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Activity of compound in rat brain
2022-01-28

Activity of compound 10 in rat N1-Methylpseudouridine tissue highlights the potential to use this new class of allosteric sGC inhibitors to study the role of the NO—sGC—cGMP signalling pathway in the brain. Reducing amounts of cGMP in cells would have implications in downstream signalling proteins,
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In addition for the function of GSNOR
2022-01-28

In addition, for the function of GSNOR in brain, since GSNOR is the sole alcohol dehydrogenase isozyme in brain, the failure to detect ethanol dehydrogenase activity poses a problem if it is assumed that this enzyme has evolved and developed as a protective mechanism for ethanol detoxification in th
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The existence of EAAT subtypes raises obvious questions as
2022-01-28

The existence of 5 EAAT subtypes raises obvious questions as to the cellular and anatomical distribution of the various transporters (for review, see Gegelashvili & Schousboe, 1998, Danbolt, 2001). While difference in techniques (i.e., protein vs. mRNA), reagents, and preparations (i.e., in vivo vs.
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In general fish has a limited ability for digestion and
2022-01-28

In general, fish has a limited ability for digestion and metabolism of carbohydrate though carbohydrate is the cheapest dietary energy and carbon source to animals and the best candidate for replacing dietary protein (Enes et al., 2009, Kamalam et al., 2017, Wilson, 1994). Furthermore, the analysis
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br Vertebrate steroid receptor evolution br Conclusion
2022-01-28

Vertebrate steroid receptor evolution Conclusion The teleost WGD event resulted in the duplication of the vertebrate GR and MR and two GRs have been retained in the majority of teleost fish studied so far. The molecular basis for this retention has yet to be fully understood. The cloning of th
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br Results br Discussion secretase mediated proteolysis
2022-01-27

Results Discussion γ-secretase-mediated proteolysis of integral membrane proteins is required for diverse biological processes (Lal and Caplan, 2011). One γ-secretase target of particular interest is Notch, as recent work has shown Notch activity to be increased in obesity and associated metab
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We have previously designed an azobenzene based molecule Raz
2022-01-27

We have previously designed an azobenzene-based molecule, Razo, which could switch the conformations of G-quadruplex structures by photoregulation. 12, 13, 14, 15 However, it lacks selectivity to different G-quadruplexes. Therefore, we want to find a way to modify this molecule so that it could be u
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BDNF is intricately implicated in energy homeostasis Hamdouc
2022-01-27

BDNF is intricately implicated in energy homeostasis (Hamdouchi et al., 2016; Schwartz and Mobbs, 2012), regulation of mood (Sartorius et al., 2015) and adult neurogenesis (Taliaz et al., 2010; Waterhouse et al., 2012), our primary focus was to evaluate the effects of GPR40 stimulation on BDNF expre
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Free fatty acids FFAs which are
2022-01-27

Free fatty acids (FFAs), which are obtained from dietary fat or endogenous synthesis, function as nutrients and signaling molecules. Studies have shown that free fatty Z-IETD-FMK receptors 1–4 which are G-protein coupled receptors, bind free fatty acids and serve as receptors for these FFAs. Short
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To date three other allosteric binding sites of
2022-01-27

To date, three other allosteric binding sites of HIV-1 IN have also been reported. In the work of Wielens and co-workers [33], a pocket formed by the residues Tyr83, Trp108, Asn184, Ile200 and Val201 was found, which can be bound by small molecules. In the work by Rhodes et al. [34], a small-molecul
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Arena Pharmaceutical introduced a biaryl sulfone
2022-01-27

Arena Pharmaceutical introduced a biaryl sulfone derivative with antagonistic activity at H3Rs known as APD-916, ((R)-1-(2-(4'-(3-methoxypropylsulfonyl)biphenyl-4-yl)ethyl)-2-methylpyrrolidine), which was rationally designed from corresponding sulfonamides in order to yield compounds with short dura
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Taken together this study provides the proof of concept that
2022-01-27

Taken together, this study provides the proof of concept that our novel heterologous human/rat HER2-specific T cell vaccine HuRt-TEXO, which is capable of stimulating both humoral and CTL responses leading to potent antitumor immunity through the circumvention of HER2 tolerance in double transgenic
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We acknowledge some important limitations to the study Given
2022-01-27

We acknowledge some important limitations to the study. Given that SEER is a national database of abstracted clinical information, there is selection bias as to which patients underwent RS testing. As clinicians are selecting which patients to test, the RS distributions may not reflect the true dist
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Oltipraz has been shown to inhibit the
2022-01-27

Oltipraz has been shown to inhibit the growth of HCC orexin a and is being evaluated in clinical trials as a potential anti-cancer drug for HCC (Mann et al., 2009; Piton et al., 2005; Yates and Kensler, 2007). The present observation that pre-treatment of tumorigenic liver cells with oltipraz cause
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To identify structurally novel autophagy inhibitors a medium
2022-01-27

To identify structurally novel autophagy inhibitors, a medium throughput screen of our in-house library of approximately 160,000 compounds was performed. In the screening assay, MCF7 6 mercaptopurine stably transfected with eGFP-tagged light chain 3 (LC3), were employed, which can be detected by au
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