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Compounds were profiled for their inhibitory activity
2023-09-14
Compounds – were profiled for their inhibitory activity against dipeptidyl peptidase-IV Activity and/or Structure Homologues (DASH) [e.g. DPP2, DPP8 and DPP9] and non-DASH [eg. post-proline cleaving enzyme (PPCE), neutral endopeptidase (NEP), aminopeptidase P (APP), aminopeptidase N (APN)] enzymes.
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Numerous studies have reported high glutamate levels
2023-09-14
Numerous studies have reported high glutamate levels in the brains of patients with depression, indicating that the glutamate system plays a crucial role in depression (Sanacora et al., 2004; Kendell et al., 2005; Hashimoto et al., 2007). Furthermore, several clinically effective antidepressant drug
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Thus phosphorylation of p was used to measure the
2023-09-14
Thus, phosphorylation of p38 was used to measure the intracellular potency of ASK1 inhibitors. In this assay, HEK293/AP-1luc EW-7197 expressing human full-length ASK1 were incubated with compound for 18 h and then lysed and the level of phospho-p38 was quantified using the HTRF assay [33]. Result
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Previous investigations have established that aromatase
2023-09-14
Previous investigations have established that aromatase activity is regulated via two different pathways in a tissue-specific manner. The first is a slower transcription regulatory pathway that involves an alteration in gene transcription and represents what is classically thought of as the way by w
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In our approach using BRET
2023-09-14
In our approach using BRET and FRET, there is a substantial increase in BRET and FRET signals between Giα2 or Giα3-YFP and CFP- Gγ2/Rluc-Gγ2 upon apelin-13 activation, indicating that Gαi2, Gαi3 and N-terminus of Gβ1γ2 subunits become closer without subunit dissociation. In contrast, both the FRET a
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Apelin APJ triggers a variety
2023-09-14
Apelin/APJ triggers a variety of cellular signaling pathways (Fig. 1). Recent studies from our laboratory showed that apelin-13 induces vascular smooth muscle cell (VSMC) proliferation by the upregulation of Cyclin D1 expression, which is involved in an ERK-dependent activation of Jagged-1/Notch3 si
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The PDZ domains of DLG interact with tumor suppressor protei
2023-09-14
The PDZ domains of DLG interact with tumor suppressor proteins, APC and PTEN, as well as with several viral oncoproteins such as the E6 protein present in oncogenic human papillomavirus (reviewed in [177]). It has been reported that overexpression of DLG in fibroblasts impairs the events in the G0/G
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br Introduction Hepatocellular carcinoma HCC is the third le
2023-09-14
Introduction Hepatocellular carcinoma (HCC) is the third-leading cause of cancer-related death worldwide and accounts for 70–85% of all liver cancer diagnoses [1]. In East and South-East Asia, the occurrence of HCC and the related number of fatalities have gradually increased in recent decades [2
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Cell surface metalloproteases coordinate signaling
2023-09-13
Cell surface metalloproteases coordinate signaling during development, tissue homeostasis, and disease. A disintegrin and metalloprotease 17 (ADAM17) is a well-characterized member among ADAM family, which mediates the cleavage of various cell surface proteins (Black, 2002, Black et al., 1997, Dello
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br Introduction Chronic kidney disease
2023-09-13
Introduction Chronic kidney disease (CKD) is a worldwide public health problem. This problem is even worse in socioeconomically deprived countries because lower income and social deprivation are associated with higher incidence of reduced GFR, progressive kidney function loss and end stage renal
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Although several ARIs have reached various phases
2023-09-13
Although several ARIs have reached various phases of clinical experimentation however most of them have been withdrawn either due to an insufficient bioavailability, their poor efficacy or adverse side effects. Currently Epalrestat is in clinical use for the treatment of diabetic neuropathy. The sid
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br Downstream signalling of AKT A consensus phosphorylation
2023-09-13
Downstream signalling of AKT A consensus phosphorylation motif has been described for AKT substrates: R-X-R-X-X-S/T-B where X represents any amino JANEX-1 and B represents bulky hydrophobic residues (Alessi, Caudwell, Andjelkovic, Hemmings, & Cohen, 1996). Numerous AKT substrates have been publi
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To validate the identified phosphorylation sites
2023-09-13
To validate the identified phosphorylation sites in the mouse heart, we analyzed HEK 293T LY2874455 transfected with Adrb1 based on the hypothesis that protein residues phosphorylated both in vivo and in vitro are more likely to be physiologically relevant. All of the phosphorylation sites identifi
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The anorexic effect observed when AR is infused into the
2023-09-13
The anorexic effect observed when AR231630 is infused into the VTA could be the result of the DA release inhibition, as previously described [11]. However, there is also a hedonic aspect in feeding that possibly involves dopaminergic mechanisms of reward. Helm et al. showed a functional link between
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br Functional consequences of ADK regulation
2023-09-13
Functional consequences of ADK regulation on astrocyte function As outlined above (see introduction), ADK critically regulates the extracellular adenosine levels in TNP-470 (Boison, 2006, Etherington et al., 2009). Changes in the levels of adenosine, as a result of the regulation of ADK expressi
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