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The human serotonin hydroxytryptamine HT receptor
2020-09-23
The human serotonin (5-hydroxytryptamine; 5-HT) receptor family consists of 14 receptor subtypes to date, which are primarily G protein-coupled receptors (GPCRs) with 5-HT3 being the sole ligand-gated ion channel (Alexander et al., 2017). These receptors are widely distributed in the central and per
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Acidic substituents showed moderate biochemical activity but
2020-09-22
Acidic substituents () showed moderate biochemical activity, but these compounds showed reduced cellular potency. Additional compounds bearing a carboxylic Remodelin mg were also prepared and tested (data not shown). All of acidic compounds showed low cellular potency regardless of their biochemica
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Our structures also provide new
2020-09-22
Our structures also provide new insights into CRTH2 drug development. The ligand binding pocket revealed by our structures comprises many aromatic residues and a few polar residues at the distal end. Correspondingly, most CRTH2 antagonists share a similar structural feature characterized by an aceta
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Previous studies from our laboratory in CD mice
2020-09-22
Previous studies from our laboratory in CD1 mice using the incisional postoperative pain model have shown that the incision induces significant mechanical postoperative hyperalgesia lasting between 7 and 10days, with peak effect between 4h-2days (Cabañero et al., 2009a, Cabañero et al., 2009b, Campi
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The results showed that ethanol and
2020-09-22
The results showed that ethanol and acetaldehyde production was not affected by the presence of CPA-7. We observed that the concentration of ethanol increased throughout the assay up to 95–179 μL L-1 regardless of the treatment. The acetaldehyde concentration reached its highest values after 6–9 day
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br Conflict of interest br Acknowledgements This study was s
2020-09-22
Conflict of interest Acknowledgements This study was supported by the National Natural Science Foundation of China (No.31571839), the Chinese Ministry Program for New Century Excellent Talents in University (NCET-12-0865), and Special Fund for Agro-scientific Research in the Public Interest (N
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Pam2CSK4 br Acknowledgements br Introduction Water and elect
2020-09-22
Acknowledgements Introduction Water and electrolytes constitute an integral part of all living things, and Pam2CSK4 governing their movements play important roles in a wide variety of physiological and/or pathophysiological processes. Given the importance of channel proteins in cancer cell pr
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Rapalink-1 synthesis Propranolol initially discovered in is
2020-09-22
Propranolol, initially discovered in 1964, is first and most widely studied as a non-selective beta-blocker. Propranolol through β-adrenergic receptor blockade has reduced heart rate and blood pressure and have anti-arrhythmogenic and anti-ischemic effects, and been proposed as an effective strategy
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br In addition to the classic nuclear genomic action estroge
2020-09-22
In addition to the classic nuclear genomic action, estrogens have been found to induce rapid effects occurring within minutes following administration. These effects are mediated through a subpopulation of estrogen receptors associated with the plasma membrane, a process usually termed “membrane-i
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Studies of nuclear transplantation of diploid imprint free P
2020-09-22
Studies of nuclear transplantation of diploid imprint-free PGCs have shown that the reconstituted oocytes developed to day 9.5 of gestation, with severely retarded embryos and abnormal placentae (Kato et al., 1999). We also reported that MII oocyte injection of imprint-free phESCs without imprinted
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The optimization of the lead compound was initiated
2020-09-22
The optimization of the lead compound () was initiated and the initial key SAR and the results of the structural modifications of lead compound are summarized in . Replacement of the carboxylic RNA moiety with other functional groups led to loss of functional activity against EP4 receptor. Although
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Recoverin is a kDa retinal
2020-09-21
Recoverin is a 23-kDa retinal protein that binds to calcium. It regulates the 8-Methoxypsoralen of rhodopsin during visual transduction within photoreceptor cells. Since the pathogenicity of anti-recoverin antibody is potent, anti-recoverin CAR patients often have progressive visual impairments, cha
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Among the high value compounds derived
2020-09-21
Among the high value compounds derived from agricultural residues there are enzymes with industrial application. The extraction processes have been focused on the development of new strategies that guarantee high recovery rates with maximum activity (Nadar et al., 2017). The residues of these two fr
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Because EBI is expressed on the major subsets of immune
2020-09-21
Because EBI2 is expressed on the major subsets of immune cells, and small molecule antagonists for EBI2 were recently described (Benned-Jensen et al., 2013, Gessier et al., 2014), EBI2 constitutes a tempting drug target reminiscent of the sphingosine-1-phosphate receptor superagonist fingolimod/Gile
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br Ubiquitin ligases Ubiquitin ligases
2020-09-21
Ubiquitin ligases Ubiquitin ligases are categorized into different interleukin 1 receptor antagonist based on their specific structural configuration and the composition of subunits—HECT (homologous to E6-AP1 (E6-associated protein 1) carboxy-terminus)-type, RING (really interesting new gene)-fin
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