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From an historical perspective ligands for GPCRs adrenaline
2024-08-20
From an historical perspective, ligands for GPCRs (adrenaline, serotonin, Pentamidine dihydrochloride or morphine, to name a few) have been identified before their receptor counterparts, at a time when the concept of receptor itself was controversial [15]. Although many cognate receptors for endoge
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Many coumarin derivatives can be found in nature There
2024-08-20
Many coumarin derivatives can be found in nature. There are more than 1300 types of those purely derived from plants, and if synthetic products are included, their number is immeasurable. According to the earliest existing records extant, herbs containing Psoralen-type compounds, e.g., methoxsalen,
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br Physiology of the apelin pathway br Role of apelin
2024-08-20
Physiology of the apelin pathway Role of apelin in heart disease Both apelin and apelin receptor null mice manifested moderate reduction in cardiac contractile function under basal conditions and their exercise capacity was markedly reduced (Table 1) [56]. Apelin has direct effects on the prop
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Plasma apelin levels predict the major cardiovascular event
2024-08-20
Plasma apelin levels predict the major cardiovascular event after percutaneous coronary intervention in patients with ST elevation myocardial infarction (STEMI), and adverse events are higher in patients with lower plasma apelin levels [75]. Apelin and its receptor are markedly upregulated in the he
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IKK Inhibitor VII Abnormalities in placentation in patients
2024-08-20
Abnormalities in placentation in patients with PE appear to be associated with changes in different components of the signaling pathway that mediates cytotrophoblast migration/invasion. Studies have showed that the activation of the Notch signaling pathway is associated with the differentiation and
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Calcium entry through postsynaptic NMDARs activates intracel
2024-08-20
Calcium entry through postsynaptic NMDARs activates intracellular signaling cascades including Ca2+/calmodulin (CaM)-dependent protein kinase II (CaMKII) and calcineurin. The spatiotemporal abundance of this Ca2+/CaM complex determines the direction of synaptic plasticity, resulting in LTP (Malinow
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CCT137690 br Concluding remarks Enhanced membrane binding up
2024-08-20
Concluding remarks Enhanced membrane binding upon calcium stimulation in CCT137690 suggests a pre-requisite step that involves a conformational change in LOX. This might facilitate it to tether to the membrane and regulate enzyme activity. The calcium binding loops and the putative active site e
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br Materials and methods br Results and discussion br
2024-08-20
Materials and methods Results and discussion Conclusions In this study, for the first time to the best of our knowledge, the stability of pure hsALDH has been studied under various conditions. The enzyme exhibited low storage stability both at 4°C and 25°C, which could be improved to a good
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br Concluding Remarks and Future Perspectives br
2024-08-20
Concluding Remarks and Future Perspectives Disclaimer Statement Introduction Aldehyde dehydrogenase ALDHs (E.C. 1.2.1.3) are multigene family of NAD(P)+-dependents group of structurally and functionally related ubiquitously distributed enzymes involved in the specific and irreversible oxida
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In order to get a better understanding of
2024-08-20
In order to get a better understanding of this synergy, we tested the effect of preliminary incubation of galunisertib with non-stimulating concentrations of gonadotropins or FSK before subsequent stimulation by FSK or gonadotropins alone, also at sub-stimulating concentrations. We observed that hu
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br Regulation and pharmacology of mPGES
2024-08-19
Regulation and pharmacology of mPGES-1 mPGES-1 (16 kDa, 152 amino acids) is a trimeric integral membrane protein of the endoplasmic reticulum with each monomer containing four transmembrane domains (Samuelsson et al., 2007; Sjogren et al., 2013). The three active site cavities are located at the
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The inhibition of the exacerbated inflammatory
2024-08-19
The inhibition of the exacerbated inflammatory response that follows injury may be an alternative approach to induce a more efficient repair [17,83]. In line with that, 5-LO is one of the most consolidated targets for dampening inflammation, mainly through the therapeutic effects of 5-LO inhibitors
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The synthetic route for the aminobenzoxazole scaffold
2024-08-19
The synthetic route for the aminobenzoxazole scaffold with a solvent accessible moiety is described in . Nitration of methoxyphenol and subsequent hydrogenation of the resulting nitro ack1 inhibitors afforded compound . Aminobenzoxazole was formed by the reaction of compound with BrCN in EtOH. Th
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The Limitations of our data include
2024-08-19
The Limitations of our data include the absence of functional/behavioral assessments and lack of direct comparison with females which would require additional studies and conceivably support sex-specific interventions for stroke [50]. Competing interests Acknowledgements This study was suppor
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br Experimental br Acknowledgment This paper was financially
2024-08-19
Experimental Acknowledgment This paper was financially supported by the Project Funded by China Postdoctoral Science Foundation (2017T100186), Natural Science Foundation of Liaoning Province (20170540858), General Scientific Research Projects of Department of Education of Liaoning Province (20
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