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N Cyclopentylmethyl analog exhibited fold
2020-10-29
N-Cyclopentylmethyl analog 25 exhibited 2.3-fold less potent receptor affinity and 1.6-fold less potent antagonist activity. Among the compounds tested, the N-isobutyl analog 23 showed the most potent EP1 receptor affinity and antagonist activity. In summary, a series of 4-( 2-[alkyl(phenylsulfonyl
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br Conclusions Two chemical coupling agents BTDE
2020-10-29
Conclusions Two chemical coupling agents, BTDE and CDI, were used to activate the free hydroxyl groups of plant cellulose powder and OPH from Flavobacterium ATCC 27551 immobilized on modified carriers by covalent linkages. The highest immobilization yields obtained in optimum conditions of effect
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There are five phosphorylated serines in casein However only
2020-10-29
There are five phosphorylated serines in β-casein. However, only phosphorylated Ser35 was identified in the samples hydrolysed with GE at 37 and 50 °C, i.e., f32-42 and f32-44 of β-casein. The identification indicates that phosphorylated peptides were less detectable from the non-phosphorylated pept
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br Restenosis after angioplasty remains
2020-10-29
Restenosis after angioplasty remains a remarkable challenge, although drug-eluting stents have reduced the incidence of restenosis considerably . Vascular smooth muscle sesamin (VSMCs) play a pivotal role in the development of intimal thickening and restenosis. VSMCs proliferate and migrate from
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br DAG kinase activity is confined to specific cell compartm
2020-10-29
DAG kinase activity is confined to specific cell compartments A number of reports demonstrating agonist-dependent translocation of DGKs to distinct membrane compartments suggest that DGK activity is restricted to localized DAG pools generated after activation of receptors. Perhaps the best eviden
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br Cytokines and NK cells br
2020-10-29
Cytokines and NK cells Combined effects of cytokines and other stimuli on NK cell function Cytokine-stimulated NK daminozide receptor have enhanced capacity to kill tumor cells. However, usually, individual cytokines do not seem to be sufficient for full activation, proliferation, survival and
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procollagen c proteinase br Role of CRF receptors in the BNS
2020-10-28
Role of CRF1 receptors in the BNST in stress-induced relapse to cocaine seeking The seminal work of Stewart and co-workers [19] showed that rats that have extinguished their auto-administration of different drugs of abuse relapse to drug-seeking behaviour when exposed to footshock, even after a 4
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In the preclinical evaluation of CRF receptor antagonists ef
2020-10-28
In the preclinical evaluation of CRF1 receptor antagonists, effects were mainly focused on the regulation of hyperactivated HPA axis and the modulation of anxiety or depressive-like behaviors in CRF challenge [16], [17], [18] or stress models [16], [19], [20]. However, it remains to be concluded whe
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br Acknowledgments br Introduction Cell cycle
2020-10-28
Acknowledgments Introduction Cell cycle arrest or delay may occur at 3 major checkpoints, i.e. G1/S, intra-S and G2/M. p53 has a central role in controlling the G1/S checkpoint, and its loss or deactivation, occurring in the majority of cancers, forces cancer cells to rely on the S and G2/M ch
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Recently it has been shown that among
2020-10-28
Recently, it has been shown that among the ELR (+) chemokines mentioned above, particularly IL-8 induces neutrophil migration via CXCR-1 chemokine receptor. For example, Godaly et al. [18] reported the potent role of CXCR-1 chemokine receptor in the process of neutrophil migration across epithelial
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What is the predominant mechanism underlying the benefits of
2020-10-28
What is the predominant mechanism underlying the benefits of udenafil, i.e. the vascular vs. myocardial effect? Lewis et al. suggested that the benefit of sildenafil in HFrEF would be derived from augmented RV systolic function that mainly results from pulmonary vasodilation, suggestive of the ‘vasc
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Two isoforms of intracellular ER ER and ER
2020-10-28
Two isoforms of intracellular ER, ERα, and ERβ, after binding to estrogens and translocate to the nucleus, activate some transcription factors and signaling pathways. The deregulation of estrogenic pathways can elevate transcriptional activity contributed to the development of cancer. Expression of
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br Experiments br Numerical simulations br Discussion br
2020-10-28
Experiments Numerical simulations Discussion Conclusions By large-caliber PELE with various d/D against RHA plate at low velocity of 415 m s−1, impact experiments against 30 mm RHA target were carried out. Numerical simulations were also conducted to monitor progress of PELE expansion an
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Hinokitiol has versatile abilities as anticancer antimicrobi
2020-10-28
Hinokitiol has versatile abilities as anticancer, antimicrobial and molecule transport agents and appears to have no developmental toxicity or carcinogenic effects (Imai et al., 2006b). For anticancer activities, it causes apoptosis and AZD8931 arrest in many different types of cancers, such as mur
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Which other approaches can complement signaling
2020-10-28
Which other approaches can complement signaling optogenetics to paint a more complete picture of developmental Erk signaling? For now, the authors have dynamically manipulated Erk signaling but measured the Erk output at steady-state using classic immunofluorescence techniques (Johnson and Toettcher
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