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Propranolol initially discovered in is
2020-08-26
Propranolol, initially discovered in 1964, is first and most widely studied as a non-selective beta-blocker. Propranolol through β-adrenergic receptor blockade has reduced heart rate and blood pressure and have anti-arrhythmogenic and anti-ischemic effects, and been proposed as an effective strategy
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The question remains however as to
2020-08-26
The question remains, however as to the downstream signaling by Epacs that contributes to persistent sensitization of sensory neurons. Activation of the Ras family of GTPases by Epac1 (RapGEF3) or Epac2 (RapGEF4) (Bos, 2003, de Rooij et al., 1998) is linked to a number of downstream signaling effect
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br EphB as a therapeutic target in cancer Eph
2020-08-26
EphB4 as a therapeutic target in cancer Eph receptors and ephrins are promising new therapeutic targets in cancer. Various strategies have been employed to evaluate the interference of tumor-promoting effects or the enhancement of tumor suppressive effects. The inhibition of the Eph-ephrin system
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More than thirty enzymes with PLA activity have been
2020-08-26
More than thirty enzymes with PLA2 activity have been described and, based on sequence similarities, they are currently classified in 16 groups, each containing several sub-groups [16]. However, based on biochemical features these enzymes are frequently grouped into six major families: secreted phos
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br Introduction Our understanding of how ligands interact
2020-08-26
Introduction Our understanding of how ligands interact with G protein coupled receptors is evolving, particularly the recognition that some have the ability to preferentially activate a subset of intracellular signalling cascades – so called pathway biased ligands [1]. Additionally, it is now acc
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br Introduction Epithelial mesenchymal transition EMT is a
2020-08-26
Introduction Epithelial-mesenchymal transition (EMT) is a biological process by which epithelial Eeyarestatin I lose cell polarity and cell-cell adhesion, and gain mesenchymal features with an increase of migratory and invasive properties [1]. EMT is essential for mesoderm formation during embry
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br Results br Discussion The ubiquitin system
2020-08-26
Results Discussion The ubiquitin system has in recent years become an exciting area for drug discovery (Cohen and Tcherpakov, 2010), as multiple enzymatic steps within the ubiquitylation process are druggable. The potential of targeting the ubiquitin-proteasome pathway was first demonstrated i
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br Conclusion The results of the current study show
2020-08-26
Conclusion The results of the current study show that boldness is associated with higher gene expression of drd2a, drd2b and oprd1b in zebrafish males. The results are correlational and additional experiments are needed to clarify the causal role of these receptors in zebrafish behavior. Confl
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AVE 0991 Upstream Stimulatory Factor USF binding to the
2020-08-26
Upstream Stimulatory Factor (USF) binding to the −65 E-box is required for the regulation of FAS promoter activity in fasting/feeding [97], [98]. DNA-PK are identified as a USF-interacting protein [99]. In response to feeding/insulin, the transient double-stranded DNA breaks occurred during the tran
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Does a universal mechanism for TLS exist Our previous
2020-08-26
Does a universal mechanism for TLS exist? Our previous studies using the bacteriophage T4 DNA polymerase generated the model provided in Fig. 7 that quantifies the molecular forces influencing key steps in the polymerization pathway during the replication of a non-instructional versus miscoding DNA
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The pathogenesis of formation of an
2020-08-24
The pathogenesis of formation of an intradural tumor is unclear. Initially, several lines of evidence suggested a neural crest cell of origin for Ewings’s sarcoma based on expression of neuroectodermal markers on tumor Exemestane australia [45,46]. However more recently, studies have shown that exp
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The structure of the HOIP
2020-08-24
The structure of the HOIP RBR–LDD module bound to UbcH5~Ub reveals insights into an activated HOIP component [47]. Contacts between the E2~Ub and the non-cognate RBR module in the crystal suggest how a structure in which the active sites of the E2 and the E3 are in close proximity might look. In thi
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We recently described the benzoxazin one analogue
2020-08-24
We recently described the 1,3-benzoxazin-4-one analogue of LY294002 and showed it to have pan-PI3K and DNA-PK activity [2]. We have also reported on the activity of other family members, such as 3 which causes sensitization of lung cancer and colon cancer cells to radiation [11] and 4 (LTUSI122) as
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Although high concentrations of SCR
2020-08-24
Although high concentrations of SCR7-G and SCR7-R inhibited LigIV as reported [11], the SCR7 derivatives were more effective inhibitors of LigIIIα and, in particular, LigI. Although it is possible that differences in the DNA substrate underlie this discrepancy, it appears more likely that this refle
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Thus RhoA mediated inhibition of DGK
2020-08-24
Thus RhoA-mediated inhibition of DGKθ is a well-characterized pathway, conserved from C. elegans to mammalian tissues, which enables G-protein coupled receptors to regulate the extent and kinetics of DAG-mediated signaling by fine tuning DGK enzymatic activity. Acknowledgments Introduction Ce
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