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Ghrelin readily crosses the blood brain barrier
2022-04-21
Ghrelin readily crosses the blood difluprednate sale barrier (Banks et al., 2002, Banks et al., 2008), and recent studies have identified central nervous system sites of action for ghrelin-mediated appetite and hyperphagia (Alvarez-Crespo et al., 2012, King et al., 2011, Schele et al., 2016, Skibick
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The mechanism by which Piezo acts in the regulation
2022-04-21
The mechanism by which Piezo1 acts in the regulation of RBC volume is not firmly established. Its curved structure implies that it is activated by an increase in membrane tension (11), a mechanism indicated by electrophysiological measurements (16). However, the RBC membrane mechanics at its physiol
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Moreover after the initial bleaching of
2022-04-21
Moreover, after the initial bleaching of the fluorescent molecules in the targeted cell exposed to laser illumination, the neighboring reservoir Lomerizine HCl are expected to give in return new fluorescent ones if the cells are coupled together by gap junction channels. This supposes that the level
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br Structures of human secretase Before the
2022-04-21
Structures of human γ-secretase Before the near-atomic resolution structures, the highest resolutions achieved for γ-secretase were 15 and 12Å [19, 21]. The 15-Å structure revealed a 51 8 chamber in the transmembrane domain and two pores at the top and bottom of γ-secretase, which were speculated
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In the light of the above mentioned
2022-04-21
In the light of the above-mentioned considerations, it is interesting to note that the FPR-related research with regards to bias agonism did not prosper during considerably during the last decade (possible exceptions are [[8], [9], [10], [11]]. However, with new insights in receptor chemistry and fu
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TTNPB br Results and discussion br Conclusion In summary
2022-04-21
Results and discussion Conclusion In summary, we designed and discovered a series of novel GPR40 agonists containing 3,5-dimethylisoxazole with improved tPSA and ideal cLog P. Most of these compounds were confirmed as excellent GPR40 agonists in vitro. Especially, compound 11k exhibited robust
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br Discussion In response to an increase in
2022-04-21
Discussion In response to an increase in glucose or DHA concentration, FBPase showed nuclear import and recruitment in a peripheral cell compartment. Interestingly, FBPase and GS were co-recruited to the periphery of the cells. This is precisely the site where glycogen is initially synthesized an
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In the previous paper we
2022-04-21
In the previous paper, we described the design and synthesis of tricyclic thiazoles as FBPase inhibitors, and a series of SAR studies led to the identification of phosphate 3 and difluoromethylenephosphonate 4 exhibiting potent FBPase inhibitory activities (IC50=13, 47nM, respectively) (Fig. 2). In
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br Experimental procedures br Results br Discussion This stu
2022-04-21
Experimental procedures Results Discussion This study demonstrates that the genetic disruption or pharmacological inhibition of FAAH completely prevented all manifestations of pain symptoms in an NTG-induced migraine animal model. Thus, FAAH disruption or blockade abolished the activation o
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Over the years a number of studies have reported
2022-04-21
Over the years, a number of studies have reported results concerning the behavior of the two endothelin receptor subtypes, ETA and ETB, that do not fit the classical model of two G protein-coupled receptors acting independently of one another. For example, in the rat anterior pituitary gland, both E
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In the Joint United Nations
2022-04-21
In 2015, the Joint United Nations Program on HIV/AIDS (UNAIDS) proposed that by 2020, 90% of people living with HIV should be aware of their HIV status, as the first part of 90-90-90 strategy to end AIDS epidemic. Early detection of HIV allows initiating care for proper treatment, which impacts in m
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An azabicyclic compound named S a a hexahydro
2022-04-21
An azabicyclic (S)-10-Hydroxycamptothecin mg named S 38093, (4-[3-(3,3a,4,5,6,6a-hexahydro-1H-cyclopenta[c]pyrrol-2-yl)propoxy]benzamide), was introduced by Servier with H3R antagonist and inverse agonist activity (Sors et al., 2017). The compound contains all the drug-likeness criteria owing to it
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FoxM a downstream target of Gli has been
2022-04-20
FoxM1, a downstream target of Gli, has been mainly related to Berbamine hydrochloride regulation and cellular proliferation in tumor (Alvarez-Fernandez and Medema, 2013, Halasi and Gartel, 2013, Teh et al., 2002). Especially, FoxM1 is a regulator of G1/S and G2/M transitions and M-phase progression
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Following our initial observation of an
2022-04-20
Following our initial observation of an unexpected increase in the maximal rates of cGMP formation by NO-stimulated sGC in the presence of cytosolic PCA preparations [15], we attempted to purify, identify and characterize the responsible protein(s). The purification protocol described in the present
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br Materials and methods br Results br Discussion
2022-04-20
Materials and methods Results Discussion Directly modulating specific target proteins and signaling pathways with small-molecule drugs or agonistic mmp inhibitor is widely used for cancer metastasis therapies [[39], [40], [41]]. ANXA7 acts as a metastasis suppressor in prostate cancer. How
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