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Both GPR A and GPR are located
2021-12-01
Both GPR109A and GPR81 are located on chromosome 12q24 [3] and mediate anti-lipolytic effects through coupling to Gi-type G proteins [17]. It is important to note that with the recent deorphanization of these receptors, there has been a recommendation to the International Union of Basic and Clinical
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Probenecid Tight junctions regulate the transfer of ions
2021-11-30
Tight junctions regulate the transfer of ions as well as small molecules across endothelial barriers (Li et al., 2015). We also investigated whether resistin affects tight junctions, which play an important role in the conformation of polarized endothelial barriers (Matsuzaki et al., 2010). A previo
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br Origin of the vertebrate hexokinase gene
2021-11-30
Origin of the vertebrate hexokinase gene family Multiple hexokinases have been found in vertebrates, plants and yeast (Wilson, 1995, Cárdenas et al., 1998). A hexokinase in both vertebrates and yeast has, unfortunately, been named glucokinase. The sharing of the name glucokinase has suggested to
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br Acknowledgments We would like to acknowledge
2021-11-30
Acknowledgments We would like to acknowledge Jenna Hall, Marita Rivir, Kathleen Smith, Joyce Sorrell, and Emily Yates for assistance with in vivo pharmacology studies. We would like to acknowledge Joe Chabenne and Steph Mowery for assistance with in vitro cell-based assays, and Patrick J. Knerr f
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endothelin receptor antagonist br Acknowledgements Research
2021-11-30
Acknowledgements Research was funded by the Natural Sciences and Engineering Council of Canada (NSERC) (Grant #210290) SGF. The funding body played no role in the design or execution of the study. The authors declare no conflict of interest. Introduction HBO2 therapy is the use of 100% oxygen
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The primary cancer lesion was mostly
2021-11-30
The primary cancer lesion was mostly in the uterus and adnexa, followed by the gastrointestinal tract, brain, blood, and kidney and Celecoxib sale (Fig. 2A). Histopathological findings indicated that most cancers were adenocarcinomas, followed by squamous cell carcinomas, glioblastomas, malignant ly
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PKC s effect on quantal size
2021-11-30
PKC’s effect on quantal size may involve regulation of endocytotic protein components responsible for mediating kiss-and-run exocytosis. There is a growing body of evidence to suggest that canonical endocytotic proteins—dynamin, amphiphysin, syndapin, and others—may play a role in modulating fusion
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In addition to indoles two additional structural variants we
2021-11-30
In addition to indoles –, two additional structural variants were synthesized to explore the synthetic flexibility and structure–activity relationships of this system. The first of these was the homologation of the acetic Piperaquine side chain to prepare compound (). The extension of the chain was
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SB 290157 trifluoroacetate salt Taken together the four HRs
2021-11-30
Taken together, the four HRs couple with several different signaling pathways modulating various G-proteins (Fig. 1). Histamine H1R The H1R, including many other biogenic amine receptors, is one of the GPCR family members (see for a complete list e.g. http://www.gpcr.org/7tm/ or http://tools.gpc
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Although histamine can induce both proliferation and
2021-11-30
Although histamine can induce both proliferation and differentiation in vitro (Molina-Hernandez and Velasco, 2008), the promotion of neurogenesis conferred by H3R antagonism here does not seem to be caused by either the proliferation or the reduction of apoptosis of NSCs (Figure S3). Furthermore, H3
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Over recent decades there were three
2021-11-30
Over recent decades, there were three breakthroughs of high intensity heavy-ion acceleration [6]. The first is the invention of radio frequency quadrupole (RFQ) type accelerator, which could accelerate more than dozens of milli-ampere ion beams and is a good solution to space-charge-effect of heavy-
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Substrate affinity and specificity can be enhanced by dockin
2021-11-30
Substrate affinity and specificity can be enhanced by docking interactions, in which regions distal to the site of Akt Inhibitor IV bind to grooves, pockets, or surfaces outside of the kinase catalytic cleft 1, 2, 5, 6. Like catalytic site interactions, docking interactions can involve recognition
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After establishing improved GSNOR potency some of
2021-11-30
After establishing improved GSNOR potency, some of the potent inhibitors were further evaluated for microsomal stability and CYP inhibition studies (). Majority of the tested analogs revealed high metabolic stability in human and rat liver microsomes, and moderate to low stability in mouse liver mic
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GPR belongs to the G protein coupled
2021-11-30
GPR84 belongs to the G protein-coupled receptor family, and it was first identified from human peripheral blood neutrophils [,]. GPR84 is now considered to be a member of receptor for medium chain fatty brucine mg (MCFA) with carbon chain lengths of 9–14 []. GPR84 is mainly expressed in bone marrow,
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Lactate induced GPR activation was
2021-11-30
Lactate-induced GPR81 activation was confirmed with a fluorimetric imaging plate reader (FLIPR) assay, in which lactate induced a [Ca2+] flux in CHO cells stably expressing Gqi5 and HA-GPR81 but not vector control (Fig. 1C). The EC50 of lactate in the FLIPR assay was 4.3±0.73mM, a value well within
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