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FXR agonists represent an attractive class of drugs for
2022-07-05

FXR agonists represent an attractive class of drugs for patients with PFIC. Synthetic and semi-synthetic FXR agonists, with higher affinity and potency to activate FXR, have been successfully tested in animal models of cholestasis. In these murine models, the semi-synthetic steroidal FXR ligand obet
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GLP is released in response to
2022-07-05

GLP-1 is released in response to ingestion of nutrients including carbohydrates, protein, and fat. Recent studies aimed at identifying the receptors involved in nutrient stimulated GLP-1 secretion have identified free fatty CCK-8 receptor 4 (FFA4/GPR120) as a potential 7TM receptor involved in long
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Herein we report the discovery of AM
2022-07-05

Herein, we report the discovery of AM-3189 (). AM-3189 maintains the in vivo efficacy of AMG 837 while displaying a superior pharmacokinetic profile and minimal CNS exposure. As we reported previously, activity on the GPR40 receptor varies significantly with substitution at the β-carbon relative to
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Contrary to the transient nature of
2022-07-05

Contrary to the transient nature of signal transmission through PLCβ, genome-wide RNAi screens revealed that the signaling events driven by Gαq that result in aberrant cell proliferation depends on highly specific protein-protein interactions, rather than solely on diffusible second messenger system
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Orlistat Previous studies have shown that ox LDL induced hep
2022-07-05

Previous studies have shown that ox-LDL-induced hepatic sinus dysfunction is the result of multiple pathways, multi-factorial regulation, and in the present study, we reported for the first time that ox-LDL regulates the basement membrane protein VN through the integrin αvβ5 pathway under high gluco
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The organ culture method has previously shown
2022-07-05

The organ culture method has previously shown to be a suitable model for investigations of receptor upregulation on vascular smooth muscle cells (Adner et al., 1996). In our study, the organ culture method was applied in order to examine whether LPS from P.g. was capable of altering the gene express
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The molecular mechanism of gliotransmitter release
2022-07-04

The molecular mechanism of gliotransmitter release is not fully understood until now, and previous studies have emphasized that the elevation of [Ca2+]i triggers vesicular Zoniporide hydrochloride of glutamate. Parpura et al. reported that the essential role of Ca2+ release from internal stores in g
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Based on pharmacophore modeling a good HDAC
2022-07-04

Based on pharmacophore modeling, a good HDAC inhibitor has at least three sides/regions: the attachment side of the Zn2+ cofactor/HDAC active site (Zn2+ binding group/ZBG), hydrophobic cap (CAP) and linker containing connecting unit (CU) with electronegative groups (Mohan et al., 2011, Rossi et al.,
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Carbidopa sale The present results indicate that
2022-07-04

The present results indicate that oxidative damage in CFS muscles is not due to the decline in the efficiency of antioxidative enzymes. This suggests that there is an increase in the generation of reactive oxygen species consistent with a mitochondrial origin of the damage. Mitochondria represent th
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The different NO stimulated and
2022-07-04

The different NO-stimulated and ODQ-inhibited cNMP patterns in terms of absolute and relative magnitude and time course reported herein suggest distinct functional roles of cGMP, cCMP and cUMP. Therefore, it will be necessary to dissect cellular effects of these cNMPs in numerous cell systems. For t
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br Introduction Soluble guanylyl cyclase GC
2022-07-04

Introduction Soluble guanylyl cyclase (GC-1) maintains vascular function through the NO/GC-1/cGMP pathway [1,2] by catalyzing the conversion of GTP into cGMP (Fig. 1). The GC-1 heme prosthetic group binds NO with picomolar affinity, resulting in a 100- to 200-fold increase in catalytic activity.
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Two genes PATL and RASSF whose
2022-07-04

Two genes (PATL2 and RASSF1), whose relationship to HIV infection had not previously been reported, were identified in this study. Although PATL2 and RASSF1 have been implicated in cell division and tumor suppression, respectively (Scheller et al., 2007, Rather et al., 2014, Liu et al., 2002), their
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In conclusion we have identified ten novel GPCR genes and
2022-07-04

In conclusion, we have identified ten novel GPCR genes and a pseudogene. Transcripts for GPR78, GPR81, GPR94, GPR95, GPR101, GPR103 and P2Y were detected in various CNS and peripheral tissues. Given the high levels of identity observed within paralogous oGPCR gene clusters, future efforts will likel
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The ketone body receptor HCA
2022-07-04

The ketone body receptor HCA2 is most likely not active under normal conditions, since local levels and plasma levels of ketone bodies such as β-HB are too low to activate the receptor. However, overnight fasting or prolonged starvation results in plasma levels of the ketone body in the millimolar r
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While a role for YAP TAZ signaling in oligodendrocytes has
2022-07-04

While a role for YAP/TAZ signaling in oligodendrocytes has not been described, these NK 252 receptor are also responsive to mechanical stimuli. OPC proliferation and migration can be altered by plating on substrates of varying stiffness [20], resulting in differentiation in a density-dependent mann
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