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enzyme substrate br Signals transmitted via MEGJ MEGJ facili
2022-04-18
Signals transmitted via MEGJ MEGJ facilitate the direct transfer of ion currents or small molecules between EC and VSMC. Molecules passing through MEGJ are mainly second messengers such as Ca2+, IP3, and cAMP [31,32,] or endothelium-derived hyperpolarization (EDH) signals [34, 35, 36]. Moreover,
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A group of small molecule with a more promising therapeutic
2022-04-18
A group of small molecule with a more promising therapeutic mechanism are known as γ-secretase modulators (GSMs), which modulate the cleavage activity of γ-secretase (and likely a host of other substrates) and specifically reduce the levels of the fibrillogenic Aβ42 peptide without altering the ε-si
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br Fipronil resistance associated with A S and
2022-04-18
Fipronil resistance associated with A2′S and A2′G mutations Fipronil is a second-generation NCA (Fig. 1), and A2′S and A2′G mutations provide a low level of cross-resistance to fipronil (Cole et al., 1995, Gao et al., 2007). As shown in Table 1, the A2′S Carmustine confers high resistance to diel
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Recently we indicated that cell
2022-04-18
Recently, we indicated that cell motility was regulated by the different induction of GPR120 and GPR40 in liver epithelial WB-F344 Coumarin treated with chemical agents. The cell motility of WB-F344 cells was stimulated by phorbol ester 12-O-tetradecanoylphorbol-13-acetate (TPA) which is a potent t
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Following the discovery of diketo compounds S and L as
2022-04-16
Following the discovery of β-diketo compounds S-1360 [31] and L-731988 [32] as anti-HIV integrase inhibitors, a group of researchers discovered a potent 133 2 based derivative (1) as the inhibitor of HIV integrase functioning at the 3′-processing and strand transfer steps of HIV integrase. Bioassay
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The histamine H receptor H R amino acids
2022-04-16
The histamine H3 receptor (H3R; 326–445 amino-acids) is located on histaminergic neuron somata, dendrites and axon varicosities, as well as on the axon varicosities and somata of other neurons, providing negative feedback to inhibit histamine synthesis and the release of histamine or other transmitt
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The presence of the H
2022-04-16
The presence of the H3 receptor in humans was confirmed approximately 25 years ago, and the receptor was successfully cloned in 1999 (Thurmond, 2010). The H3 receptor is unique, as it controls feedback of histamine release, particularly in the central nervous system, where it modulates neurotransmit
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br Conflict of interest br Acknowledgements This work
2022-04-16
Conflict of interest Acknowledgements This work was funded by the University of Turin (ex60% 2014), World Wide Style Project (WWS; University of Turin/Fondazione CRT) and University of Florence (ex60% 2014). ACR and AP designed the study; AP, EB and IO conducted the literature search and analy
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Adenine sulfate The synthetic pathway of the target
2022-04-16
The synthetic pathway of the target compounds , , , and is presented in . The intermediate was synthesized according to a reported method. The intermediate was prepared by mixing UA with an equimolar concentration of KCO, a catalytic amount of KI, and more than two equivalents of 1,2-dibromoethan
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In summary we have designed and explored synthetic
2022-04-16
In summary, we have designed and explored synthetic routes towards novel acylsulfamoyl benzoxaborole-based HCV NS3 protease inhibitors. Interestingly, the resulting, unoptimized P1–P3 and P2–P4 macrocyclic inhibitors were equipotent in an enzyme assay and somewhat less potent in replicon assays, com
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Despite the similarities there are some differences between
2022-04-16
Despite the similarities, there are some differences between the augmentation by hypoxia and that by thymoquinone. While in porcine coronary arteries they both depend on calcium sensitization mediated by ROCK12, 32, 33, L-type calcium channels are involved only in thymoquinone-induced augmentation.
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The difference in the expression of functional FFARs
2022-04-16
The difference in the expression of functional FFARs between neutrophils and monocytes/macrophages suggests that the role of FFA2R may be restricted to the very early phase of acute inflammation where neutrophils are dominating players called into action, whereas GPR84 may have a broader functional
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In normal tissues the expression patterns of GPR and
2022-04-16
In normal tissues, the expression patterns of GPR120 and GPR40 are not uniform. GPR120 is highly expressed in adipocytes, lung and intestinal tract, while GPR40 is shown to be expressed in pancreatic islet AZD4547 and intestinal tract [7], [20]. It is considered that the distribution of the GPR120
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In order to investigate whether this off target
2022-04-16
In order to investigate whether this off-target activity was related to a particular structural feature of this YM-155 hydrochloride or was characteristic of the series, compounds , and were selected as being matched pairs with compound but with structural variation in terms of the R, R and R groups
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Thyroid hormone triiodothyronine T and its precursor
2022-04-16
Thyroid hormone 3,5,3′-triiodothyronine (T3) and its precursor, thyroxine (T4), are iodinated compounds, which are known to regulate the expression of genes involved in various biological processes, such as development, growth and metabolic control. The iodothyronine deiodinase types I, II and III (
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