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DiscoveryProbe™ Inhibitor Library In the present work we ask
2019-09-26
In the present work, we ask whether rNMP incorporation is an evolutionarily conserved property of DNA synthesis in Archaea. For this purpose, we used the best characterized hyperthermophilic anaerobe, Pyrococcus abyssi GE5 [47]. This strain duplicates its genome as fast as Bacteria, supported by euk
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It is conceivable however that the distortion induced by ado
2019-09-26
It is conceivable, however, that the distortion induced by adozelesin in dsDNA may decrease the processivity of the translocating RecBCD enzyme so that it dissociates more frequently from adducted DNA relative to unmodified DNA. Premature termination from the DNA would also produce partially unwound
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The overall shape of p iSH is dramatically
2019-09-26
The overall shape of p110α/iSH2 is dramatically different from DGKB or SK1, instead of forming a homodimer, p110α/iSH2 heterodimer has a triangular shape with iSH2 laying on the top and ABD, RBD, helical and kinase domain of p110α sitting in the bottom (Fig. 2B) (Gabelli et al., 2010; Huang et al.,
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In these studies the inflammatory
2019-09-26
In these studies, the inflammatory cytokine IL-8 was demonstrated as one of the responsible molecules induced by CysLTs via activating CysLT2 receptors. IL-8 is synthesized in and released from mononuclear cells, macrophages, fibroblasts and airway epithelial cells, and it promotes inflammation as a
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Our present data show that neuroleptics can affect CYP
2019-09-26
Our present data show that neuroleptics can affect CYP3A via a direct interaction with the enzyme and a significant indirect mechanism (enzyme regulation) produced in vivo. The obtained results revealed interactions of the neuroleptics (added in vitro to control liver microsomes, Model I) with rat C
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Proteins that associate to PCNA
2019-09-26
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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To better understand the mechanism of splicing in CLCN
2019-09-26
To better understand the mechanism of splicing in CLCN1, we began by constructing a minigene spanning exons 5–7 of CLCN1, resulting in the synthetic CLCN1 (5–7) minigene. We also established a new assay using real-time reverse transcription (RT)-PCR, which can distinguish between splicing variants b
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A more refined picture of
2019-09-26
A more refined picture of cholinesterase activity patterns may be obtained by measuring ChE activity of the same sample before and after addition of certain cholinesterase inhibitors, with differential specificity for different components of total ChE activity, such as BW284c51 (BW1,5-bis-(4-allyldi
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Pyoluteorin br Materials and methods br Results
2019-09-26
Materials and methods Results Discussion PKA and Epac are two principal effector proteins involved in cAMP signaling; they are expressed in a wide range of tissues and control diverse biological functions [10]. The existence of two cAMP effectors provides more precise regulation of cAMP sig
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The ADME profile of AAT was very
2019-09-26
The ADME profile of AAT-008 () was very promising, with high stability in HLM. The pre-clinical pharmacokinetic properties of AAT-008 were also assessed in rats (Sprague-Dawley, male), dogs (beagle, male), and monkeys (cynomolgus, male). The experimentally determined parameters are summarized in .
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br O GlcNAc transferase OGT belongs to
2019-09-26
O-GlcNAc transferase OGT belongs to the metal-independent GT-B superfamily of glycosyltransferases, which has been well-reviewed previously [14,15]. OGT is an essential gene encoded on the X-chromosome, and it has two main regions: a long N-terminal tetratricopeptide repeat (TPR) region and a C-t
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Further modifications on the position
2019-09-25
Further modifications on the 8-position of compound led to compound 4 (8-pCPT-2′--Me-cAMP, a.k.a. 007, ), which is a potent (half-maximal activation of EPAC1 at 2.2µM) and selective (about 100-fold EPAC/PKA selectivity) EPAC agonist. Since the discovery of compound , it has been widely used as a po
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The effects of the endocrine active agents
2019-09-25
The effects of the endocrine active agents on hepatic ERα were varied. Both nonylphenol and genistein caused an increase in hepatic ERα in female rats, whereas EE2 did not. It is doubtful that the small changes in hepatic ERα induced by genistein and nonylphenol in female rats are sufficient to alte
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Introduction Cognitive impairment is a core stable feature
2019-09-25
Introduction Cognitive impairment is a core, stable feature of schizophrenia that limits patient functioning and well-being (Keefe and Harvey, 2012) and associates with poor functional outcome (Fervaha et al., 2014, Kontaxaki et al., 2014). Studies also indicate that cognitive deficits occur prior
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Introduction Rotavirus RV a member of Reoviridae family is a
2019-09-25
Introduction Rotavirus (RV), a member of Reoviridae family, is a non-enveloped virus which has a double-stranded RNA genome of 11 segments surrounded by three concentric protein layers. It has been reported to cause estimated 25% of moderate-to-severe illnesses (Kotloff et al., 2013) and 30% of tot
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