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Epigenetic drugs such as HDAC inhibitors regulate
2022-01-12
Epigenetic drugs, such as HDAC inhibitors, regulate gene expression by affecting the activity of histone or DNA modifying enzymes and their associated transcriptional response [141]. BET bromodomain protein inhibition is another epigenetic approach for blocking the Hedgehog pathway at the downstream
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br Material and methods br Results br
2022-01-12
Material and methods Results Discussion In vitro testing is necessary to study DAA activity and putative RASs. Compared to enzymatic assays and replicons, HCV infectious culture systems reflect the full viral life cycle and previous results in these systems reflected clinical data.[13], [14
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Small but statistically significant variance in PhyChem inde
2022-01-12
Small but statistically significant variance in 7 PhyChem indexes measured using intra-host HVR1 variants was shown to be strongly associated with CIP and MIP. All HVR1 sequences (N = 28,622) used here share only 6782 profiles of the selected 29 DAC’ of 7 PhyChem indexes. The significant majority (9
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While phosphorylation site motifs are typically described in
2022-01-12
While PF-04620110 site motifs are typically described in terms of residues that promote phosphorylation, negatively selected residues can also be an important component of substrate recognition. Such ‘forbidden’ resides can act as a filter to prevent phosphorylation of a site by the ‘wrong’ kinase,
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Transcriptional elongation is a checkpoint
2022-01-12
Transcriptional elongation is a checkpoint for productive transcription. In ESCs, ∼50% of the genes enriched for H3K4me3 are initially transcribed but do not enter productive elongation (Guenther et al., 2007, Rahl et al., 2010). Following promoter escape, the transcriptional elongating protein comp
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GLP is known to be expressed in a
2022-01-12
GLP-1 is known to be expressed in a subset of taste bud cells and has been shown to co-localize with GPR120 in the circumvallate papillae [22]. Local GLP-1 regulates taste preference for sucrose [54]. Analogous to intestinal mediation of GLP-1 by GPR120, Martin et al.[22] report induction of GLP-1 s
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In both families GPR A
2022-01-12
In both families, GPR109A mRNA in kidney fat was positively correlated with NEFA as a tendency. A positive correlation between this fat depot and insulin was observed in lean-type cows. In fat-type cows, mesenteric GPR109A mRNA correlated positively with insulin and negatively with urea on a moderat
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Glial cells have emerged as
2022-01-11
Glial cells have emerged as important protagonists of the central nervous system (CNS) physiology (Chen and Swanson, 2003; Kettenmann and Verkhratsky, 2008; Parpura and Verkhratsky, 2012). As widely described in the literature, astrocytes regulate glutamatergic synapses by clearance of glutamate in
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br Treatment KD is currently
2022-01-11
Treatment KD is currently the treatment of choice for GLUT1-DS. It is a high-fat, carbohydrate-restricted diet that mimics the metabolic state of fasting; so, the KD relies an exogenous rather than body fat for ketone production, thus maintaining ketosis without weight loss. As the developing br
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Herein in consider of the high similarity between GR HBP
2022-01-11
Herein, in consider of the high similarity between GR HBP site and AR HBP site, we applied rational drug design strategy to develop AR/GR antagonists based on the chemical structures of antiandrogens and crystal structure of GR. The following bioassay identified Z19 as a dual AR/GR antagonist. Z19 i
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Congenital Gcgr mice exhibit increased hepatic Fgf expressio
2022-01-11
Congenital Gcgr mice exhibit increased hepatic Fgf21 expression and circulating FGF21 levels. Previous studies by other investigators demonstrated that neutralization of circulating FGF21 with specific Calcitriol impairs glucose control in these mice [6]. In addition, the FGF21 analog LY2405319 lowe
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CaCl was from the Radiochemical Centre Amersham
2022-01-11
45CaCl2 was from the Radiochemical Centre (Amersham, UK), NaVO3 was from Reachim (Moscow, Russia). Tetrodotoxin was purchased from Calbiochem, DTNB from Merck, Darmstadt, Germany. Nifedipine was synthesized in the Institute of Drug Research, Modra, Slovakia and was kindly provided by Dr. Zdeno Mahrl
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The pharmacokinetic properties of were amenable to
2022-01-11
The pharmacokinetic properties of 12 were amenable to oral dosing allowing in vivo comparison to 6. Compared to a maximum efficacious dose of 6 (60mg/kg), 12 demonstrated improved glycemic control during OGTT in high-fat fed/STZ treated (HF/STZ) and BDF/diet-induced obesity (DIO) mouse models of typ
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FXa is a vitamin K dependent
2022-01-11
FXa is a vitamin K-dependent serine protease consisting of two chains linked by a disulfide bridge. The heavy chain contains 303 our and the light chain has 139 amino acids. The catalytic triad comprised of Ser195, His57, and Asp102 exhibits the trypsin-like β-barrel structure [12]. The active sit
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br Experimental br Acknowledgments br Human
2022-01-11
Experimental Acknowledgments Human immunodeficiency virus-1 (HIV-1) is the causative agent of acquired immunodeficiency syndrome (AIDS), and without treatment results in a debilitating disease that cripples the immune system of the patient, increasing susceptibility to opportunistic diseases
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