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br Allosteric inhibitors In general
2019-09-25

Allosteric inhibitors In general, candidate drugs that bind to a GPCR at a site that is distinct (allosteric site) from the binding site of the endogenous agonist (orthosteric site) are attracting increasing attention 39, 42, 58. Allosteric modulators display saturability of their effect, probe d
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In SLO permeabilized human sperm
2019-09-25

In SLO-permeabilized human sperm, the AR elicited by calcium, persistently active Arf6 [41] and Rab3A, 8-pCPT-2′-O-Me-cAMP [8], diacylglycerol and a non-hydrolyzable analog [35], is sensitive to the PLC blocker U73122. Furthermore, 8-pCPT-2′-O-Me-cAMP elicits a calcium signal in non-permeabilized sp
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51 8 br Materials and methods br Results br
2019-09-25

Materials and methods Results Discussion COX-2-mediated production of PGE2 is involved in cell growth and metastasis of many cancers. Previous studies indicated that COX-2 was overexpressed in many cancer tissues and that PGE2 increased cancer cell growth, a process that could be suppressed
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Related with the studies by Zizza et al described above
2019-09-25

Related with the studies by Zizza et al. described above [66], work by Ward et al. [68] suggested that the C2 domain of cPLA2α, which binds to zwitterionic membranes with high affinity in a Ca2+-dependent manner, has a high membrane remodeling activity, producing dramatic changes in membrane curvatu
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br Target enzyme attributes and substrate
2019-09-25

Target enzyme attributes and substrate peptide selection Protein kinases catalyze the phosphorylation of serine, threonine, and tyrosine residues in both proteins and peptides using ATP as the phosphoryl donor. The human kinome is comprised of 518 protein kinases and 40 lipid kinases. The vast ma
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br Results br Discussion PKR is activated by
2019-09-25

Results Discussion PKR is activated by viral dsRNA and exerts its antiviral effect through phosphorylation of eIF2a. Because eIF2a phosphorylation leads to attenuation of protein synthesis, many viruses have evolved mechanisms to block or suppress PKR activation. Some viruses use alternative t
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In the present study we determined concentration
2019-09-24

In the present study, we determined concentration–response relationships for selected synthetic progestogens using in vitro luciferase transactivation assays driven by PR, ARα and ARβ from Murray–Darling rainbowfish () and compared the profiles with those obtained from similar assays based on human
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Furan analogs and N methylpyrrole analogs had
2019-09-24

Furan analogs and N-methylpyrrole analogs had completely different SARs. For example, replacement of the furan-2-sulfonyl moiety of 6 with the furan-3-sulfonyl moiety resulted in 8 with a decreased EP1 taurolidine affinity and an increased antagonist activity, while the corresponding chemical modif
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br Acknowledgements br Introduction Endothelial cells consti
2019-09-24

Acknowledgements Introduction Endothelial GSK1904529A constitute a unique source of humoral factors that may regulate the functions of other cell types via paracrine or endocrine pathways [1]. Among the many molecules originated from the endothelium, nitric oxide (NO) plays versatile roles in
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To predict levels of SCF assembly
2019-09-24

To predict levels of SCF assembly, Liu et al. (2018) first quantified the remaining necessary kinetic parameters and derived a model in combination with known functions and concentrations of components. The model agrees astonishingly well with many experimental observables. In terms of SCF assembly,
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RLS is a genetically complex disorder in which genetic and
2019-09-24

RLS is a genetically complex disorder in which genetic and environmental factors contribute to the phenotype (Trenkwalder, Allen, Högl, Paulus, & Winkelmann, 2016). This disease is highly familial and six genetic variants with single nucleotide polymorphisms have been identified by genome-wide assoc
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As DNA methylation plays a critical role in organismic
2019-09-24

As DNA methylation plays a critical role in organismic development and human diseases, the interest in DNA methyltransferases is constantly increasing. Extensive studies on the repertoires of dnmts genes have indicated increasing dnmts members in eukaryotes (Goll and Bestor, 2005; Ponger and Li, 200
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In laboratory strains of Escherichia coli three mechanisms
2019-09-24

In laboratory strains of Escherichia coli, three mechanisms of repair for alkylated bases are known. The first involves constitutively expressed Ogt and inducible Ada methyltransferases, directly removing methyl groups from O6-methylguanine (O6meG) and O4-methylthymine (O4meT) [1], [2], [3], [4]. In
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For any vector let and For let The
2019-09-24

For any vector , let , and . For , let The information matrix for the partial likelihood at Eq. (2.2) can be expressed as It is well known that ALW-II-41-27 under certain regularity conditions such as (A)–(D) in Andersen and Gill (1982), where and denote the maximum likelihood estimator from
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br Materials and methods br Results br Discussion The
2019-09-24

Materials and methods Results Discussion The main finding of the present study is that selective ETA and dual ETA/ETB receptor blockade markedly improve endothelium-dependent vasodilatation in patients with type 2 diabetes and vascular complications. The magnitude of improvement did not dif
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