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Imidazo purine diones were another cluster
2020-06-23
1-Imidazo[2,1-]purine-2,4(3,8)-diones were another cluster of compounds identified from the Chembridge screen (). A benzyl group at the R2 position was preferred over a phenyl or 2-phenylpropyl (. and ), and -substitution of the benzyl group increased potency to the nanomolar level ( IC=0.20μM . ).
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br Materials and methods br Results br
2020-06-23
Materials and methods Results Discussion In this study, we developed a new CysLT1 and CysLT2 receptors-mediated Schisandrol B guinea pig model for screening both CysLT2 receptor and CysLT1/2 receptor antagonists. Unlike human CysLT2 receptors, which are equally stimulated by both LTC4 and L
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br Materials and methods br Results br
2020-06-22
Materials and methods Results Discussion It has been demonstrated that up-regulation of EPHB4 impaired trophoblast migration and invasion during placentation, which may contribute to the pathogenesis of preeclampsia [11], [24]. However, the upstream regulating mechanism of EPHB4 expression
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ligand gated ion channel The action of pt PGE
2020-06-22
The action of 17-pt-PGE2 as an EP1 receptor agonist [34] was demonstrated in several experimental settings, including cancer, neurons, vascular system, kidney and was confirmed by application of EP1 receptor selective antagonists [35], [36], [37], [38], [39], [40], [41]. Receptor binding studies in
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There has recently been some
2020-06-22
There has recently been some interest in Uba6, which is most similar to slime mold, with BLAST identities of 59% and positives 73% in the 400–600 ADD range. The 400–600 ADD correlation of the two profiles is a striking 87%, so functional differences probably arise outside the ADD binding domain. Hu
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It is noteworthy that little is known as to
2020-06-22
It is noteworthy that little is known as to the role of autophagy in regulation of eNOS phosphorylation and eNOS uncoupling. eNOS monomers, but not eNOS dimers could be degraded by ubiquitination [39], harbingering the existence of protein degradation pathways in modulation of eNOS turnover and acti
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It was demonstrated that ET signaling is the
2020-06-22
It was demonstrated that ET-1 signaling is the primary axon guidance mechanism that accounts for sympathetic innervation of the sinoatrial node and myocardium in the developing mouse heart [11]. In this article, we will review the findings relating to the basic profiles; i.e. molecular features of
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Ample evidence has shown that
2020-06-22
Ample evidence has shown that ET-1 system plays a pivotal role in the development of cardiovascular anomalies and pharmacological inhibition of ETA prevents the development of cardiac hypertrophy [[37], [38], [39]]. Yanagisawa and coworkers, who first reported the cardiomyocyte-specific endothelin A
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Ethyl naphthoates a h were successfully
2020-06-22
Ethyl 1-naphthoates (10a–h) were successfully reduced to 1-naphthylmethanols (12a–h) by using LiAlH4 with 8–87% yields. Then PCC was used to convert the alcohols into the corresponding 4-alkyl-1-naphthaldehyde derivatives (13a–h) with relatively higher yields (58–90%) as represented in Scheme 2. The
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br Introduction Coping with DNA damage is possible
2020-06-22
Introduction Coping with DNA damage is possible thanks to surveillance mechanisms (checkpoints), that detect the problem and promote its solution [1], [2], and to repair and tolerance pathways that remove the lesions or reduce the damage consequences [3], [4]. Failures in these processes have a h
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DGK deficiency caused a significant increase in the SERT pro
2020-06-22
DGKδ deficiency caused a significant increase in the SERT protein level, but its mRNA level was not affected (Fig. 1). These results suggest that SERT protein stability is directly reduced by interaction with the DGKδ protein. In contrast, DGKδ deficiency regulated both TPH-2 and MAO-A protein and m
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Introduction Prolyl hydroxylation is a widely observed post
2020-06-22
Introduction Prolyl hydroxylation is a widely observed post translational modification in collagen, an abundant animal protein. The high content (~13% per chain of the triple helical structure) of 4-hydroxyproline (Hyp,O) in collagen, togather with the natural abundance of collagen has led to the e
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Does hydroxylation of proline have a specific
2020-06-22
Does hydroxylation of proline have a specific role in the structure and function of the conotoxins? Several studies in the literature provide insights into the role of proline hydroxylation in the Conus peptides. The consequences of proline hydroxylation on oxidative folding and biological activity
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br RING dimerization RING type domains are found
2020-06-22
RING dimerization RING-type domains are found in many different structural contexts. While many exist as single-chain nmda receptor (Fig. 3A), a notable feature of RING-type E3s is their tendency to form homodimers and heterodimers (Fig. 3C–F). Homodimeric RING-type E3s include cIAP, RNF4, BIRC7
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cAMP mediated signaling pathways are
2020-06-22
cAMP-mediated signaling pathways are important for maintaining metabolic homeostasis, and the effects of the glucagon/catecholamine–cAMP–PKA axis on energy balance have been well documented [20]. For example, Heparin of the PKA 2β regulatory subunit (RIIβ) in mice leads to increased expression of u
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