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br Regulatory mechanisms of ASK activity
2025-01-02

Regulatory mechanisms of ASK1 activity The functions of ASK1 in disease ASK1 inhibitor As mentioned above, ASK1 plays a pivotal role in the pathogenesis of various diseases; hence, an ASK1 inhibitor has therapeutic potential. Although inhibitors of the ASK1 downstream kinases p38 and JNK ar
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br Acknowledgements This work was supported by the Victorian
2025-01-02

Acknowledgements This work was supported by the Victorian Government Operational Infrastructure Support Program. KAB is supported by the Mavis Robertson Fellowship from the National Breast Cancer Foundation (NBCF; ECF-16-004), by an NBCF Novel Concept Award (NC-14-011), and by NHMRC project grant
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At the top of the S
2025-01-02

At the top of the S1 subsite cylinder are two “cap” residues: E572 and M1034 [13]. Atomic structures of PfA-M1 have revealed important clues into potential roles for the cap residues in substrate selection. In the PfA-M1:bestatin co-crystal structure ([13]; Fig. 1), the P1 phenyl ring occupies the S
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br Materials and methods br Results br Discussion
2024-12-31

Materials and methods Results Discussion In the present study, we identified HBP1 as a novel substrate of AKT. This was demonstrated by in vitro phosphorylation assays and western blotting using phosphosite-specific antibodies. Three sites were identified by mass spectrometry and mutagenesi
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To further clarify the vascular cell types expressing
2024-12-31

To further clarify the vascular cell types expressing AR subtypes, double immunofluorescence staining for ARs and vascular endothelial EZH2 negative control or vascular smooth muscles was performed. As shown in Fig. 3, Fig. 4, overlay images show the expression of all ARs subtypes that we examined i
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Ibandronate sodium synthesis Targeting the BCR is the ideal
2024-12-31

Targeting the BCR is the ideal strategy to identify the antigen reactive B cells. However, there is concern that B cells could be activated when BCR are bound and cross-linked by antigens, a possibility that is obviously negative for the treatment of autoimmune disease. Proby et al. (2000) tried to
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Based on the improved characteristics of
2024-12-31

Based on the improved characteristics of the mutant ECDs we proceeded to crystallization trials, starting with the β1-BPloop as the most promising. We obtained rod shaped hexagonal crystals reproducibly, but with moderate diffraction ability (Fig. 5). Furthermore, the crystals were sensitive in mou
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However although in vitro studies in heterologous systems ha
2024-12-31

However, although in vitro studies in heterologous systems have provided very important indications of potential novel pharmacology, the studies with endogenous receptors in native tissues are essential to provide evidence for GPCR heteromerization in vivo and to confirm its physiological relevance.
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Chronic inflammation is associated with both initiation and
2024-12-31

Chronic inflammation is associated with both initiation and progression of many neoplastic conditions [149], and ATX may be a player in the process. ATX/LPA signaling is positively correlated with the invasive and metastatic potential of several cancers including melanoma, breast cancer, ovarian can
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exemplifies three of the compounds investigated in
2024-12-31

exemplifies three of the compounds investigated in the selection for a candidate drug (CD). Our first criteria was an IC The HU 308 as such did not show any genotoxicity in the SOS/umu assay, but this does not say anything about any possible genotoxicity of its metabolites or degradation products.
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In addition to pH regulation by ion counter
2024-12-31

In addition to pH regulation by ion (counter-) fluxes, acidification is regulated by the abundance of V-ATPase on organelles, by the pumping activity of the complex and by proton leakage. In yeast, the V-ATPase VO subunit a is the only subunit expressed in two isoforms termed Stv1p and Vph1p. V-ATPa
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In HepG cells compound showed
2024-12-31

In HepG2 cells, GSK-LSD1 hydrochloride showed inhibition of total lipid syntheses with an IC of 8μM. A cell based Alamar Blue cytotoxicity assay was used in parallel to differentiate the effect on the inhibition of lipid synthesis versus potential cytotoxicity. Under identical incubation conditions,
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Additionally we used the predicted Cyp a
2024-12-31

Additionally, we used the predicted Cyp19a1b amino Moniliformin sodium salt sequence from a number of bony fish species to infer their genetic relatedness and found that R. quelen occupies an ancient position within the Siluriformes group. A phylogenetic tree was constructed and it included both fu
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br Androgen interference with the action of arachidonic acid
2024-12-30

Androgen interference with the action of arachidonic Ketoconazole metabolites’ actions; the other side of the coin Arachidonic acid, being a polyunsaturated fatty acid present in the phospholipids of the membrane of cells, is highly abundant within the organism. It is mainly involved in cellular
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mu opioid receptor antagonist The association of male gender
2024-12-30

The association of male gender with increased atherosclerosis has stimulated interest in the role of androgen signalling in this condition. Androgens act (Fig. 2) by direct activation of androgen receptor (AR), a nuclear receptor that acts as a ligand-regulated transcription factor (Gao et al., 2005
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