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Also important in binding of E to the ER is
2019-12-11

Also important in binding of E2 to the ER is the hydroxyl on the D ring, which has a stabilizing contact with His-524 in ERα (Fig. 7) and with His-475 in ERβ (Fig. S1) [8,9,36,37]. The spatial relationship of the functional groups on the A and D rings on E2 has been used to develop chemicals conta
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br Materials and methods br Results br
2019-12-11

Materials and methods Results Discussion Here we show expression of the EP1 receptor in the hippocampus of mice and the functional influence of the EP1 receptor on kainic KPT-330 induced seizures. Mice lacking a functional EP1 receptor gene displayed a lower tendency to enter status epilep
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endothelin receptor antagonist Besides EGFR other tyrosine k
2019-12-11

Besides EGFR, other tyrosine kinase receptors are currently gaining attention as potential therapeutic targets. Included among these is the fibroblast growth factor receptor (FGFR) family, which is involved in the progression of a variety of cancers.7, 8, 9, 10, 11 In lung cancer, fibroblast growth
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The molecular mechanisms regulating the differentiation of
2019-12-11

The molecular mechanisms regulating the differentiation of Th1 versus Tfh comt inhibitor from IL-12-stimulated CD4+ T cells remain largely uncharacterized in humans. This topic has been extensively studied in mice (Weinmann, 2014), because IL-12 stimulation promotes mouse naive CD4+ T cells to expr
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Egr together with catecholamine biosynthetic enzymes such as
2019-12-11

Egr1, together with catecholamine biosynthetic enzymes, such as tyrosine hydroxylase (TH), dopamine β-hydroxylase (DBH), and phenylethanolamine N-methyltransferase (PNMT), is induced in adrenal medulla by different types of stress (Liu et al., 2005, Morita et al., 1996, Nankova et al., 1993, Papanik
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In this paper we describe a facile and universal
2019-12-11

In this paper, we describe a facile and universal method for in situ crosslinking of DNA micelles, using spherically directed reduction of metal ions. As shown in Scheme 1A, a single-stranded DNA (ssDNA) consisting of a ligand domain, a template domain, and a lipid domain was designed as a monomer t
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Many PIM inhibitors have been reported to date
2019-12-11

Many PIM inhibitors have been reported to date [7], [8], [9] however, none of them has been marketed so far. SGI-1776 is a representative first-generation PIM inhibitor, which had been under clinical trials for leukemia and prostate cancer [10]. While most of the first-generation PIM inhibitors are
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Tunicamycin Our module is designed to allow in
2019-12-11

Our module is designed to allow in-process measurement of [C]-tracer molar activity (MA, GBq/μmol at EOB) using a Tunicamycin detector with a UV detector at the outlet of the HPLC-portion of the system. In the HPLC chromatogram, peak analysis of the chromatographic data utilized PeakSimple software
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br Estrogen receptors activate mGluR signaling pathways
2019-12-11

Estrogen receptors activate mGluR signaling pathways In order to distinguish the opposing effects of estradiol on CREB phosphorylation, we turned to a “bottom-up” approach, working backwards from CREB phosphorylation to pharmacologically isolate the two signaling pathways (Boulware et al., 2005).
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To develop antagonists selective for
2019-12-11

To develop antagonists selective for the mouse EP1 receptor, we started with compound (), synthesized as previously described (). Diethyl dipicolinic Lck Inhibitor () was reduced with NaBH to . Parikh–Doering oxidation of with sulfur trioxide–pyridine complex and DMSO produced the unstable aldehy
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The cpm corresponding to bound
2019-12-11

The cpm corresponding to bound substrate in the sample well can be expressed as the difference between the total cpm in the sample well (3Hswtotal; 14Cswtotal) and the cpm for the unbound substrate in the sample well, as illustrated by Eq. (2): By combining Eqs. (1), (2), cpm for the bound substrat
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Lavallee et al reported that PREG could be esterified by
2019-12-10

Lavallee et al. [30] reported that PREG could be esterified by lecithin:cholesterol acyltransferase (LCAT). LCAT uses cholesterol and phosphatidyl choline present in the newly formed high-density lipoprotein (HDL) as substrates and convert them into cholesteryl esters and lysophosphatidyl choline. T
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br Mechanisms of acquired resistance
2019-12-10

Mechanisms of acquired resistance to 1st and 2nd generation EGFR inhibitors After treatment with first or second generation EGFR TKIs, virtually all patients after approximately 12 months develop acquired resistance (AR). Different mechanisms of AR to EGFR TKIs have been reported to date and may
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PBMC derived macrophages not only
2019-12-10

PBMC-derived macrophages not only express EBI2 but also have the ability to respond to their natural agonist 7α,25-OHC by activating downstream signal transduction pathways. In line with previous findings, our data confirm that receptor stimulation induces calcium mobilization which can be blocked b
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A key inciting event in atherosclerosis is the deposition of
2019-12-10

A key inciting event in atherosclerosis is the deposition of circulating low-density lipoprotein (LDL) in the subendothelial space of major arteries. In the subendothelium, native LDL is no longer protected by circulating antioxidants and is oxidatively modified to oxidized LDL (OxLDL) [5]. OxLDL is
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