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br Perspectives Given the complexity of the
2025-01-17
Perspectives Given the complexity of the cellular interactome and of protein scaffolding, further progress in revealing how individual membrane proteins, including APP and AChE, interact with each other at various levels, from cell-surface shedding to gene regulation, will clarify some intrinsic
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Although effects of low concentrations of agonist
2025-01-17
Although effects of low concentrations of agonist were not as thoroughly documented for heteromeric receptors such as the major guanfacine hydrochloride α4β2 nAChR, a similar mechanism of action was described to explain the potentiation of these receptors with low concentrations of acetylcholine-est
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This study does have several
2025-01-17
This study does have several limitations, mainly related to the DMSO vehicle. While DMSO is a known anti-inflammatory mediator,5, 12 it has been shown to upregulate ALOX5, which was not seen in this study (as we are likely underpowered to detect this difference). A manifestation of this anti-inflamm
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LOXO-101 br Acknowledgements DHA was funded by a research
2025-01-17
Acknowledgements DHA was funded by a research grant from Viamet and IMB and DHA were/are consultants for Viamet/Innocrin. DHA also supported by NIH P51-OD011106. Introduction Congenital adrenal hyperplasia resulting from 17alpha-hydroxylase and 17,20-lyase deficiency (17OHD) is a rare autosom
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Our previous studies found that some
2025-01-17
Our previous studies found that some steroid mimetic structures such as stilbene, biphenyl, naphthalene and benzothiophene rings were suitable for lipophilic moieties of 17,20-lyase inhibitors, and several inhibitors obtained using a steroid A, C-ring mimetic approach have already been published. Du
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Having taken a step back
2025-01-17
Having taken a step back from affinity to gain better exposure and solubility, we started work to replace the unstable oxazolinone, and address the selectivity over the hERG channel. Keeping in mind the binding mode of the series from crystal structures, triazole was identified as another mildly aci
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br Autophagy at the Synapse The synapse is a highly
2025-01-17
Autophagy at the Synapse The synapse is a highly specialized neuronal compartment that forms the basic unit of communication between neurons. Communication relies on electrical signals that are propagated down the axon of the presynaptic neuron, where they trigger the quantal release of neurotran
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Polyphenols like flavonoids have the
2025-01-17
Polyphenols like flavonoids have the potential to penetrate into lipid bilayers which is vital for enabling protection against oxidation. Rosmarinic Sulindac sulfone is a natural polyphenol antioxidant isolated from Sphaeranthus amaranthoides. Polyphenols can inhibit the propagation of lipid oxidat
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In liver the essential organ
2025-01-17
In liver, the essential organ of lipoprotein synthesis, ACL plays a fundamental role in lipogenesis and steroidogenesis by supplying cytosolic 5-moUTP modified mRNA to both pathways. By using a tricarboxylic acid cycle intermediate (citrate) to produce acetyl CoA, ACL can be seen as an important br
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RN486 anti-inflammatory The Type A series contains of the co
2025-01-17
The Type-A series contains 6 of the 11 confirmed hits, making it a highly attractive lead template. Seven (7) out of 8 Type-A series of 3-substituted-2-furoic acids are highly active (84–100% inhibition) at the high concentration of 100μM. We could deduce some interesting, albeit preliminary structu
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br Funding This study was supported
2025-01-16
Funding This study was supported by a grant from the Science and Technology Program of Guangzhou (No. 2014Y2-00181) and the personnel training program of Southern Medical University (No. PY2015N023). Conflict of interest statement Authors’contributions Introduction Chronic cerebral hypo
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br Polymorphic variation ERAP is polymorphic
2025-01-16
Polymorphic variation ERAP1 is polymorphic and several single nucleotide polymorphisms (SNPs) in its gene that encode amino ubiquinone coq10 australia changes have been associated with predisposition to a variety of diseases, ranging from viral infections to cancer and autoimmunity (Alvarez-Navar
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The aldehyde reductase AKR A and aldose reductase AKR B
2025-01-16
The aldehyde reductase (AKR1A1) and aldose reductase (AKR1B1) belong to aldo-ketoreductase (AKR) superfamily catalyzing the reduction of corresponding aldehydes and ketones involved. Both the closely related enzymes AKR1A1 and AKR1B1 have 65% structural similarity and differ only at the active site.
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AhR is also known to cross
2025-01-16
AhR is also known to “cross-talk” with a variety of other cell signaling pathways, which has been the focus of a number of recent reviews [40], [41], [42]. It has long been known that TCDD is anti-estrogenic. For example, activation of AhR by TCDD and related HAHs inhibits estrogen dependent uterus
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Lipotoxicity is the accumulation of excess lipids in non adi
2025-01-16
Lipotoxicity is the accumulation of excess lipids in non-adipose tissues that leads to cell dysfunction or cell death. It may play an important role in the pathogenesis of diabetes, and contributes to the rate of progression of CKD [7,8]. Emerging evidence indicates that renal lipid dysregulation is
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