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The eradication of agonist activity in compound
2022-05-11
The eradication of agonist activity in compound was also confirmed in the ex vivo growth hormone (GH) release experiment conducted in isolated primary rat pituitary Sodium Picosulfate as shown in . Compound did not produce any noticeable GH secretion at up to 10μM concentration. It could also ant
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Next we investigated the transfer of peptides and proteins
2022-05-11
Next, we investigated the transfer of peptides and proteins between contacting cells by nano-LC-MS/MS analysis using the fractions corresponding to molecules higher than 3 kDa. The MS data analysis revealed the direct transfer of several labelled peptides between receivers and donors. Labelled pepti
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CO-1686 More recently Dal Peraro and coworkers
2022-05-11
More recently, Dal Peraro and coworkers [38] carried out 4 μs CG MD simulations of GS with six randomly placed C9915-55 peptides embedded into a synaptic plasma bilayer model. This lipid raft model was constituted by 32 different CO-1686 and cholesterol (54.74%). In this study, the authors observed
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Clinical trials of all GSIs have ended
2022-05-11
Clinical trials of all GSIs have ended prematurely, raising the question on our understanding of their target, the γ-secretase/presenilin. Development of compounds to target γ-secretase and reduce Aβ production is complicated by the fact that γ-secretase/presenilin has critical biological function,
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br Conclusion In summary a series
2022-05-11
Conclusion In summary, a series of novel GPR40 agonists bearing phenylpropiolic Terazosin motif with favorable metabolic stability were prepared and evaluated for their activities as GPR40 agonists. Among them, compound 9 was identified as a structurally distinct GPR40 agonist possessing potent a
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br Fenton reaction based nanomaterials for
2022-05-11
Fenton reaction-based nanomaterials for ferroptosis In Fenton reaction, H2O2 is converted by Fe2+ or Fe3+ to highly oxidative ROS (Eqs. (1) and (2)), which is commonly used to catalyze the degradation of refractory organics [34]. Since the tumor microenvironment is characterized by low acidity an
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br Acknowledgements br Introduction Muscle FBPase is very se
2022-05-11
Acknowledgements Introduction Muscle FBPase is very sensitive to AMP inhibition and in the presence of physiological concentrations of this effector in muscle fibres FBPase should be almost completely inactive [1], [2]. Recently, we have presented evidence that, in vitro, muscle aldolase binds
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It is known that microglial function and morphology are clos
2022-05-11
It is known that microglial function and morphology are closely related [20], but no studies have addressed whether neuroinflammation induced by alcohol might modify microglial UNC2881 (i.e. morphology, neuroimmunochemical phenotype) through an eCB-dependent mechanism. Since this alcohol-induced mi
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The HIF complex was initially
2022-05-10
The HIF complex was initially identified as an important component of the cell machinery involved in the response and Flubendazole receptor to hypoxia (Semenza, 2001). Further studies have shown that HIF can also modulate whole-body energy homeostasis by controlling hypothalamic neurons (Varela et
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br Materials and methods br
2022-05-10
Materials and methods Results Discussion I have identified an alternative transcript of the integrin αE gene that is abundantly expressed in testis. In humans, this transcript (hAED) includes part of intron 26 and exons 27, 29, 30, and 31 of the conventional αE gene and Northern analysis in
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In our previous studies examining erectile responses in
2022-05-10
In our previous studies examining erectile responses in sGCα1−/− mice, we found that the sGCα1 subunit was required to obtain proper erectile responses to substances generally known to exert their actions by sGC.17, 18 Based on our previous observation of residual relaxing responsiveness to exogenou
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br Results and discussion GSTP is a
2022-05-10
Results and discussion GSTP1 is a Phase II cytoprotective and detoxifying enzyme. Due to its role in the detoxification of numerous endogenous and exogenous chemical agents (with electrophilic functional groups), individuals with Ile105Val mutation in this gene show enhanced risk of atopic disord
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A number of in vivo
2022-05-10
A number of in vivo studies have investigated the antitumor activity of distinct GSK-3 inhibitors in a variety of cancer cell line-derived tumor xenograft models [14], [21], [22], [24], [33], [39], [40]. These studies utilized toolkit GSK-3 inhibitors as monotherapies. Although inhibition of tumor g
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Differentiation to either Th or Th cells is significantly in
2022-05-10
Differentiation to either Th1 or Th2 etravirine is significantly influenced by the relative expression of T-bet and GATA-3, respectively (Zhu et al., 2006, Jenner et al., 2009). T-bet acts as a key regulator of Th1 cell fate determination and directly activates IFN-γ and suppresses IL-4 (Szabo et a
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Little is known about the role of GPR in physiology
2022-05-10
Little is known about the role of GPR35 in physiology and pathology. Using GPR35 knockout and wild-type mice showed that GPR35 activation by KYNA improves energy metabolism and inflammation, while demonstrated that GPR35 plays an important role in the development of angiotensin II-induced hyperten
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