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Our previous high throughput screening HTS campaign using
2020-11-20

Our previous high-throughput screening (HTS) campaign using automated, robust, and sensitive fluorescence based health-related assay [10], [11] led to the identification of several EPAC specific inhibitors (ESIs), and was subsequently followed by extensive hit-to-lead optimizations [20], [21], [22]
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Given that CE plays an essential
2020-11-20

Given that CE plays an essential role in schistosome invasion, its immunoreactivity and protective potential is of significant interest. The native form of SmCE was found to be poorly immunogenic in immunized mice. An earlier study found that sera from S. mansoni patients have shown the presence of
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br Funding This work was partly
2020-11-20

Funding This work was partly supported by the grant ‘Maria Grazia Cuccoli’ from Fondazione Cassa di Risparmio di Bologna. Declarations of interest Acknowledgements Introduction The main strategy of oncolytic viral therapy is based on the fact that naturally occurring or engineered virus
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br Results br Discussion It has
2020-11-20

Results Discussion It has been thought that commitment to the plasma cell fate begins while DBeQ are still in the GC (Suan et al., 2017, Victora and Nussenzweig, 2012), but the main obstacle to test this model and, if correct, to clarify how the plasma cell-prone GC cells develop has been our
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Protein degradation via UPP involves two steps
2020-11-20

Protein degradation via UPP involves two steps. One step is the conjugation of multiple ubiquitin to a substrate. The other step is the degradation of tagged protein by the downstream 26S proteasome complex. Protein ubiquitination is the E1–E2–E3 enzymatic cascade (Hershko & Ciechanover, 1998). E1-a
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Against this backdrop we set
2020-11-20

Against this backdrop, we set out to identify synthetic and endogenous ligands that bind directly to and regulate the activity of Nurr1. Owing to the pivotal role Nurr1 plays in producing and processing dopamine, and the need for neurons to tightly regulate dopamine levels, we postulated that the re
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At this stage it is
2020-11-20

At this stage it is still difficult to assign specific domains to some of the regions observed in these structures, although some attempts have already been made (Brewerton et al., 2004). Clearly, higher resolution data is needed. In the future, even if an atomic structure of DNA-PKcs is determined,
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During the past three decades platinum based DNA alkylating
2020-11-20

During the past three decades, platinum-based DNA-alkylating agents have been employed in the treatment of various cancers [14]. Oxaliplatin is currently used as a first-line treatment for colorectal cancer (CRC) [15]. Unfortunately, a large portion of CRC patients receiving oxaliplatin-based chemot
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Compound was synthesized by the directed metallation procedu
2020-11-20

Compound () was synthesized by the directed -metallation procedure (DOM) at the stage of the amide using butyl lithium and dry ice as CO source for the introduction of the carboxylic group. Thiophene amides were prepared from commercial 3-thiophenecarboxylic Immunology Inflammation Compound Library
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The current study provides evidence for a previously unknown
2020-11-20

The current study provides evidence for a previously unknown role for DHODH as a growth/survival factor in KRAS mutant tumors. While many aspects of the link between DHODH inhibition and survival of KRAS mutant cells remain to be established, de novo pyrimidine biosynthesis appears to be a crucial p
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br Materials and methods br Results br Discussion
2020-11-19

Materials and methods Results Discussion In this study, we developed a new CysLT1 and CysLT2 receptors-mediated f4 cat guinea pig model for screening both CysLT2 receptor and CysLT1/2 receptor antagonists. Unlike human CysLT2 receptors, which are equally stimulated by both LTC4 and LTD4[9]
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Substitutions on the benzene ring of the phenyl acetic
2020-11-19

Substitutions on the benzene ring of the phenyl acetic RNA moiety were evaluated to study their effect on DP and CRTH2 selectivity (). Compound has strong affinity for CRTH2, but it only has moderate affinity for DP. Small substitutions such as methoxy () and fluorine () next to the aryloxy group
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In rats exposed to day of
2020-11-19

In rats exposed to 1 day of nicotine withdrawal (24 h after the last nicotine administration) we expected a decrease of general locomotor activity and a decrease of global striatal dopamine release, which were assessed in a previous study following 14 days of nicotine exposure and 24 h of nicotine w
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prostaglandin receptor Large yellow croaker Larimichthys cro
2020-11-19

Large yellow croaker (Larimichthys crocea) are widely cultured in China but have inferior meat texture compared with wild fish. This result results from excess lipid deposition in the muscle, which reduces mechanical strength (Thakur et al., 2003). The liver is the central of lipid metabolism and st
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In the context of our ongoing studies to define
2020-11-19

In the context of our ongoing studies to define the phytochemical and biological properties of oxyprenylated secondary metabolites of plant and fungal origin, we wish to report herein the investigation on the interaction of some natural and semisynthetic O-alkylcoumarins with promising ChE inhibitor
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