
2024-11-22

Crystal structures were obtained of sulfonamide 18 and amide 19 as a derivative of amide 36 (Fig. 7A and B). The precise rotameric orientation of amide 36 was of significant interest to understand the compound's interaction with the protein. As it would be difficult to assign the rotomer of 36, the
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br Materials and Methods br Results br Discussion XHP
2024-11-21

Materials and Methods Results Discussion XHP is a traditional Chinese anti-cancer medicine that is widely used for the treatment and adjuvant treatment of breast cancer. XHP has been shown to induce apoptosis in various breast cancer quick way in vitro, including Hs578T, MCF-7, and MDA-MB2
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In an effort to increase
2024-11-21

In an effort to increase antioxidant properties of peptides from WP, Le Maux et al. (2016) altered the hydrolysis conditions (pH, enzyme type, reaction time, and temperature). Hydrolysis of WP (81% protein) test samples with papain (EC 3.4.22.2) at a constant pH of 7.0 gave significantly higher ORAC
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Androgen receptor translocates from the cytoplasm to
2024-11-21

Androgen receptor translocates from the cytoplasm to the nucleus after binding to its ligands (Quigley et al., 1995). In the current study, although propofol did not significantly affect total androgen receptor protein levels, it significantly decreased nuclear androgen receptor levels. These findin
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TMPyP4 tosylate Although AMPK is a negative regulator of
2024-11-21

Although AMPK is a negative regulator of bioenergetic reprogramming in cancer cells, little is known about the role of AMPK in immunometabolism in sepsis. Our current study indicates that AMPKα dysfunction enhances PKM2-dependent aerobic glycolysis, which results in HMGB1 release in macrophages and
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