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Several studies have found that GPR possesses a distinct pha
2022-08-22
Several studies have found that GPR55 possesses a distinct pharmacology from that of CB1 and CB2, and that only certain cannabinoids act at this receptor. In transfected Rosiglitazone maleate expressing hGPR55, out of more than 20 synthetic and endogenous cannabinoids evaluated, only 2 compounds, S
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br Conflict of interest br Acknowledgment
2022-08-22
Conflict of interest Acknowledgment This work was supported by National Program on Key Basic Research Project of China (No. 2013CB127305); The National Natural Science Foundation of China (No. 314020785); Hubei Provincial Creative Team Project of Agricultural Science and Technology (No. 2007-6
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Compared to methadone or morphine
2022-08-22
Compared to methadone or morphine, buprenorphine is a partial mu-opioid agonist, which shows high affinity for, and slow dissociation from, mu-opioid receptors. This maintenance of homeostasis may help to counter the development of an overt withdrawal syndrome, and may explain the lower risk of deve
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The inhibition of NSAIDs towards GLOI provides a direction f
2022-08-22
The inhibition of NSAIDs towards GLOI provides a direction for the development of novel effective GLOI inhibitors. Although the inhibitory activity of indomethacin was determined and the interactions between it Creatinine sale and GLOI were probed by NMR titration experiments, no detailed inhibitory
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Analysis of the i motif structures during
2022-08-19
Analysis of the i-motif structures during biased unfolding of G-quadruplexes leads to the conclusion that at acidic pH the i-motif is absolutely unaffected by that process. The hydrogen bonds within the i-motif are intact (Fig. 3D) and they only fluctuate around mean values. On the other hand, the i
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Cryptochlorogenic acid Endothelial cells receive a variety o
2022-08-19
Endothelial cells receive a variety of information from the environment which finally guides them through all phases of neovascularization. Angiogenic signals enhance the proliferation of endothelial cells, upregulated resistance to apoptosis, alterations within proteolytic balance, reorganization o
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So what makes a FFAR agonist different and interesting
2022-08-19
So what makes a FFAR1 agonist different and interesting? As shown in the , the cellular mechanism is different from those of present insulin-releasing pharmacotherapies—namely the secretion initiators (sulphonylureas and meglitinides) and the incretin-based secretion potentiators (glucagon-like pept
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Most studies to date have focused on the physiological funct
2022-08-19
Most studies to date have focused on the physiological functions of FPS in plants. As mentioned above, numerous factors affect FPS expression and FPS function. However, FPS enzymatic assays require radiolabeled substrate and thus detailed enzymatic characterizations of FPS, including substrate speci
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Remarkably most of these molecules are also quite effective
2022-08-19
Remarkably, most of these molecules are also quite effective in interfering with the proliferation of the drug-resistant cancer cell lines, with IC50 values ranging from 0.59 to 2.93 μM against MCF-7/ADR cells, and from 0.160 to 1.17 μM against NSCLC-resistant H1975 cells. Among these molecules, com
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We also evaluated the effect of varying ionic str
2022-08-19
We also evaluated the effect of varying ionic strength. These experiments included previously characterized H3 (residues 1–21) and SNAIL (residues 1–9) peptides [8], [34] to allow a comparative analysis with different ligands (Fig. 1A). As shown in Fig. 2 and listed in Table 2, it is evident that a
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1,3-PBIT dihydrobromide A complimentary approach with Per
2022-08-19
A complimentary approach with Per2:Luc 1,3-PBIT dihydrobromide exposed to hypoxia as well as with mBmal1:Luc circadian reporter cells in which we overexpressed variants of HIF-1α and HIF-2α revealed that hypoxia and HIFs can not only shorten the period but also decrease the amplitude of the clock (
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In the same research group
2022-08-19
In 2017, the same research group released a free internet accessible database (HemeOxDB, http://www.researchdsf.unict.it/hemeoxdb), to make it easier the analysis of the literature and, consequently, the design of potent and selective HO-1 inhibitors. The database reported the entire set of HO-1 and
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The endocytic inhibitors MDC and
2022-08-19
The endocytic inhibitors MDC and CPZ and dynamin GTPase blocker (dynamin mutant) have been shown to significantly decrease the intracellular accumulation of cGMP. Moreover, earlier reports suggested that G-protein-coupled receptor (GPCRs) continue to signal by generating cAMP throughout internalizat
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GSK can function in regulating
2022-08-19
GSK-3 can function in regulating insulin signaling and glucose metabolism. Inactivation of GSK-3 activity results in dephosphorylation and activation of GS that leads to improved glucose tolerance. However, there are additional mechanisms that can lead to increases in GS activity and improve insulin
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br Materials and methods br
2022-08-19
Materials and methods Results Discussion and conclusions Our data demonstrate that native and 2-OMe-LPC analogues are GPR119 ligands and activate insulin secretion from βTC-3 pancreatic cells. LPC 18:1 was the first proposed endogenous ligand for GPR119 [1], however natural LPC has limited
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