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br Discussion One binding site MB Fig is located in
2023-04-25
Discussion One binding site, MB327-1 (Fig. 4) is located in the extracellular domain between the γ and α subunits. MB327 adopts an extended conformation in the MB327-1 site and is oriented parallel to the channel. The second putative binding site, MB327-2 (Fig. 4) is situated deep inside the chan
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Compounds are representatives of an array of MBG targets rel
2023-04-25
Compounds – are representatives of an array of MBG targets (, ) related to imidazole standard that were synthesized and initially tested in a rat CYP17 lyase screening assay (). The inhibitors were synthesized as racemates by coupling of 6,7-dimethoxy-naphthalene-2-isopropyl ketone with the requisit
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The most potent compounds within the current series
2023-04-25
The most potent compounds within the current series of compounds were therefore , , , , and , with L-Kynurenine possessing the best selectivity towards the lyase reaction in comparison to the hydroxylase reaction, indeed, this compound was found to possess an IC value of 1210nM against the 17α-OH
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Schisandrol B Stroke also known as a cerebrovascular
2023-04-25
Stroke, also known as a cerebrovascular accident or Schisandrol B attack, is one of the leading causes of death and disability worldwide (Haley et al., 2017; Hankey, 2017; Lie et al., 2017). According to the data released by the World Health Organization (WHO), stroke occurs every 5 s worldwide (WH
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74 9 synthesis Aurora kinases were initially identified as p
2023-04-25
Aurora kinases were initially identified as protein kinases essential for error-free chromosome segregation during mitosis and meiosis. Aurora A appears to control premetaphase events, such as bipolar spindle assembly 3, 4, with Aurora B and C directing metaphase and postmetaphase events, including
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Receptor Subtypes and Their Function Critical Appraisal Larg
2023-04-24
Receptor Subtypes and Their Function – Critical Appraisal Largely unselective ligands of the benzodiazepine binding site, such as diazepam, are known to elicit a wide range of in vivo effects including hypnosis, sedation, anxiolysis, and muscle relaxation. Genetically modified mice were introduced
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Despite functional studies demonstrating the role of HT in
2023-04-21
Despite functional studies demonstrating the role of 5-HT in ureteral contractility, the source of endogenous 5-HT in the ureter is unclear. Since 5-HT-containing enterochromaffin cells, which are present in the gastrointestinal tract, could not be found in the ureter (Nocito et al., 2007, Ripoche,
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The AChR is composed of five homologous membrane spanning su
2023-04-20
The AChR is composed of five homologous, membrane-spanning subunits. AChRs containing two α, one β, one δ and one γ subunit (AChRγ) predominate during embryonic development and mice lacking AChRγ die at birth (Takahashi et al., 2002). After birth, the AChRγs are replaced during the first 2 postnatal
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br AD and COX LOX pharmacology Early studies
2023-04-20
AD and COX/5-LOX pharmacology Early studies on the role of cyclooxygenases in AD were inspired by epidemiological data suggesting that COX inhibitors such as nonsteroidal anti-inflammatory drugs (NSAIDs) could be beneficial in AD patients (Lucca et al., 1994, McGeer et al., 1990). This line of re
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Whereas more research is needed to identify
2023-04-20
Whereas more research is needed to identify the precise mechanism by which FIN exerts its antidyskinetic effect, the 4-P-PDOT that it can negatively modulate dopaminergic transmission is also supported by our previous findings. Indeed, we have previously shown that FIN completely reversed the behav
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Aurora A or B selective and
2023-04-20
Aurora -A or -B selective and pan-aurora inhibitors have demonstrated different preclinical and clinical therapeutic efficacies [2,[19], [20], [21], [22], [23]]. For example, clinical trials for a pan-Aurora inhibitor VX-680 (developed by Vertex) were halted at phase II for toxicity reasons (one cas
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Thiazole heterocycles constitute an interesting class of mol
2023-04-20
Thiazole heterocycles constitute an interesting class of molecules, which exhibit a broad spectrum of biological activity, including antifungal properties [[16], [17], [18], [19]]. Encouraged by our previous study that describes the activity of hydrazine-thiazole derivatives against C. gattii and C.
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Recent studies have supported the existence of
2023-04-20
Recent studies have supported the existence of an inward RAS regulatory mechanism in which AT1 receptors downregulate angiotensin-converting enzyme 2 (ACE2) and subsequently impair angiotensin-(1-7) generation and MAS functionality (Jessup et al., 2006, Gallagher et al., 2008, Xia et al., 2009, Pern
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Nogo-66 (1-40) sale How do increased levels of ammonia as ob
2023-04-20
How do increased levels of ammonia as observed in clinical HE constrain synaptic plasticity? Numerous studies have investigated the modulation of signal transduction pathways activated in LTP or LTD irrespective of being necessary or sufficient for changes in synaptic efficacy (Wen et al., 2013). Ye
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Changes in actin microfilaments are mediated by changes in e
2023-04-19
Changes in DOI hydrochloride mg microfilaments are mediated by changes in extracellular matrix, mechanical stimulation or growth factors intracellular signaling. We observed significant changes in a number of intracellular signaling pathways associated with changes in actin dynamics during hMSCs di
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