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br Localization of D receptors
2020-06-03

Localization of D2 receptors in striatum One characteristic of D2Rs that has complicated their study is their expression in multiple neuronal populations within striatum, both pre- and postsynaptically (Beaulieu and Gainetdinov, 2011). In addition to spiny projection neurons (SPNs), which are the
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br Anti inflammatory effects of MTX In addition to cytotoxic
2020-06-03

Anti-inflammatory effects of MTX In addition to cytotoxic and cytostatic effects, the anti-inflammatory activity of MTX was also described by several studies. Inhibition of ATIC by MTX has been found to result in the accumulation of 5-aminoimidazole-4-carboxamide-1-β-d-ribofuranosyl 5′-monophosph
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Compound was prepared from chloroindole by acylation to give
2020-06-02

Compound was prepared from 6-chloroindole () () by acylation, to give , and subsequent reduction to give . The thiazole was then installed using conditions developed by Buchwald and co-workers to give . Hydrolysis of the ester yielded the thiazole fruquintinib synthesis derivative (). Derivatives
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The biological actions of ET are mediated via two
2020-06-02

The biological actions of ET‐1 are mediated via two distinct receptor subtypes, the endothelin A and endothelin B receptors (ETA/ETB). While activation of ETA is assumed to mediate contraction of smooth muscle cells, the activity of ETB is related to transient vasodilation [22]. In human corpus cave
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Due to the high attractiveness of E
2020-06-02

Due to the high attractiveness of E2 and E3 ligases as drug targets, a number of drug discovery assays have been published, based on detection by fluorescence (Dudgeon et al., 2010, Krist et al., 2016, Zhang et al., 2004), interleukin 2 receptor (Davydov et al., 2004, Huang et al., 2005, Kenten et
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hUcn II influence on MAP is mediated
2020-06-02

hUcn II influence on MAP is mediated by the activation of CRF2 receptors. In vitro binding studies established that hUcn II is a selective ligand for CRF2 receptors with a slightly higher affinities for CRF2β compared with CRF2α and low or no affinity for CRF1 receptor [13], [19], [24]. Recent in vi
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br Experimental Procedures br Acknowledgments br Bisphenol A
2020-06-02

Experimental Procedures Acknowledgments Bisphenol A (BPA) has been recognized as one of the most potent endocrine disruptors, functioning even at very low doses. Although it is anticipated that Remodelin mg receptor (ER) would mediate these effects of low-dose BPA, studies revealed that BPA
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Based on the SUMO SIM interaction involved in
2020-06-02

Based on the SUMO–SIM interaction involved in SUMOD positioning, a SUMO2ΔSBD (SIM-binding domain; Q30A, F31A, I33A) mutant can be investigated that disrupts this important binding interface (Eisenhardt et al., 2015; Meulmeester, Kunze, Hsiao, Urlaub, & Melchior, 2008). In Fig. 4A, multiturnover assa
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Examination of Wnt signaling via for
2020-06-01

Examination of Wnt signaling via, for example, complexes of frizzled (Fz) and lipoprotein-receptor-related protein (LRP) receptors has been hindered by difficulties in producing Wnt ligands due to their inherent hydrophobicity [20]. This bottleneck was recently bypassed by constructing highly solubl
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The secondary objective of the present study was to
2020-06-01

The secondary objective of the present study was to evaluate the pharmacokinetics, safety, and tolerability of multiple oral doses of 450-mg delafloxacin to reach steady state in healthy male and female subjects. After multiple dosing of oral delafloxacin, steady state was reached after 4 days of do
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br Additional CDKs with a role in cancer br Small
2020-06-01

Additional CDKs with a role in cancer Small molecule CDK inhibitors The majority of protein kinase inhibitors developed to date are type I inhibitors: they bind at the ATP–binding site, are ATP-competitive and target the kinase in its active state; with the activation loop DFG motif in the ‘in
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To extend these toxicity minimization strategies
2020-06-01

To extend these toxicity minimization strategies to 3D tissues, a more complicated mass transfer model is necessary to account diffusion in the interstitial space, as well as transport across cell membranes. Until recently, tissue mass transport in cryobiology was modeled using classic spatially dep
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The proposed FDIR technique is presented in the following fo
2020-06-01

The proposed FDIR technique is presented in the following format: Section 2 contains a survey of typical orbits of interest with regard to the ACSF sale environment found in them, which is contrasted with a LEO orbit. Additionally, how the requirements for the satellite system can be estimated is p
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It has long been known that native
2020-05-29

It has long been known that native BChE is a major factor in the inactivation of cocaine, an ester-type drug of abuse [190]. But recently some researchers conceived the idea that BChE mutations could improve that function to a point that would favorably impact cocaine overdose. Rapid progress was ma
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br Materials and methods br Results
2020-05-29

Materials and methods Results Discussion The effect of progestogen treatment showed some tendencies affecting the body length and weight, however these data were not verifiable statistically. This observation could be explained with the relatively short exposure period and/or the relatively
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