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Our observation that squalestatin caused only small differen
2022-12-12
Our observation that squalestatin caused only small differences in the production of Aβ40 and Aβ42 was in contrast to prior reports of the effects of other cholesterol synthesis inhibitors. This may be due to using squalestatin, a more specific cholesterol synthesis inhibitor that does not affect is
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Perhaps the first evidence of AMPKs therapeutic ability
2022-12-12
Perhaps the first evidence of AMPKs therapeutic ability in DM1 came from Thomas Cooper’s laboratory where they demonstrated that insulin-independent glucose uptake was unaffected in human DM1 muscle 4-IPP treated with MET, an AMPK activator and first-line therapy for type 2 diabetes mellitus [76].
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br Introduction There are greater than five
2022-12-12
Introduction There are greater than five million Americans living with Alzheimer's dementia and more than 35 million people worldwide [1], and without a way to stop or slow the progression, there will be nearly a tripling of individuals affected by 2050 (13.8 million) [1]. The urgency to develop
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br Conclusions and clinical relevance Astrogliosis and
2022-12-12
Conclusions and clinical relevance Astrogliosis and an increase in ADK is a pathologcial hallmark of epilepsy. The consequence of increased ADK in the epileptic PP 2 is a decrease in the ambient adenosine tone and A1R activity. As a result, systemic administration of A1R agonists or ADK inhibito
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Regarding the HT B receptors they act as terminal receptors
2022-12-09
Regarding the 5-HT1B receptors, they act as terminal receptors and are involved in the presynaptic regulation of the release of 5-HT. But at spinal level these receptors are principally situated post-synaptically (Sari, 2004). The ability of autoreceptors to regulate extracellular levels of 5-HT dur
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The mechanism by which Gas prevents inflammation has
2022-12-09
The mechanism by which Gas6 prevents inflammation has been reported to be via inhibition of Toll-Like receptors (TLRs) signaling (Cui et al., 2016). After injury, TLRs become stimulated, leading to downstream activation of TRAF3 and TRAF6 and translocation of several transcription factors, such as I
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Aurora A or B selective
2022-12-09
Aurora -A or -B selective and pan-aurora inhibitors have demonstrated different preclinical and clinical therapeutic efficacies [2,[19], [20], [21], [22], [23]]. For example, clinical trials for a pan-Aurora inhibitor VX-680 (developed by Vertex) were halted at phase II for toxicity reasons (one cas
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br Conclusion br Competing interests br Funding
2022-12-09
Conclusion Competing interests Funding The Bolger Prostate Cancer Research Fund (no grant number), the National Institute of General Medical Sciences of the National Institutes of Health (1-R01-GM58553, G. B. Bolger, principal investigator), and the National Cancer Institute of the NIH to t
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br Antibiotic drug discovery approaches Traditionally
2022-12-09
Antibiotic drug discovery approaches Traditionally, novel NVP-BGJ398 phosphate were largely discovered by phenotypic screening approaches of various sources of compounds, such as natural products isolated from extracts of soil microbes and semi-synthetic or fully synthetic compound libraries der
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Salmeterol xinafoate The loss of synaptic proteins such as s
2022-12-09
The loss of synaptic proteins such as synaptophysin from the Salmeterol xinafoate is indicative of synapse degeneration and provided a good correlate of the degree of dementia in AD [12], [13], [14]. Consequently, the loss of synaptic proteins from cultured primary neurons incubated with Aβ provides
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What is the mechanism by which
2022-12-09
What is the mechanism by which Wnt7a-Fz7 signaling enhances AMPAR localization and synaptic strength? Following induction of LTP, the number of AMPARs rapidly increases at extrasynaptic sites (Makino and Malinow, 2009, Yang et al., 2008a) through PKA-dependent phosphorylation of GluA1 at S845 (He et
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Activation of AhR is also known to upregulate the
2022-12-09
Activation of AhR is also known to upregulate the expression of AhRR (AhR repressor), an inhibitor protein of AhR [29]. However, the exact mechanism by which AhRR represses AhR signaling is not well understood. The initial study by Mimura and colleagues suggested that AhRR is capable of directly com
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REM sleep is proposed to create an environment to
2022-12-07
REM sleep is proposed to create an environment to facilitate plasticity processes that create a generalized downregulation of synaptic strength (Grosmark et al., 2012; Tononi and Cirelli, 2014), while synapses are upregulated specifically by the reactivation of neuronal firing sequences experienced
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Talabostat mesylate A rational approach for the design
2022-12-06
A rational approach for the design of new steroid compounds as possible competitive inhibitors of CYP17 include chemical modification at C17 of the enzyme's natural substrates, pregnenolone (1) and progesterone (2), introducing groups with moderate to strong dipole properties at C20, such as oxime a
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There are several AP binding sites in the sequence
2022-12-05
There are several AP-1 nox4 sale in the sequence of TIMP-1 promoter [18,19]. EBV could up-regulate TIMP-1 expression by binding to the AP-1 site in the TIMP-1 promoter [18]. IL-32, a newly multi-function cytokine, could activate AP-1, NF-κβ, p38MAPK signal pathways, and induce cytokine expressions,
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