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Molecular simulation has proven useful in describing the dyn
2024-04-27
Molecular simulation has proven useful in describing the dynamics and energetics of NMDA receptor LBD cleft closure and the potentiating role of glycans (Yao et al., 2013, Dai and Zhou, 2013, Dai and Zhou, 2015, Dai and Zhou, 2016, Dutta et al., 2015, Omotuyi and Ueda, 2015, Sinitskiy and Pande, 201
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At the outset of targeting the two Gln side chain
2024-04-27
At the outset of targeting the two Gln756 side-chain rotamers, it was unclear which rotational isomer would lead to more potent ASK1 inhibitors. While such a preference might have been anticipated, the cohort of ASK1 inhibitors in Table 3 did not provide any guidance regarding which of the Gln756 am
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Misoprostol Available data thus indicate that there are at l
2024-04-27
Available data thus indicate that there are at least two ways that HMGA proteins can induce localized changes in the chromatin structure of inducible gene promoters, both of which involve positioned nucleosomes that must be “remodeled” before gene transcription can occur. The first mechanism is exem
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In mice the Tfm mutation
2024-04-27
In mice, the Tfm mutation increased the anxiety-state assessed in the novel object and in light/dark box tests, whereas no changes were detected in the open field or elevated plus maze tasks (Zuloaga et al., 2008). As for Tfm rats, this seemed to be related to an increased HPA response to stress. Th
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br Results br Discussion Here we
2024-04-27
Results Discussion Here, we uncovered a role for Wnt-Fz7 signaling in LTP-dependent spine plasticity and synaptic localization of AMPARs. We demonstrated that LTP induction increased Wnt7a/b protein at Allopurinol and spines. Direct blockade of endogenous Wnts impaired LTP-mediated structural
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There is a growing body of evidence
2024-04-27
There is a growing body of evidence showing that pentobarbital causes memory disorders [3], [4], [5]. Our results that a single injection of pentobarbital into bilateral hippocampus significantly impaired hippocampus-dependent spatial memory retrieval (Fig. 1) add support to that evidence. Previous
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Inflammatory factors released by activated cells during AD
2024-04-27
Inflammatory factors released by activated cells during AD are very important for the disease progression. Not only several inflammatory cytokines, such as IL-1β, IL-18, and IL-33, but also anti-inflammatory ones, as IL-10 and IL-13, are upregulated in the brain of AD patients (Morimoto et al., 2011
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When a clinician diagnoses a person with AD
2024-04-27
When a clinician diagnoses a person with AD, the person is transformed into a patient with the disease. The person is a member of a patient group associated with behaviors, abilities, and experiences related both formally and informally to the diagnosis [10]. The diagnostic label implies what signs
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During the course of our ACK
2024-04-26
During the course of our ACK1 inhibitor program, a high-throughput screening (HTS) campaign of our internal sample collection was conducted. A series of -aryl pyrimidine-5-carboxamides of the general structure () was identified. Earlier studies of the structure–activity relationship (SAR) of identif
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The first natural product described
2024-04-26
The first natural product described as 5-LO inhibitor was the polyphenol nordihydroguaiaretic eukaryotic initiation factor from the Mexican dessert plant Larrea divaricata in 1981 (Bokoch and Reed, 1981), short after the initial identification of 5-LO in 1979 (Borgeat and Samuelsson, 1979). Long ti
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HCC aetiology is multifactorial and
2024-04-26
HCC aetiology is multifactorial and the disease is often preceded by other conditions including liver fibrosis and cirrhosis that are associated with HCV, HBV, alcoholic and non-alcoholic hepatitis. The discovery of new therapeutic targets will require a greater understanding of the pathogenic mecha
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Although we have achieved a great deal of success
2024-04-26
Although we have achieved a great deal of success in the development of tools to understand autophagy in health and disease, highly specific reagents for autophagy manipulation and deep knowledge of autophagy is required to advance the research in therapeutic treatment. Better disease (ischemia) ani
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br Innate immune mechanisms that
2024-04-26
Innate immune mechanisms that confront viral infection Autophagy induction by virus sensing Antiviral xenophagy and virophagy The presence of viral particles within autophagosomal structures has been visualized in only rare instances. This is the case for HSV-1 when it is devoided of ICP34
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NVP-CGM097 Why do glutamate and glycine bind to
2024-04-26
Why do glutamate and glycine bind to the NVP-CGM097 in such different ways? Given the overall structural similarity between the GluN2A and GluN1 LBDs, one might conclude that the LBDs also bind ligands via similar processes. NMDA receptors with engineered disulfide linkages that lock the GluN1 lobe
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The most likely explanation for
2024-04-26
The most likely explanation for the species differences in aromatase distribution and the unique LDC000067 distribution in humans is the unique location, size and highly elaborate organization of the human aromatase gene (e.g. Bulun et al., 2003). The human Cyp19 is a large gene located on chromosom
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