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Introduction DHFR is an important enzyme in both mammals and
2019-08-05
Introduction DHFR is an important enzyme in both mammals and microorganism including Mycobacterium tuberculosis (Mtb). It catalyzes folic TUG-770 in conversion to dihydro and tetrahydro folic acid which is a crucial step in folate pathway [1]. Inhibition of folate pathway leads to interruption of t
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During the course of our
2019-08-05
During the course of our research on mGlu PAMs,, the hydroxyacetophenone scaffold was found to possess dual mGlu PAM and CysLT1 antagonism activity, presumably as orthosteric antagonist (). There is currently an increasing interest in drug discovery to explore multitarget drugs or polypharmacology
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The phenolic hydroxyl group of ezetimibe tolerated various s
2019-08-05
The phenolic hydroxyl group of ezetimibe tolerated various structural modifications (disaccharide, carboxyalkyl and glucuronide) that retained inhibitory activity.13, 14, 15 We conjugated glycylglycine to phenolic hydroxyl group and synthesized ten 1H-pyrrole-2,5-dione derivatives 14a-j successfully
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br Estrogen receptors activate mGluR
2019-08-02
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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br Discussion We are reporting a cryptic insertion
2019-08-02
Discussion We are reporting a cryptic insertion of chromosome 22 material (EWS) to the long arm of chromosome 11 (11q24, FLI-1) recognizable by FISH in Florfenicol exhibiting trisomy 8 as the sole cytogenetic anomaly. In ES and PNET tumors, trisomy 8 is the most common secondary abnormality [6].
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br The orphan estrogen related receptor exists as three subt
2019-08-02
The orphan estrogen-related receptor exists as three subtypes (ERRα, ERRβ, and ERRγ) in the human genome. ERRα is expressed in metabolically active tissues such as muscle and adipose. ERRγ is expressed in the spinal cord and CNS. ERRβ appears to play a role in development, as postnatal expression
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Our results from neutropenic mice infected
2019-08-02
Our results from neutropenic mice infected with both fungal strains revealed that the inflammatory process was more severe 72hours post-infection (Fig. 4). Angioinvasion was mainly observed 48hours after infection for both strains. Transformation of A. fumigatus conidia into hyphae in immunocompeten
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br Author Contributions br Acknowledgments br
2019-08-02
Author Contributions Acknowledgments Introduction Osteoporosis is a common bone disease that frequently leads to disruption of the alveolar and systemic bones with age. Novel osteoanabolic strategies to treat osteoporotic bone loss or augment fracture repair efficiently are desired. Since b
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br Ubiquitination and deubiquitination pathways Ubiquitinati
2019-08-02
Ubiquitination and deubiquitination pathways Ubiquitination is a part of the post-translational modification (PTM) process. Ubiquitination affects proteins in various ways, but its main functions are to signal protein degradation via the 26S proteasome, modify cellular location of proteins, affec
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In laboratory strains of Escherichia
2019-08-02
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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We aim to apply the
2019-08-02
We aim to apply the same technology to target other collagen-binding proteins using motifs from collagens that are specific for other receptors or matrix components. Previously, we synthesized THP libraries, called Toolkits, composed of an active guest sequence flanked by five GPP host triplets that
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br Clinical potential of ET
2019-08-01
Clinical potential of ET receptor biased ligands Is there a clinical need for ET receptor biased ligands? Evidence is strongest from research in epithelial ovarian cancer demonstrating that ET-1 stimulated ETA-mediated β-arrestin signalling leads to activation of the oncogenic mediator NF-κB [21]
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Because stimulation and blockade of dopamine D
2019-08-01
Because stimulation and blockade of dopamine D2 receptor all cause a similar disruption of maternal behavior, one critical question is whether they do so through the same or different behavioral mechanisms. One idea is that stimulation or blockade of D2 receptors similarly suppresses maternal motiva
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All DGKs have at least
2019-08-01
All DGKs have at least two cysteine-rich regions homologous to the C1A and C1B motifs of PKCs [26]. In theory, these domains may bind DAG, perhaps localizing DGKs to where DAG accumulates. However, no DGK C1 domain has so far been conclusively shown to bind DAG. In fact, structural predictions sugge
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Family and twin studies have estimated the heritability
2019-08-01
Family and twin studies have estimated the heritability of obesity to be between 40 and 70% [5], [6], [7]. However, all known risk variants can only account for ∼3% of the variance in BMI [8], [9]. Therefore, alternate methods are needed to identify additional risk factors. In recent decades, Drosop
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