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We next turned our attention
2020-01-08
We next turned our attention to the 6-position of the indole (). It was found that the chlorine atom present in was extremely important. The des-chloro analogue showed nearly 30-fold less affinity for the EP receptor in the binding assay and was nearly 30-fold lower in activity in the functional a
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Concerning family A GPCRs although
2020-01-08
Concerning family A GPCRs, although it has been described that several receptors are able to operate as monomers (Arcemisbéhère et al., 2010; Bayburt et al., 2011; Chabre & le Maire, 2005; Ernst, Gramse, Kolbe, Hofmann, & Heck, 2007; Hanson et al., 2007; Kuszak et al., 2009; Whorton et al., 2007), e
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In rodents but not humans two splice variants of
2020-01-08
In rodents but not humans, two splice variants of Chk are identified as Ntk and Ctk, which possess and lack the N-terminal unique domain, respectively. While Ctk is abundantly expressed in the brain, Ntk is selectively restricted to myeloid and lymphoid cells, especially megakaryocytes [31]. This ra
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br Acknowledgement We acknowledge for funding support from M
2020-01-08
Acknowledgement We acknowledge for funding support from Maryada Foundation, a DoD/Army Contract No. W911NF-06-1-0095, and National Institutes of Health through the New England Center of Excellence for Biodefense (Grant AI057159-01). Introduction The Gram-negative bacterium Lysobacter sp. XL1
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Nicotine is the main psychoactive component of tobacco that
2020-01-07
Nicotine is the main psychoactive component of tobacco that causes addiction. Besides the regulation of the stress responses, CRF has been implicated in nicotine addiction based on several lines of evidence (Bruijnzeel and Gold, 2005, Sarnyai et al., 2001). First, acute administration of nicotine, l
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br ET Antagonist for the Future Macitentan
2020-01-07
ET Antagonist for the Future: Macitentan and Atresentan Macitentan is an insurmountable antagonist, resulting from structure-activity studies to improve the efficacy and tolerability of bosentan, and gained approval in the United States in 2013 for the treatment of PAH. Actelion describes the com
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Nimodipine administration also inhibited the eIF ATF
2020-01-07
Nimodipine administration also inhibited the eIF2α/ATF4 singnaling which is a crucial evolutionarily conserved adaptive pathway during cellular stresses including hypoxia and ischemia (Evans et al., 2016; Manwani and McCullough, 2013). While, the eIF2a/ATF4 pathway, activated by different forms of s
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The estrogen receptor ER dependent
2020-01-07
The estrogen receptor(ER)-dependent signaling pathway plays an important role in bone metabolism by restoring the balance between osteoblastic bone formation and osteoclastic bone resorption [21]. ER has two major isoforms, ERalpha (ER-α) and ERbeta (ER-β), which mediate the effect of estrogen and o
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flavopiridol br Discussion Several DPP inhibitors are curren
2020-01-07
Discussion Several DPP-4 inhibitors are currently available for use in the treatment of type 2 diabetes mellitus. Due to the different chemical structures there are marked differences both in the binding kinetics on the target enzyme [10] and also different pathways of elimination [13] exist. In
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The binding of collagen X to DDR
2020-01-07
The binding of collagen X to DDR2 differs from the binding of collagen X to α2β1 integrin in that the triple helical conformation is essential for DDR2 binding. We previously reported that heat denatured pepsinised collagen X supported cell adhesion via α2β1, indicating that the triple-helical confo
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br Introduction Cardiovascular disease continues to be the l
2020-01-07
Introduction Cardiovascular disease continues to be the leading cause of death in developed countries. Atherosclerosis, a chronic inflammatory cardiovascular disease, is characterized by the progressive buildup of oxidized low density lipoproteins in the arterial walls (Ross, 1999). In the develo
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br Conflict of interest statement br
2020-01-06
Conflict of interest statement Acknowledgement The study was financially supported by the Ministry of Education, Youth and Sports of the Czech Republic – projects “CENAKVA” (No. CZ.1.05/2.1.00/01.0024) and “CENAKVA II” (No. LO1205 under the NPU I program), by the Grant Agency of the University
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Picrotoxin Based on the above background gliptins
2020-01-06
Based on the above background, gliptins may exert natriuretic and diuretic effects as well [[112], [119]]. In accordance with this, Girardi and co-workers have demonstrated a physical interplay between DPP-4 and the NHE3 exchanger in the brush-border epithelium of the proximal renal tubule, suggesti
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Semantics play an important role in software component based
2020-01-06
Semantics play an important role in software component-based development as they improve components identification, selection and integration through, among others, the use of ontologies (Kaur and Mishra, 2017). Analogously, they allow to improve discovery, composition and reuse in the context of We
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Multi subunit RING type E ligases are
2020-01-06
Multi-subunit RING-type E3 ligases are exemplified by the CULLIN-RING-ligase (CRL) and the anaphase-promoting complex/cyclosome (APC/C) [19]. CRLs constitute the biggest family of other multi-component E3 ligases. These consist of a cullin scaffold protein (CULLIN 1, 2, 3, 4A, 4B, 5, 7), a substrate
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