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Pyrimidine is the important pharmacology core in
2024-05-16
Pyrimidine is the important pharmacology core in many Aurora inhibitors, such as VX-680, ENMD-2076, CYC-116 and ENMD-2076 [12]. To identify additional effective Aurora inhibitors, we designed a series of 2,4-diaminopyrimidine compounds, our modeling studies suggested that the KL 001 core as well as
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Over the past decade extensive research has been directed to
2024-05-16
Over the past decade, extensive research has been directed toward the discovery of Aurora-selective small-molecule inhibitors. As a result, a handful of Aurora inhibitors has been identified. Among them, 1 (VX-680) and 2 (SNS-314) have entered human clinical trials as pan-Aurora kinase inhibitors (F
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Previously using a P lacZ reporter gene
2024-05-16
Previously, using a P-lacZ reporter gene system, it has been shown that the β-galactosidase activity was 9-fold higher in the stationary phase Eltrombopag when compared with those of the exponential phase [15]. Furthermore, inositol supplementation did not have a major effect on the expression of β-
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Similar to the importance of MeJA
2024-05-16
Similar to the importance of MeJA in postharvest A. bisporus quality maintenance at 10°C storage (Meng et al., 2012a), MeJA was also observed to play a pivotal role in this event at 4°C storage. Cap opening is an important mushroom quality indicator (Braaksma et al., 1999). During postharvest storag
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br Results Four HT esters butyrate caprylate laurate and ste
2024-05-16
Results Four HT esters (butyrate, caprylate, laurate and stearate esters) were chosen as representative compounds of increasing lipophilicity (Fig. 1). We will refer to them as C4HT, C8HT, C12HT and C18HT, respectively. They have been synthesized, purified and characterized according to our previ
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br Identification of the croaker mAR
2024-05-16
Identification of the croaker mAR cDNA Testosterone (T) was observed to alter steroidogenesis through a nongenomic mechanism (not blocked by the transcription inhibitor, actinomycin D) in Atlantic croaker ovarian tissues (Braun and Thomas, 2003). This action of T was mimicked by T conjugated to B
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A candidate protein for the regulation of AMPAR transport
2024-05-16
A candidate protein for the regulation of AMPAR transport is CaMKII, a Ca2+-dependent kinase with diverse cellular functions. With respect to synaptic transmission, CaMKII is recognized as a key synaptic protein that is required to modify the number of synaptic AMPARs in response to LTP and LTD stim
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These mutations induce the gene
2024-05-16
These mutations induce the gene auto-activation in 10–40% of adenocarcinomas, triggering the EGFR-signaling pathway in the absence of ligand. That leads to an uncontrolled acceleration of cell proliferation, survival and anti-apoptotic signals (Couraud et al., 2012). The frequency of these mutations
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Gliomas and Aldehyde Dehydrogenase Aldehyde dehydrogenases
2024-05-16
Gliomas and Aldehyde Dehydrogenase Aldehyde dehydrogenases (ALDHs) are key metabolic enzymes involved in regulation of glycolysis/gluconeogenesis pathways as well as in the detoxification of endogenous and exogenous aldehydes, regulating cell function and homeostasis. ALDHs play important roles in
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ethionamide The fact that Yoda can activate Piezo in the abs
2024-05-16
The fact that Yoda1 can activate Piezo1 in the absence of other cellular components other than a cell membrane [2], suggests that it may directly interact with and activate Piezo1. However, this does not preclude Yoda1 from interacting and activating non-Piezo channels, particularly in endothelial c
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br Experimental procedures br Results
2024-05-16
Experimental procedures Results Discussion Acknowledgments Introduction β-Adrenergic receptors (β-ARs) belong to the superfamily of membrane proteins termed G protein-coupled receptors. β-ARs are distributed in the effector Cinacalcet synthesis of most of the sympathetic nerve fibers
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AdipoR and AdipoR have been reported to be
2024-05-16
AdipoR1 and AdipoR2 have been reported to be present in almost all type of tissues and low Decoquinate synthesis levels have been observed in white adipose tissue (Inukai et al., 2005). These receptors have been observed to become deregulated with the onset of obesity, resulting in a reduced level
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br Adenosine receptors and the adaptive immunity T
2024-05-16
Adenosine receptors and the adaptive immunity T lymphocytes are responsible for the cell-mediated immune response [95]. These cells can be stimulated by the presentation of antigenic moieties by APCs, such as dendritic cells or macrophages [96]. The presentation of antigenic molecules on the APC
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REM sleep is proposed to create an environment to
2024-05-15
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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br Conclusion In this brief Letter
2024-05-15
Conclusion In this brief Letter, we report an easy method for the preparation of the antileukemic natural product 1. Using a biomimetic strategy,1, 8 in which the aromatic residues are attached to a lysine moiety prior to the reduction of the central carboxylate group, a step-economical synthesis
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