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PTC-209 cAMP mediated signaling pathways are important for m
2020-03-17

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, PTC-209 of the PKA 2β regulatory subunit (RIIβ) in mice leads to increased expression of u
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Recent results from our group found that SPMs not
2020-03-17

Recent results from our group found that SPMs, not only play a part in terminating inflammation, but also have a physiological role in conjunctival goblet Cy5 TSA to maintain ocular surface health in the absence of disease. Amongst the SPMs that are effective in the conjunctiva are resolvin D1 (RvD
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br Materials and methods br Results br
2020-03-17

Materials and methods Results Discussion The incretin hormones potently stimulate insulin secretion, and it is generally assumed that this is mediated by an endocrine mechanism such that GIP and GLP-1 through the circulation reach the islet beta Oxaliplatin australia to stimulate their sec
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Verapamil a calcium channel blocker
2020-03-17

Verapamil, a calcium channel blocker used clinically as a coronary vasodilator, was amongst the first compounds identified that could reverse MDR and potentiate the effects of MDR1 substrates such as vincristine [15], [16]. Verapamil, along with a number of other MDR1 blockers, have proved largely u
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The unique property of mutant IDH in producing
2020-03-17

The unique property of mutant IDH1/2 in producing an oncometabolite that has no known physiological function makes mutant IDH enzymes as obvious potential therapeutic targets for the treatment of IDH-mutated tumors (Rohle et al., 2013, Wang et al., 2013). Clinical studies have also suggested the pre
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Members of the Nudix family typically contain a
2020-03-17

Members of the Nudix family typically contain a 23-amino-acid sequence (Nudix box) of GxExREUxEExGU, where U is usually Ile, Leu, or Val and x represents any amino acid. The EUxEE core residues serve as anchors for an Mg ligand that associates with a characteristic pyrophosphate linkage that is comm
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br Four active site residues
2020-03-16

Four active site residues of Δ1-KSTD1 are fully conserved in Δ1-KSTDs from different species (Supplementary Figure S2). These residues are Tyr-119, Tyr-487, and Gly-491 from the FAD-binding domain and Tyr-318 from the catalytic domain. The structure of the Δ1-KSTD1•ADD complex revealed that the hy
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When women reach the menopause they experience
2020-03-16

When women reach the menopause they experience a number of physical complaints such as hot flushes, vaginal dryness and mood changes [1]. Bone loss also becomes manifest at this time [1], [2], but women will often not suffer from back pain before a vertebral fracture occurs. Women who have had one f
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Fmoc-His(Trt)-OH Constitutive activity of Ras Raf
2020-03-16

Constitutive activity of Ras/Raf/MEK/ERK pathway plays a critical role on melanoma growth, thus inhibition of activity of Ras, Raf and MEK can reduce ERK activity, leading to a decrease in melanoma cell proliferation, survival and invasion (Burotto et al., 2014; Paluncic et al., 2016). Our results a
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Prostaglandin E receptor subtype EP is a transmembrane G cou
2020-03-16

Prostaglandin E receptor subtype 4 (EP4) is a transmembrane G-coupled protein receptor activated by prostaglandin E2 (PGE2). EP4 activation exerts anti-inflammatory effects in adipose tissue by dampening the levels of inflammatory chemokines [12]. In the mouse, EP4 deficiency aggravates fragmentatio
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One of the most fundamental distinctions between Ub signals
2020-03-16

One of the most fundamental distinctions between Ub signals is substrate monoubiquitination versus polyubiquitination. With the exception of the E2, UBE2W, which represents a special case because it p38 mapk inhibitor only ubiquitinates the flexible N-termini of substrates [5], [6], [20], most exam
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Sodium Picosulfate A novel series of DHODH inhibitors was
2020-03-16

A novel series of DHODH inhibitors was developed by us based on a lead that was discovered during a docking procedure and medicinal chemistry exploration. The activity of the initial lead was improved by a QSAR method and yielded low nanomolar inhibitors. Introduction The most common metabolic h
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rc opiates Ung et al examined a variety
2020-03-16

Ung et al. examined a variety of structural features based upon the location of the DFG-motif and the αC-helix to define the conformational space of the catalytic domain of protein kinases [75]. They reported that the DFG motif can move from its active DFG-Din location to the inactive DFG-Dout locat
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It has been shown that CK phosphorylates
2020-03-16

It has been shown that CK1δ phosphorylates α-, β- and γ-tubulin in vitro and that CK1δ specifically interacts with the trans Golgi network, COPI positive vesicles, and centrosomes in interphase cells [11], [12], [13], [14]. Moreover CK1δ is also associated with granular particles that are associated
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br Acknowledgements This work was supported by a grant
2020-03-16

Acknowledgements This work was supported by a grant from the Deutsche Forschungsgemeinschaft to Uwe Knippschild and Martin Wabitsch (SFB 1149/B4). P. Fischer-Posovszky is funded by a Margarete von Wrangell scholarship financed by the Ministerium für Wissenschaft, Forschung und Kunst Baden-Württem
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