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br Drug design Over the past
2021-12-24
Drug design Over the past decades, the development of synthetic, direct fXa inhibitors has undergone four phase. Although these fXa inhibitors possess various scaffolds, most of them bind to the active site in a characteristic l-shaped conformation. In other word, they have a three-component syst
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br Materials and methods br Results br Conclusions In genera
2021-12-24
Materials and methods Results Conclusions In general, the drug design process is very laborious, expensive and prone to errors. Various computational methods including docking and algorithms based on molecular dynamics and/or quantum chemistry can help considerably at the early stage of str
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Most of the GSNOR inhibitors presented here were synthesized
2021-12-24
Most of the GSNOR inhibitors presented here were synthesized according to . The synthesis started from either commercially available ketones or the ketones prepared as described in the . In , condensation of ketone and 2-furanaldehyde provided intermediate in good yield. Furan ring opening of inte
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br Introduction Atherosclerosis is a chronic inflammatory
2021-12-24
Introduction Atherosclerosis is a chronic inflammatory disease characterized by lipid and leukocyte accumulation within the arterial wall. Homocysteine (Hcy) is a thiol-containing amino epothilone derivative derived from the metabolism of dietary methionine. Epidemiological studies have shown th
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To search for potential variants of SLA DOB
2021-12-24
To search for potential variants of SLA-DOB and CD4 associated with different (percentage) levels of the five (T-lymphocyte subsets, total antibody IgG, interferon alpha (IFN-α), Toll like receptor 3 (TLR3), interleukin 6 (IL-6) in serum and porcine reproductive and respiratory syndrome virus (PRRSV
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N,N-Dimethylsphingosine receptor Although both receptors mGl
2021-12-24
Although both receptors, mGluR1 and mGluR5, are present in cortical and hippocampal areas from 1 to 2 weeks old neonates (López-Bendito et al., 2002) we have found that only mGluR1 was regulated after maternal l-Glu consumption. A possible explanation could be based on the different ontogenetic prof
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GW 6471 The simple carrier model for GLUT
2021-12-24
The simple carrier model for GLUT1 transport activity proposes that the transporter alternates between an outward facing glucose binding site and an inward, cytoplasmic, facing glucose binding site. Cytochalasin B is an endofacial inhibitor and appears to preferentially bind to the open, inward faci
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GKRP binds to the inactive super open conformation of
2021-12-24
GKRP binds to the inactive, super-open conformation of GCK, acting as a competitive inhibitor of glucose association with the enzyme (Fig. 3) [45]. Upon formation of the inhibitory complex with GKRP, GCK is sequestered into the hepatocyte nucleus [48]. The detailed mechanism by which GKRP mediates t
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Taken together our results show that at least
2021-12-24
Taken together, our results show that, at least in the in vitro cell line model, methylation within the proximal promoter region of GHSR is an important determinant of its expression; however, to determine whether this represents a physiologically and or pathophysiologically relevant event, further
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Introduction Glucose dependent insulinotropic polypeptide
2021-12-24
Introduction Glucose-dependent insulinotropic polypeptide (GIP) is a hormone secreted postprandially from enteroendocrine K cells in response to ingestion of either fat [1], protein [2], or carbohydrates [3]. GIP is primarily known for its glucose-dependent insulinotropic actions mediated via the G
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In addition we assessed the viability of tetrahydroquinoline
2021-12-23
In addition, we assessed the viability of 1,2,3,4-tetrahydroquinoline (13t) and 1,2,3,4-tetrahydroisoquinoline (13u) as the tail on account of our previous SAR results. To our delight, 13t and 13u each had comparable activity to that of 13c, with 13u being slightly more potent than 13c. Further stru
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The present study also demonstrated that edoxaban inhibited
2021-12-23
The present study also demonstrated that edoxaban inhibited both free and clot-bound FXa activity. The IC50 values for free and clot-bound FXa in this study are well consistent with Ki values for free FXa and FXa incorporated in prothrombinase complex (0.561 and 2.98nM, respectively) in our previous
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alpha adrenergic blockers br Introduction Edible bird s nest
2021-12-23
Introduction Edible bird's nest (EBN), known as the health and precious food, is produced from the saliva secretion of several different swiftlet species. Researches have shown the nutritional value of the EBN with the containing of glycoproteins, carbohydrates, essential amino acids, minerals an
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Glutamate is a ubiquitous principal excitatory
2021-12-23
Glutamate is a ubiquitous principal excitatory neurotransmitter in the orphan receptor that plays a central role in a variety of brain functions (Delgado, 2013, Hawkins, 2009). Several studies reported that CSF glutamate was associated with mental illness, including major depressive disorder, anxio
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nfat br Experimental methods br Acknowledgments We thank
2021-12-23
Experimental methods Acknowledgments We thank all members of the Hermanson lab, especially Ana Teixeira, Shirin Ilkhanizadeh and Karolina Wallenborg, for assistance and discussions, Peter Löw for anti-synaptotagmin antibody, and Lars Björklund, Ole Isacson, Christer Höög, Claes Wahlestedt and
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