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We recently identified a G A dependent epigenetic mechanism
2023-01-10
We recently identified a G9A-dependent epigenetic mechanism for transcriptional activation of the serine pathway in cancer cells (Ding et al., 2013). G9A, also known as EHMT2 and KMT1C, is a H3K9 methyltransferase that has a primary role in catalyzing H3K9me1 and H3K9me2 in euchromatin (Shinkai and
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NLX a k a F or befiradol exhibits nanomolar affinity
2023-01-10
NLX-112 (a.k.a. F13640 or befiradol), exhibits nanomolar affinity at 5-HT1A receptors, and, in ptio mg to the 5-HT1A receptor agonists listed above, it presents exceptional selectivity and high efficacy at these receptors (Colpaert et al., 2002, Newman-Tancredi et al., 2017). Additionally, it has s
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During the course of our ACK inhibitor program a high
2023-01-10
During the course of our ACK1 inhibitor program, a high-throughput screening (HTS) campaign of our internal sample collection was conducted. A series of -aryl pyrimidine-5-carboxamides of the general structure () was identified. Earlier studies of the structure–activity relationship (SAR) of ident
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MicroRNA miRNA is an abundant group of small nucleotide nonc
2023-01-10
MicroRNA (miRNA) is an abundant group of small (22-nucleotide) noncoding RNA molecules that directly binds with 3′ untranslated region (UTR) of target messenger RNAs (mRNAs) to regulate gene expression, playing an important role in variety of biological processes including cell proliferation, apopto
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Using our infection assays we also explored whether low
2023-01-10
Using our infection assays, we also explored whether low-pH compartments were required for the entry of ZIKVs in mammalian cells. Lysosomotropic agents such as ammonium chloride, chloroquine and Bafilomycin A1, strongly inhibited the ability of ZIKVs to enter mammalian cells. Our results are in agre
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br Introduction Stroke is a devastating condition that cause
2023-01-10
Introduction Stroke is a devastating condition that causes cognitive and motor dysfunction, neurodegenerative diseases and even acute death, and is a leading cause of mortality and morbidity worldwide (Chen et al., 2014a, Wang et al., 2016). Thus, exploration or identification of novel therapeuti
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PF also a dual Aurora A and Aurora B
2023-01-10
PF-03814735, also a dual Aurora-A and Aurora-B inhibitor, was administered in a phase I dose escalation study in a 3-weekly atipamezole for 5 or 10 consecutive days [69], [70]. To date 25 patients have been included in 7 dose levels (5–100mg/day for 5 days). Using the 5-day schedule the MTD was def
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Introduction the DNA damage response important
2023-01-10
Introduction: the DNA damage response — important implications for tumour development and treatment Cells are invariably challenged by tens of thousands of lesions inflicted on their DNA everyday (Lindhal, 1993). This DNA damage can be caused exogenously by exposure to different types of radiation
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We have shown that an extensive region in SERBP amino
2023-01-10
We have shown that an extensive region in SERBP1 (amino acids 354 to 474, using co-ordinates based on the full-length isoform, Figs. 1a and 2) is necessary for it to interact with RACK1; since this region has substantial homology to the corresponding region of HABP1 (Fig. 3) it is a reasonable hypot
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Alectinib is a second generation ALK
2023-01-09
Alectinib is a second generation ALK antagonist that is built upon a 9-ethyl-6, 6-dimethyl-11-oxo benzo[b]carbazole scaffold (Fig. 5C) [58]. This drug is effective against the ALK L1196M gatekeeper mutation along with C1156Y and F1174L mutations [7]. The 11-oxo group of the drug forms a Carbetocin
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The reduced IFN production seen
2023-01-09
The reduced IFNγ production seen with BPAL10-primed splenocytes could potentially be attributed to the impaired intracellular survival of B. pertussis, thereby leading to a weakened induction of cell-mediated immunity. Earlier studies have suggested an antimicrobial role of IFNγ in mediating the eli
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The biology of the A BR is
2023-01-09
The biology of the A2BR is complex and needs to be considered contextually as the expression and effect of receptor engagement varies according to time post hypoxic injury, cell type and downstream signaling pathway. For example, A2BR expression is dynamic - low under basal and increasing under isch
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Streptomycetes are a group of filamentous
2023-01-09
Streptomycetes are a group of filamentous Gram-positive, soil-inhabiting bacteria which have captured enormous screening interest because of their ability to produce and secrete a variety of 398 and extracellular proteins [7]. Among the diverse antibiotics produced by Streptomycetes are the nucleosi
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Materials and methods br Results
2023-01-09
Materials and methods Results Discussion The BV-tag-based electrochemiluminescence immunoassay is an extremely sensitive assay. It has been employed for detecting analytes present in only picogram quantities (e.g., bacterial toxins [26], Hyper Assembly Cloning [19]), measuring the activity o
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Most studies on d penicillamine induced
2023-01-09
Most studies on d-penicillamine-induced MG were performed before the discovery that some MG patients have anti-MuSK antibodies. After the identification of the present case, we retrospectively tested the stored frozen sera of ten earlier identified d-penicillamine MG patients with anti-AChR rb 1 mg
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