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Finally worth of mention are few papers
2022-02-15
Finally, worth of mention are few papers that report on the discovery of HO-2 selective inhibitors. In 2013, starting from the screening of a carbenoxolone library, the above-mentioned Canadian research group identified Clemizole (Table 6) as a new hit compound for the development of the first seri
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br Introduction The replacement of a regular
2022-02-14
Introduction The replacement of a regular intake of healthy oils and fibres for a diet based substantially on high fat- and high sugar-content foods has had profound consequences for public health. These changes in the way that the populations of high income, particularly Western countries, manag
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br Results and discussion br Conclusions In summary we gener
2022-02-14
Results and discussion Conclusions In summary, we generated analogues of the hit compounds 1–3, studied their structure–activity relationships, and created a series of highly potent GPR55 agonists. The most potent agonists among the series were 17a-b, 17e, 17g and 17l with EC50 values below 10
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As preclinical toxicity and efficacy both appear to be assoc
2022-02-14
As preclinical toxicity and efficacy both appear to be associated with GlyT1 inhibition, it remains to be determined whether on-target toxicity can be separated from efficacy. The present study evaluated a series of GlyT1 inhibitors for target potency, mode of inhibition, residence time, activity in
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Introduction The hypoglossal nucleus is the nucleus
2022-02-14
Introduction The hypoglossal nucleus is the nucleus of the twelfth cranial nerve and is located on both sides of the mid line in the dorsal medulla oblongata and is situated between the proximal end of the medullary central canal and the beginning of the fourth ventricle (Tomasch and Etemadi, 1962)
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Here we reported series of carbohydrate modified compounds c
2022-02-14
Here, we reported series of carbohydrate-modified compounds containing a dibromo substituted benzene ring which was derived from the red alga (). The conformation flexibility of Carboplatin and their polyol structures give them many unique biological properties as we have described earlier. More i
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Post translational modifications of the GR can
2022-02-14
Post-translational modifications of the GR can alter the transcriptional effects of GR activation [31], and may provide a mechanism for the interactions between cell signaling pathways and GR-mediated transcriptional activity. Dex-BSA treatment reportedly increased p38 MAPK activation in CD14-positi
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In the gastrointestinal GI tract CART expression has been
2022-02-14
In the gastrointestinal (GI) tract CART expression has been described in the enteric nervous system in rats (Ekblad et al., 2003), pigs (Wierup et al., 2007), sheep (Arciszewski et al., 2009), guinea pigs (Ellis and Mawe, 2003) and humans (Kasacka et al., 2012). Less is known about CART expression i
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Picrotoxin br Short Communication Lactococcus lactis is trad
2022-02-14
Short Communication Lactococcus lactis is traditionally used as a starter culture in the production of fermented dairy food products, such as cheese, sour cream, and buttermilk (Cavanagh et al., 2015). Two main pathways of lactose uptake and metabolism have been described for L. lactis. In the fi
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In perimenstrual catamenial epilepsy there is emerging
2022-02-14
In perimenstrual catamenial epilepsy, there is emerging evidence to suggest that P withdrawal plays a key role in seizure exacerbations occurring around the time of menstruation (Backstrom et al., 1984, Bonuccelli et al., 1989, Scharfman and MacLusky, 2006). The mechanisms underlying ovarian cycle-r
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Compound and several additional FPR antagonists
2022-02-14
Compound 10 and several additional FPR1 antagonists identified here specifically blocked fMLF-induced responses mediated via FPR1 in FPR1-HL60 l-name and human neutrophils, but not responses mediated via FPR2 or FPR3 (in human neutrophils and transfected HL60 cells) or Fpr1 (murine neutrophils and
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Integrin engagement triggers activation of several signaling
2022-02-14
Integrin engagement triggers activation of several signaling pathway including Fak, which is recognized as the key signal transduction factor in the integrin signaling pathway that functions by activating downstream signaling in focal adhesion plaques. Whether changes in integrin-FAK signaling pathw
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Our results further indicate that low expression of p CBP
2022-02-12
Our results further indicate that low expression of p300/CBP in CRC is directly associated with poor clinical therapeutic outcome of 5-FU treatment, potentially providing a new set of biomarkers to predict chemo-sensitivity. Although the ability of low expression of p300/CBP to predict poor prognosi
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Sometime ago we have described diamino triazines
2022-02-12
Sometime ago we have described diamino-1,3,5-triazines as histamine H4R ligands,12, 13 and aryl derivatives of the 1,3,5-triazine, which attenuated inflammatory and nociceptive response in vivo in the rodent models of inflammation induced by Levofloxacin and zymosan. In this work we describe new der
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GSK has also been used as PET radiotracer
2022-02-12
GSK-189254 has also been used as PET radiotracer (in the form of [11C]-GSK-189254, also used as [11C]-AZ12807110 by Jucaite et al. (Jucaite et al., 2013)) to assess H3R occupancy (Ashworth et al., 2010), and is currently used in an image-based phase I clinical trial study for investigating GSK-23951
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