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Together the data suggests that more work needs to
2020-12-14
Together, the data suggests that more work needs to be done to establish the role of PARP inhibitors in Ewing sarcoma. As a single agent, there is some activity in Ewing sarcoma cell lines and a highly statistically significant relationship between olaparib sensitivity and EWS–FLI1 expression. Howev
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To develop novel EPAC inhibitors
2020-12-14
To develop novel EPAC inhibitors, Zhou and co-workers optimized the HTS hit as the chemical lead. After modifications of the substituents on the phenyl ring or C6-position of compound , compound () was identified to be the more potent compound in this series with an IC value of 4.0µM (EPAC2). Dock
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N Cyclopentylmethyl analog exhibited fold less potent recept
2020-12-14
N-Cyclopentylmethyl analog 25 exhibited 2.3-fold less potent receptor affinity and 1.6-fold less potent antagonist activity. Among the compounds tested, the N-isobutyl analog 23 showed the most potent EP1 receptor affinity and antagonist activity. In summary, a series of 4-( 2-[alkyl(phenylsulfonyl
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AS601245 br A major physiological action of ET is to
2020-12-12
A major physiological action of ET-1 is to function as one of the most powerful vasoconstrictors of human blood vessels. As such, ET-1 plays a major role in regulating vascular function in all organ systems, including the kidney (Fig. 1). As in other vessels, ET-1 is thought to be released from en
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Methacholine MCh is a bronchoconstrictive
2020-12-12
Methacholine (MCh) is a bronchoconstrictive agent that has been widely used in the diagnoses of airway narrowing and hyperresponsiveness (Jonasson et al., 2009). MCh induces muscle contractions by stimulating the muscarinic cholinergic receptors that are found in both the airways and the lung parenc
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melatonin receptor agonist PRRSV is a single stranded positi
2020-12-12
PRRSV is a single-stranded, positive-sense enveloped RNA virus in the family Arteriviridae of the order Nidovirales (Meng et al., 1994, 1996). The PRRSV melatonin receptor agonist is approximately 15 kb in length and contains eleven known open reading frames (ORFs) (Snijder et al., 2013). The 3′ end
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One question relates to our finding that oxysterol
2020-12-12
One question relates to our finding that oxysterol-GPR183 signaling is critical for CP and ILF formation in the colon but dispensable in the small intestine. GPR183 and its ligand were expressed in both the small and large intestines. Moreover, 7α,25-OHC was required for ILC3 migration to CPs not on
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br Acknowledgements We thank Dr James Ritchie and his
2020-12-12
Acknowledgements We thank Dr. James Ritchie and his dedicated staff (Deptartment of Pathology, Emory University) for performing measures of serum VPA levels; Sumitomo Pharmaceuticals (Osaka, Japan) for the generous donation of DOPS, which is required for breeding Dbh −/− mice; Pfizer (Sandwich, K
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br Discussion Although DNA has a limited chemical stability
2020-12-12
Discussion Although DNA has a limited chemical stability it has long been known that DNA in blood stains may remain relative stable for weeks, months, or even years at ambient temperature,1, 2, 3, 4, 5, 6 and samples (e.g., reference samples) that have been transferred to a matrix, e.g., FTA® pap
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There are a few visible DNA staining methods which use
2020-12-12
There are a few visible DNA staining methods, which use dyes such as methylene blue, brilliant cresyl blue [7], crystal violet [8], Nile blue [9], [10] and ethyl violet [11]. However, although safe, these methods require long staining times, lack sensitivity and are not specific for nucleic acids.
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Global inhibition of integrin signaling with
2020-12-12
Global inhibition of integrin signaling with EDTA here suggests that integrin signaling potentially cooperates with DDR2 in collagen induction of lysyl oxidase. This notion is supported by a recent study that shows DDR2 cooperation with specific integrins in cell adhesion to collagen [47]. It is of
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br Rationale Recently we have shown that the nasal
2020-12-12
Rationale Recently we have shown that the nasal CysLT2 receptor localized exclusively in blood vessels and the expression level of the CysLT2 receptor in patients with nasal allergy was higher than that in patients with non-allergic rhinitis (Shirasaki et al. Allergol Int 2013). We hypothesized t
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Proteins that associate to PCNA are
2020-12-11
Proteins that associate to PCNA are characterized by having conserved motifs as the PCNA-interacting protein (PIP) motif [29,30], its variant PIP-like motif [31,32] or the APIM motif (Alk B homologue 2 PCNA interacting motif [33,34]); for instance, p21 contains a PIP motif [30], and DNA polymerases
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The early serologic response of infants
2020-12-11
The early serologic response of infants to infection with HIV-1 is obscured by the presence of transplacentally acquired maternal HIV antibody. However, the HIV JQ1 synthesis produced in vitro by peripheral blood from infants has been studied (Pollack et al., 1993) and it has been shown that neonata
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Another important mediator in fear learning is the neuropept
2020-12-11
Another important mediator in fear learning is the neuropeptide corticotropin-releasing factor (CRF). For example, local repeated administration of CRF into the basolateral amygdala potentiates the acquisition of cue-conditioned fear (Bijlsma et al., 2011) and CRF1 receptor antagonists effectively b
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