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In order to evaluate the in vivo pharmacology associated
2020-08-22
In order to evaluate the in vivo pharmacology associated with EP receptor antagonism, we wished to discover antagonists presenting a higher degree of selectivity over the other prostanoid receptors. We also wanted to increase the brain–blood ratio since it is probable that centrally mediated EP agon
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When six chemical inhibitors were
2020-08-21
When six chemical inhibitors were incubated with TRB or TRC and human liver microsomal preparation, HLM2, the results showed that ketoconazole (a CYP3A4 inhibitor) was very effective in inhibiting 4β-C hydroxylation of TRB and TR, whereas sulfaphenazole (a CYP2C9 inhibitor) and quinidine (a CYP2D6 i
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LDN 57444 At this stage it is still difficult to assign
2020-08-21
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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Soybean Glycine max is an important oilseed
2020-08-21
Soybean (Glycine max) is an important oilseed and can be a useful source of epoxy fatty acids (EFAs). This UFA contains an oxygen bridge across adjacent carbon atoms at single or multiple positions in the acyl chain, making them highly reactive and prone to cross-linking, and thus valuable industria
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Based on the deduced amino acid sequence of
2020-08-21
Based on the deduced amino GSK J1 sequence of the catalytic subunit of rG3DH, we could find sequence features that are highly conserved in FAD-harboring dehydrogenase, which include FAD binding motif and sequential cysteine residues in Cysteine-rich region. Several dehydrogenases share similarity of
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Keratin K has been identified as the
2020-08-21
Keratin 8 (K8) has been identified as the first intermediate filament expressed during development in amphibians and mammals. In zebrafish, a type II cytokeratin 8 (zf-K8) cDNA has been cloned. zf-K8 gene was maternally inherited and expressed in all surface cells throughout the embryonic stages old
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To overcome problems with the biochemical reconstitution of
2020-08-21
To overcome problems with the biochemical reconstitution of these heterodimeric cytokines fusion strategies linking both subunits together have been proposed inspired by the “hyper-IL-6” [28]. Much like fusing a protein to a solubility enhancing protein such as MBP or SUMO, fusing two subunits of a
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Apart from its high affinity the selection
2020-08-21
Apart from its high affinity, the selection of GW2580 as Bax inhibitor peptide P5 lead in our radiotracer development program was motivated by its exceptional selectivity. The observed profound impact of small structural modifications on the selected panel of four kinases tested prompted us to condu
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The presence of a vicious cycle
2020-08-21
The presence of a “vicious cycle” established between tumor proliferation and paratumor osteolysis plays a crucial role in the development of primary bone tumors [53]. Cancer cells produce soluble factors that activate directly or indirectly via osteoblasts, osteoclast differentiation and maturation
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The T cell receptor TCR
2020-08-21
The T cell receptor (TCR) pathway is associated with T cell activation and differentiation. When specific antigen peptides are recognized by the TCR, lymphocyte-specific protein tyrosine kinase (lck) phosphorylates the immune-receptor tyrosine-based activation motifs (ITAMs) of the TCR-CD3 complex a
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Long stretches of ssDNA have also been observed in rad
2020-08-20
Long stretches of ssDNA have also been observed in rad53-1 mutant Lonidamine under replication stress using EM images (Sogo et al., 2002). Deletion of EXO1, a 5′-to-3′ exonuclease, can suppress the generation of ssDNA detected in rad53-1 mutant cells (Cotta-Ramusino et al., 2005). It was thus propos
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Introduction Psoralea corylifolia L Leguminosae
2020-08-20
Introduction Psoralea corylifolia L. (Leguminosae) is a well-known traditional Chinese medicine, and it has been widely used for the treatment of various diseases like bronchial asthma, leucopenia, vitiligo and psoriasis in East Asian countries (Zhang et al., 1990). Previous studies have reported t
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br Clinical trials of CRM inhibitors KPT clinical trials hav
2020-08-20
Clinical trials of CRM1 inhibitors KPT-330 clinical trials have been initiated with promising very early results. One trial includes patients with advanced solid tumors whose disease has progressed after at least one prior therapy for metastatic disease (NCT01607905). Another trial includes patie
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br Methods br Results br Discussion On the
2020-08-20
Methods Results Discussion On the other hand, surgical patients have to some extent stress during pre- and/or post-operative period. It is well known that CRF/CRF1 receptor is involved in the activation of HPA during acute and chronic stress (Papadimitriou and Priftis, 2009, Zelena et al.,
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R428 Semantics play an important role in software component
2020-08-20
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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