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The most classic case of
2021-11-12
The most classic case of acquired and relapsing epilepsy is temporal lobe epilepsy (TLE), which originates from the hippocampal formation, a structure situated in the mesial temporal lobe (Majores et al., 2007). Our experiment used the prominent pilocarpine-induced TLE model. Systemic administration
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The eradication of agonist activity in compound was
2021-11-12
The eradication of agonist activity in compound was also confirmed in the ex vivo growth hormone (GH) release experiment conducted in isolated primary rat pituitary CC-223 as shown in . Compound did not produce any noticeable GH secretion at up to 10μM concentration. It could also antagonize the
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Furthermore our results are the first
2021-11-12
Furthermore, our results are the first to demonstrate that the stimulating effect of GALP on AVP release in rats is independent of galanin receptors. The same stimulatory GALP influence on AVP secretion has been also observed in the presence of galantide, an antagonist of Gal receptors in the incuba
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br Introduction Farnesoid X receptor FXR is a bile
2021-11-12
Introduction Farnesoid X receptor (FXR) is a bile DAMGO regulated nuclear receptor highly expressed in the liver, intestine, kidney and adrenal glands in rodents.1, 2, 3, 4 FXR regulates transport proteins, the bile salt export pump (BSEP) and the organic solute transporter α (OSTα) that are inv
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br Materials and methods br
2021-11-12
Materials and methods Results To examine the apoptosis in FLS in vitro, we measured the number of GS-1101 in early apoptosis (Annexin V+, 7-AAD−) and late apoptosis/necrosis (Annexin V+, 7-AAD+) using flow cytometry after incubation with or without stimulating Fas antibody. In the absence of
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Several observations about structure activity relationships
2021-11-12
Several observations about structure–activity relationships can be made from this series, including that: (1) all lead compounds are NSAIDs of the 2-arylpropionic A922500 class, (2) analogues with -oriented aryl substituents showed the best inhibition of FAAH, and (3) replacing the ether linkage of
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alpha amanitin The coenzyme S adenosylmethionine SAM binding
2021-11-12
The coenzyme S-adenosylmethionine (SAM)-binding pocket of Set7 is connected to the histone-tail binding groove by a conserved lysine-channel, similarly observed in vSET (Figures 2D and S3). The Set7 SAM-binding pocket is negatively charged as observed in other known HMTase structures. However, the b
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sodium salt synthesis Maillard reaction also known as
2021-11-12
Maillard reaction, also known as non-enzymatic browning reaction, is a complex chemical reaction between carbonyl groups of reducing sugars and free amino groups of amino acids, peptides, proteins or some other nitrogen containing compounds. Maillard reaction plays an important role in food industry
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br Conflict of interest br Acknowledgments We thank Professo
2021-11-12
Conflict of interest Acknowledgments We thank Professor Chen Rui (Southeast University, China) for providing plasmid P1P2N-HIF1. This study was supported by research grants from National Natural Science Foundation of China (81573189, 81730087). Introduction The consumption of large amounts
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The zinc dependent HDACs are classified into four
2021-11-12
The zinc-dependent HDACs are classified into four groups based on their structure, complex formation, and expression pattern: class I (HDAC1, HDAC2, HDAC3, and HDAC8), class IIa (HDAC4, HDAC5, HDAC7, and HDAC9), class IIb (HDAC6 and HDAC10), and class IV (HDAC11) [16]. We recently reported on a cyto
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For further understanding of the interaction between
2021-11-12
For further understanding of the interaction between these inhibitors and proteins (BRafV600E and HDAC1) for guiding the SAR, compound 10e, the most potent compound of this series, was chosen as a representative for docking into the BRafV600E (PDB code: 1UWJ) and HDAC1 (PDB code: 1C3R), revealing ex
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Recently an increasing number of studies
2021-11-11
Recently, an increasing number of studies have highlighted the crucial role of nociceptive factors produced by microglia under neuropathic pain conditions (Mika et al., 2013; Popiolek-Barczyk and Mika, 2016). iNOS is an important pronociceptive factor that is strictly expressed by microglia/macropha
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In prostate cancer PCa glucose metabolism plays a
2021-11-11
In prostate cancer (PCa), glucose metabolism plays a major role in progression [14]. Androgens can activate the metabolic regulator AMP-activated kinase (AMPK), promoting oxidative phosphorylation (OXPHOS) [15]. Besides, androgens increase GLUT1 [16], which overproduction has been described in the
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Despite the potential promise of
2021-11-11
Despite the potential promise of both of these peptides, such compounds are still susceptible to efficient renal filtration (Emmanouel et al., 1978, Holst, 1991, Deacon et al., 1996). However, numerous studies have demonstrated that fatty 76 7 dervatisation of related regulatory peptides results in
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Cys loop GABA receptors are well
2021-11-11
Cys-loop GABA receptors are well-studied targets for insecticides and also play an important role in nematode biology. These receptors are also targets for the anthelmintic piperizine (Accardi et al., 2012). The nematode GABA receptor most studied is the UNC-49 receptor which plays a role in muscle
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