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To develop antagonists selective for the mouse EP
2019-09-10
To develop antagonists selective for the mouse EP1 receptor, we started with compound (), synthesized as previously described (). Diethyl dipicolinic 3463 () was reduced with NaBH to . Parikh–Doering oxidation of with sulfur trioxide–pyridine complex and DMSO produced the unstable aldehyde . 4-Chlor
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ApoE is secreted from astrocytes
2019-09-10
ApoE is secreted from astrocytes/glia into the interstitial fluid and is important for metabolizing Aβ because of its propensity for binding Aβ as a cholesterol and phospholipid acceptor in reverse cholesterol transport [8]. Aβ oligomers show a direct toxicity to neurons, and ApoE inhibits oligomer
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br Perspective and conclusion Collagen
2019-09-10
Perspective and conclusion Collagen Toolkits II and III have been used to determine the CW069 for DDR1 and DDR2, and the main binding site is the GVM-GFO motif [103,108]. The co-crystal structure of the DS domain of human DDR2 bound to a synthetic collagen-like peptide containing the GVM-GFO mot
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Like all other cellular processes ubiquitination is also
2019-09-10
Like all other cellular processes, ubiquitination is also tightly regulated; more so, as myriads of pathways are controlled via this conjugation and dysregulation of ubiquitination has been implicated in various diseases including cancer [16], [17]. Quite a few of such regulatory mechanisms that con
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Protein kinase casein kinase CK comprises a
2019-09-09
Protein kinase casein kinase 1 (CK1) comprises a family of highly related, constitutively active serine/threonine protein kinases (reviewed by [15]). CK1 is involved in controlling a wide variety of different cellular events including protein turnover [16], [17], nuclear import [18] and the cellular
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Next to organophosphates carbamates and metals cholinesteras
2019-09-09
Next to organophosphates, carbamates and metals, cholinesterase activity can also be affected by other pesticides, such as newer generation neonicotinoid insecticides (NN). NNs do not inhibit AChE activity via the organophosphate-sensitive binding site of the enzyme, but rather, by acting as a struc
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Thus the exact mechanisms responsible
2019-09-09
Thus, the exact mechanisms responsible for progestogen-induced changes in immune response are not known but the effects are believed to be exerted through receptor-mediated interactions. Since the mPR α is known to be a G protein-coupled receptor in fish, downstream signaling cascades via secondary
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Here we examined whether Intracellular ER may
2019-09-09
Here, we examined whether Intracellular ER may mediate Cd-induced ovarian cancer proliferation. To determine this relationship, we used ICI 182,780 as a general inhibitor of ERα and ERβ. The results suggest a metalloestrogenic effect of Cd in ovarian cancer cell lines. Inconsistency with our results
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The discoidin domain receptors DDR and DDR are
2019-09-09
The discoidin domain receptors, DDR1 and DDR2, are receptor tyrosine kinases that are activated by different types of collagen (Shrivastava et al., 1997, Vogel et al., 1997). Both receptors interact with a number of fibrillar collagens, and DDR1, but not DDR2, is also activated by the network-formin
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br Are incretins the only mediators
2019-09-09
Are incretins the only mediators of the anti-hyperglycaemic effects of DPP-4 inhibitors? Even though both GLP-1 and GIP were identified as substrates for DPP-4 early on [17], [19], [20], [22], and DPP-4 inhibition in vivo raises levels of the intact endogenous forms of both of them [43], [44], fr
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If the unwanted objects detected by OpenComet are
2019-09-09
If the unwanted objects detected by OpenComet are manually deleted, and then the DNA (%) in tail is computed, the performance of the present method can be compared more effectively. Therefore, performance of OpenComet is analysed in two ways as Approach 1 and Approach 2. Approach 1, considers the DN
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Are the hydrogens removed simultaneously
2019-09-09
Are the hydrogens removed simultaneously or one by one? — Δ1-KSTDs can catalyze the exchange of alkali-labile tritium or deuterium atoms at the C2 Moniliformin sodium salt kinase of their substrates, even when enzyme turnover was prevented by the absence of an electron acceptor for the oxidative ha
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In recent years the use of
2019-09-09
In recent years, the use of liquid chromatography/tandem mass spectrometry (LC–MS/MS) has become a preferred approach to measure drugs and metabolites in biological fluids due to its very high selectivity and sensitivity [17], [18], [19], [20], [21], [22], [23], [25], [30]. The great sensitivity of
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br Materials and methods br Results br Discussion In
2019-09-09
Materials and methods Results Discussion In this study, we have shown that fat body-specific knockdown of the key splicing factors U1-70K and U2AF lead to decreased triglyceride storage phenotypes in larvae. Additionally, there was no accompanying defect in glycogen storage observed in thes
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br Conclusions and future perspectives It is now evident
2019-09-09
Conclusions and future perspectives It is now evident that selective ETA or nonselective endothelin receptor antagonism provides therapeutic potentials against a variety of cardiovascular diseases such as hypertension, PAH, and diabetic microvascular dysfunction (Fig. 1). However, PAH is currentl
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