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br MUTYH associated polyposis br MUTYH
2022-04-20

MUTYH-associated polyposis MUTYH and its metal cofactors MUTYH harbors two vital cofactors, both of which are located remotely from the active site (Fig. 6). One of these cofactors, a [4Fe-4S]2+(Fe-S) cluster, is chelated by four Cys residues in the N-terminal domain, and positions an Fe-S clu
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br Funding This work was supported
2022-04-20

Funding This work was supported by the Deutsche Forschungsgemeinschaft (SFB766 and GRK1708). Conflict of interest Acknowledgements Introduction Hepatitis C virus (HCV) infection is a global problem affecting about 3% of the world’s population [1], [2]. Mother-to-child transmission of HC
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kynurenine To further investigate if GPR was the
2022-04-20

To further investigate if GPR40 was the functional target of these phenylpropiolic kynurenine analogs, GW-1100, a selective antagonist of GPR40-mediated Ca2+ elevations in HEK293 cells with an IC50 value equal to 1 μM, was used to inhibit agonist-induced intracellular calcium flux [15]. HEK293-GPR4
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br Acknowledgements br Introduction Protein translation
2022-04-20

Acknowledgements Introduction Protein translation demands high fidelity. There are number of molecular checkpoints to fulfill this demand. Among these, insuring that a particular tRNA gets aminoacylated by its conjugate amino acid, which in turn is catalyzed by a particular aminoacyl-tRNA synt
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Apple juice is the most consumed apple
2022-04-20

Apple juice is the most consumed apple derivative since more than 20% of freshly harvested apples are consumed as juice (Schulze et al., 2014). Apple juice production implies several technological interventions, among which are skin and pomace removal, enzymatic depectinization, and pasteurization.
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br Central control of GI ghrelin secretion The
2022-04-19

Central control of GI ghrelin secretion The CNS communicates with the GI tract through the vagus nerve originating in the DMV and sympathetic spinal afferents emanating from the thoracic spinal chord (Bray, 2000). The cells that secrete peripheral ghrelin are under direct control of these two pat
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In summary the SAR of a series
2022-04-19

In summary, the SAR of a series of phenylpropanoic acid-free fatty Nalidixic acid mg receptor agonists is described which resulted in the identification of potent FFA4 agonists. The superior pharmacokinetic properties of compound led to its selection as an in vivo tool compound which afforded robust
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Recently they reported an enyne chemotype agonist Fig with l
2022-04-19

Recently, they reported an enyne chemotype agonist (21, Fig. 13) with low lipophilicity, small polar surface area (PSA) and high potency (Clog P=3.8, tPSA=37 A2, EC50=20nM), further derived from TUG-424. The compound endowed fast oral gsk3b inhibitor (tmax=15min) and a decent pharmacokinetic profile
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The apparent lack of effect of
2022-04-19

The apparent lack of effect of Fas deficiency on MAV-1 replication in infected mice could be due to immunoevasion by virus inhibition of Fas activation. If that were the case, Fas deficiency would likely have minimal additional effect. HAdV infection triggers Fas internalization from the cell membra
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br Materials and methods br Results
2022-04-19

Materials and methods Results Discussion Several histamine H3 receptor antagonists have progressed into clinical development for indications including Alzheimer's disease, schizophrenia, pain and narcolepsy. Each of the compounds studied herein has been extensively characterized in its own
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Diclofenac Thus while there is ample
2022-04-19

Thus, while there is ample evidence to rule out a generalized blockade of TGF-ß signaling by Hippo pathway activation upon establishment of cell–cell contacts, more recent studies have established that, in specific contexts, Hippo and TGF-ß signaling may either interfere or cooperate with each other
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Hypoxia HIF and Inflammation Cellular responses to hypoxia a
2022-04-19

Hypoxia, HIF, and Inflammation Cellular responses to hypoxia are essential for life and are now recognized to be dysregulated in a wide range of disease processes. The key players in these pathways are a family of transcription factors, the hypoxia-inducible factors (HIFs; see Glossary), as well as
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br Introduction Local anesthetics LAs are a set of
2022-04-19

Introduction Local anesthetics (LAs) are a set of common medicines used for pain management in clinical settings. Up to now, LAs have been extensively used for peripheral nerve blocks, interventional spinal procedures, and epidural anesthesia [1]. In addition to their anesthetic and analgesic eff
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br Trifluoromethylketones This group of compounds was demons
2022-04-19

Trifluoromethylketones This group of compounds was demonstrated to bind the zinc 3CAI in the active site due to its easy hydration, forming the required chelating intermediate. Ontaria et al. [92] have proposed variations around the cap group of trifluoromethylthiophene as the core motif for the
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br Methods br Results br Discussion Our results show that
2022-04-18

Methods Results Discussion Our results show that the DRG and the spinal cord express significant amount of GPR35, a previously orphan Gi protein coupled receptor whose stimulation with zaprinast or with KYNA may reduce inflammatory pain. The receptor is also expressed in primary cultures of
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