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The biological actions of ghrelin are mainly due to
2022-06-29
The biological actions of ghrelin are mainly due to its interaction with GHSR-1a (Howard et al., 1996). The pharmacological properties of D-Lys3-GHRP-6, a selective antagonist of GHSR-1a, have been extensively studied (Beck et al., 2004, Benso et al., 2007, Sibilia et al., 2006). To study the recept
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Iodination of commercially available with
2022-06-29
Iodination of commercially available with excess ICl in AcOH gave a quantitative yield of , which was cyclized with benzyl thioamides to give the 2-benzyl-9,10-dihydro-4-1-thia-3,4-diaza-benzo[]azulenes . Coupling of the iodides with heterocycles including imidazoles, triazoles, or zinc cyanide usin
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The structural similarity software vROCS
2022-06-29
The structural similarity software vROCS (OpenEye) [45] has been utilized by Musumeci et al. [46] to screen the Maybridge [47] HitFinder database (∼14,400 compounds) using Distamycin A (Fig. 3B) as a query. Using the Tanimoto coefficient (Section 6.4) and vROCS's colour scoring (atom/feature similar
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PF 1022A mg br Experimental procedures br Conflicts of inter
2022-06-28
Experimental procedures Conflicts of interests Introduction Here we investigate differences in growth properties and short-term morphological changes in response to ET-1 in Chinese hamster ovary (CHO) cells stably and separately expressing ETA or ETB receptors. A stably transfected CHO syst
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Materials and methods br Results and discussion br
2022-06-28
Materials and methods Results and discussion Acknowledgments This work was supported in part by the Japan Society for the Promotion of Science KAKENHI Grants JP21300174 and JP25282144 (H.K.). Introduction Epigenetic modifications of histones, such a lysine acetylation, play a key role in
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Cisatracurium Besylate We notice that previous reports
2022-06-28
We notice that previous reports of arsenic exposure are not completely consistent with each other, in terms of exposure-changed histone acetylations. In an early investigation, As exposure (7.5 μM) of HepG2 Cisatracurium Besylate increased H3K9ac after 24 h, when analyzed by methods of immunofluore
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Conflicting data concerning the involvement of H R on glycae
2022-06-28
Conflicting data concerning the involvement of H2R on glycaemia has also arisen. Its antagonism was reported to decrease [35], not affect [36], [37] and increase [38], [39] Azithromycin synthesis levels. In comparison, the clinical experience with antipsychotic drugs generated clearer evidence for
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Studies conducted in our laboratory
2022-06-28
Studies conducted in our laboratory, thus far, have shown that HKDC1 is broadly expressed [28]. Using the first developed HKDC1 mouse model, we found that complete loss of HKDC1 function is embryonic lethal, similar to other HKs [29,30]. Further studies using HKDC1 heterozygous knockout mice showed
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br Future perspectives sGC signaling is
2022-06-28
Future perspectives sGC signaling is important in the maintenance of multiple physiological functions. sGC is localized to cell membranes with both sGC Cys modifications and heme regulation identified as the crucial components in regulating sGC activity. Specifically, S-nitrosation of several com
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The Rab to Rab switch
2022-06-28
The Rab5 to Rab7 switch on endosomes co-occurs with the release of the Rab5 GEF Rabex5 from endosomes, which prevents further Rab5 activation [5]. In addition, the Rab5 GAP is recruited to inactivate remaining Rab5 [67]. Recent data suggest that another GAP, TBC1D5, which binds the retromer complex,
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Acute in vivo experiments were performed in normoglycemic SV
2022-06-28
Acute in vivo experiments were performed in normoglycemic 129SVE mice to confirm GPR119 activation and corresponding rat 4 control. GIP release was utilized as a biomarker for target receptor engagement and plasma GIP levels were measured 45min after oral dosing (). Both 3 and 10mg/kg produced an in
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Both GPR A and GPR are
2022-06-28
Both GPR109A and GPR81 are located on chromosome 12q24 [3] and mediate anti-lipolytic effects through coupling to Gi-type G proteins [17]. It is important to note that with the recent deorphanization of these receptors, there has been a recommendation to the International Union of Basic and Clinical
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Although EAAT may not be
2022-06-28
Although EAAT3 may not be involved in the induction of morphine-induced CPP, our results suggest that other EAATs may play a role in the behavior because riluzole, an EAAT activator (Frizzo et al., 2004, Fumagalli et al., 2008), abolished morphine-induced CPP. Consistent with this suggestion, a few
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Due to the requirement of high
2022-06-28
Due to the requirement of high-end methods such as total internal reflection fluorescence (TIRF) microscopy to visualize lipid rafts, isolation procedures are employed to study the protein content of lipid rafts [29]. The different methods utilized to isolated lipid rafts and other low density micro
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During the course of our optimization of the
2022-06-27
During the course of our optimization of the diarylsulfonamide chemotype as FFA4 agonists, we identified xanthene as a potent and selective antagonist of FFA4 (). Xanthene was able to block the agonist induced intracellular Ca response elicited by both linoleic gpcr and compound in competition s
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