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Finasteride has been shown to be a mechanism based inhibitor
2022-11-08
Finasteride has been shown to be a mechanism-based inhibitor of 5AR-2 [9]. Finasteride acts as an alternate substrate for 5AR-2 and is initially bound in an extremely stable enzyme-bound NADP-dihydrofinasteride adduct which is ultimately processed to dihydrofinasteride. The NADP-dihydrofinasteride a
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Evidences have suggested that impairment of CK
2022-11-08
Evidences have suggested that impairment of CK activity contributes to inhibition of Na+, K+-ATPase and H+-ATPase activities during infectious diseases, since these ATPases are dependent of ATP, as observed by Baldissera et al. [31] in fish experimentally infected by Aeromonas caviae. We observed th
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In addition to drawing attention to Ser
2022-11-08
In addition to drawing attention to Ser454 of ACL as a phosphosite that is regulated by both BDK and PPM1K, our phospho-proteomics screen identified several additional sites in other proteins. For example, Ser25, Ser29, and Ser79 of the lipogenic enzyme acetyl-coA carboxylase 1 (ACC1) were found to
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Production of reactive oxygen species ROS during
2022-11-08
Production of reactive oxygen species (ROS) during RSV infection is one the important ways that neutrophils can injure the lungs [2], [24], [25]. Lipoxygenases are considered as an important source of producing ROS inside the MAPK Inhibitor Library sale [26]. Several studies have indicated that the
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The downstream targets of ATR involved in
2022-11-08
The downstream targets of ATR involved in mediating human telomerase recruitment have not yet been identified. Under stalled fork conditions, activated ATR is able to phosphorylate and activate ATM (Stiff et al., 2006, and Figures 4C and 4D); whether this HOBt of ATM participates in a positive feedb
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We also showed that steatosis induced
2022-11-08
We also showed that steatosis induced an additional increase of ASK1 activation that was associated to the exacerbation of hepatocyte and liver damage and was unrelated to ER stress. Indeed, several settings, also different to ER stress, can induce ASK1 activation and many of them involve oxidative
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The structural analysis of the ASK activation segment which
2022-11-08
The structural analysis of the ASK1 activation segment, which was not phosphorylated in the crystal structure, showed interactions mimicking those found in activated kinases. In addition, the isolated unphosphorylated ASK1-CD is active and able to autophosphorylate itself at three sites, Thr813, Thr
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Sorafenib was the first small RTK
2022-11-07
Sorafenib was the first small RTK inhibitor drug to be developed and was initially approved against renal cell carcinoma, then against hepatocellular carcinoma (HCC) and more recently for differentiated thyroid treatment [111]. Sunitinib soon followed, being approved for gastrointestinal stromal tum
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br Materials and methods br Results br Discussion Diabetic k
2022-11-07
Materials and methods Results Discussion Diabetic kidney disease (DKD) is the most common cause of end-stage renal disease [15], [16]. The pathogenesis of DKD is not fully understood, and there is no effective treatment. Although previous studies suggested that early lesions of DKD are foun
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In addition a substantial knowledge has
2022-11-07
In addition, a substantial knowledge has been gained about the main properties of AT1R, such as ligand preference, signaling, regulation, and trafficking. However, it is less known how AT1R and other plasma membrane receptors affect each other’s function, and how these crosstalk mechanisms can be ut
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Tephrosia purpurea Linn pers Fabaceae a
2022-11-07
Tephrosia purpurea (Linn.) pers, (Fabaceae), a widely growing herbaceous perennial is reported to exhibit significant anti-hyperglycemic activity in animal models [7], [8], [9] as well as able to delay the development of diabetic complications [10], [11]. Recently, we have reported T. purpurea for i
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Nrf br AhR br Nrf and
2022-11-07
Nrf2 AhR Nrf2 and AhR: friends or foes for energetic metabolism? Perspectives in carcinogenesis upon xenobiotic exposure Acknowledgements Introduction Integration of endogenous and exogenous signals via appropriate receptors is at the core of biological differentiation and adaptive r
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The results also showed that the A receptor http www
2022-11-07
The results also showed that the A3 receptor agonist increased the phosphorylated levels of Akt, leading to activation of the PI3K/Akt pathway. A3 BAY 80-6946 stimulation has protective effects against RGC death following ischemia-reperfusion, glutamate toxicity, and optic nerve transection models
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Control of retinal vascularization during development and OI
2022-11-07
Control of retinal vascularization during development and OIR likely involves close interactions among endothelial cells, neurons and glial benfotiamine (microglial and astrocytes) (see Fig. 2). In particular, the interaction between endothelial tip cells and astrocytes plays a critical role in deve
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To our knowledge BAY has not progressed to clinical developm
2022-11-07
To our knowledge, BAY 60-6583 has not progressed to clinical development and remains to be the only ADORA2B agonist that has been developed.33, 34 Further development of similar compounds would be beneficial in future fibrosis research. One of the limitations of our study is being limited to in vit
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