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Using constant potential amperometry and electrochemical enz
2022-11-04

Using constant potential amperometry and electrochemical enzyme-based biosensors selective for choline—and, therefore, an accurate readout of motilin receptor release (Baker et al., 2015; Bruno et al., 2006a; Parikh et al., 2004, 2007)—tonic and phasic release of acetylcholine were measured simulta
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In young animals the HT A receptor
2022-11-04

In young animals, the 5-HT2A bcl-2 inhibitor antagonist ketanserin, at relatively low concentrations, shifted 5-HT concentration-response curves rightward, suggesting a role for 5-HT2A receptors in mediating 5-HT-induced contractions of the ureter. The slopes of the ketanserin Schild plots for the
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The knowledge on the structure of CYP including its active
2022-11-04

The knowledge on the structure of CYP17, including its active site, provides a rationale for understanding many mutations that are found in enzyme dysfunction in clinical disease as well as the enzyme's dual hydroxylase and lyase catalytic capabilities. This knowledge will assist rational drug desig
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Moreover showed reduction in fibroblast growth factor
2022-11-04

Moreover, showed 73% reduction in fibroblast growth factor–induced neovascularization in a mouse corneal micropocket assay at a dose of 100mg/kg and 50% reduction at 50mg/kg. Both results were highly statistically significant (PABT have recently shown only moderate efficacy (40% inhibition) in an A
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br Introduction Stroke is a devastating condition that cause
2022-11-04

Introduction Stroke is a devastating condition that causes cognitive and motor dysfunction, neurodegenerative diseases and even acute death, and is a leading cause of mortality and morbidity worldwide (Chen et al., 2014a, Wang et al., 2016). Thus, exploration or identification of novel therapeuti
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Roles of Aurora kinases in
2022-11-04

Roles of Aurora kinases in directly activating multiple oncogenic pathways and promoting proliferation as well as transformation have also been demonstrated. Aurora-A has been shown to up-regulate telomerase reverse transcriptase mRNA through c-myc [26]. The kinase was also implicated in activating
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exemplifies three of the compounds investigated in the selec
2022-11-04

exemplifies three of the compounds investigated in the selection for a candidate drug (CD). Our first criteria was an IC rapamycin buy 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 produc
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However joint reviews and the consensus from experts offer d
2022-11-03

However, joint reviews and the consensus from experts offer disparate recommendations with regard to their management in the context of anesthesia, whereas some reviews [6], [7] set out certain doubts regarding their use during the perioperative period. On the other hand, the guidelines for the mana
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br Conclusions Our study confirms that N terminal mutations
2022-11-03

Conclusions Our study confirms that N-terminal mutations can affect Aβ fibril and oligomer formation, despite lying outside the core amyloid region of Aβ. Of the three factors that may influence Aβ-mediated toxicity (primary structure of Aβ, assembly structure and cellular responses), our results
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Most intriguingly however there was no change
2022-11-03

Most intriguingly, however, there was no change in basal glutamatergic neurotransmission despite a loss of about half of the neuronal AMPAR population. Highest levels of ammonia did neither affect the amplitude nor the frequency of AMPAR mediated mEPSCs. As revealed by our recordings from somatic ou
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In this study PRP positively regulated MIIP
2022-11-03

In this study, PRP4 positively regulated MIIP levels and significantly inhibited the invasion of HCT116 cells. Further investigations elucidated that PRP4 dephosphorylated MIIP via PP1A regulation, which was confirmed by PP1A inhibition in the presence of OA. Upon dephosphorylation, MIIP possibly in
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Regarding the HT B receptors they act as terminal
2022-11-03

Regarding the 5-HT1B receptors, they act as terminal receptors and are involved in the presynaptic regulation of the release of 5-HT. But at spinal level these receptors are principally situated post-synaptically (Sari, 2004). The ability of autoreceptors to regulate extracellular levels of 5-HT dur
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Finasteride has been shown to be a mechanism
2022-11-03

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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A rational approach for the design of new steroid
2022-11-03

A rational approach for the design of new steroid compounds as possible competitive inhibitors of CYP17 include chemical modification at C17 of the enzyme's natural substrates, pregnenolone (1) and progesterone (2), introducing groups with moderate to strong dipole properties at C20, such as oxime a
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The present study indicates elevated ATX activity as a
2022-11-03

The present study indicates elevated ATX activity as a highly sensitive and specific biomarker to differentiate ICP from other pregnancy-related liver disorders or pruritic dermatoses. In Neurotensin to the current gold standard for diagnosis, total fasting serum bile salt levels, ATX appeared as a
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