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A number of chemical strategies have been developed to
2020-07-17
A number of chemical strategies have been developed to design activatable optical imaging probes and have been summarized in several excellent reviews 11., 12., 13., 14., 15.. Fluorogenic enzyme substrates are one of the most explored activatable probe types for enzyme detection. These probes contai
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Although many of the genetic changes remain to be
2020-07-16
Although many of the genetic changes remain to be elucidated, there is evidence to support a difference in incidence and rate of rupture of cerebral aneurysms between men and women, and between pre- and postmenopausal women, suggesting that aneurysm formation may be affected by hormonal changes.18,
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Enlarging the ligand binding pocket by reduction of
2020-07-16
Enlarging the ligand-binding pocket by reduction of the size of the residue F435 switched DES to an agonist indicating that F435 is involved in mediating the antagonistic effect of DES (Fig. 7E) [13]. The conformation of the smaller side chain of L435 was either not altered by DES or was too small t
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Studies have shown that endothelial
2020-07-16
Studies have shown that endothelial cells damaged by SAH can release a large amount of ET-1, thus its plasma level is elevated and is positively correlated with the symptoms of SAH (Lei et al., 2015, Masaoka et al., 1989). Our data obtained from SAH-along rabbits were consistent with these findings.
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br Additional CDKs with a role in cancer br Small
2020-07-16
Additional CDKs with a role in cancer Small molecule CDK inhibitors The majority of protein kinase inhibitors developed to date are type I inhibitors: they bind at the ATP–binding site, are ATP-competitive and target the kinase in its active state; with the activation loop DFG motif in the ‘in
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The large body of structural knowledge
2020-07-16
The large body of structural knowledge that is currently available for CRM1 has contributed to atomic level and mechanistic understanding of many steps in the CRM1 nuclear export cycle. However, structural analysis could still inform on several outstanding questions and guide future discoveries pert
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Synthetic peptides have proven highly valuable in
2020-07-16
Synthetic peptides have proven highly valuable in replicating the characteristics of collagen and in defining the sites on collagen essential for binding and studying protein–collagen interactions. There are, however, disadvantages to synthetic collagen-like peptides. First, the thermal stability of
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Finally considering the encouraging inhibitory and selectivi
2020-07-16
Finally, considering the encouraging inhibitory and selectivity properties of compound and against isolated CK1δ, we have also acquired a very preliminary cytotoxicity profile on human ovarian carcinoma cell line (2008) and on its cisplatin-resistant clone (C13). Results showed that after 48h of e
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Natural progestogens play an important role
2020-07-16
Natural progestogens play an important role in the stimulation of oocyte growth and maturation as well as in spermatogenesis and sperm maturation, and they act as sex pheromones in teleost fish (Kime, 1990, Kobayashi et al., 2002, Nagahama and Yamashita, 2008, Scott et al., 2010). A complex series o
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LY 2389575 hydrochloride br Effects of estrogen on vascular
2020-07-16
Effects of estrogen on vascular function Atherosclerosis is a chronic inflammatory condition of the vascular wall (Figure 1) that can be converted to an acute clinical event by the induction of plaque rupture or erosion, leading to thrombosis [58]. This perpetuating process is characterized by ph
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Treatment with AAV EP also improved aspects of adverse
2020-07-16
Treatment with AAV9-EP4 also improved aspects of adverse cardiac remodeling. The increased collagen deposition noted in the peri infarct and remote zone after MI was substantially attenuated by use of AAV9-EP4 and there were significant reductions in the number of macrophages and T AZD0156 infiltra
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It has been observed in our results that patients carrying
2020-07-16
It has been observed in our results that patients carrying risk allele “a” are at the greater risk of developing psoriasis. Same results have been presented by Coto-Segura et al., 2011, in a study conducted on Spanish population where they reported association of VNTR polymorphism among the patients
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br Acknowledgments br Introduction br Endothelin receptors S
2020-07-16
Acknowledgments Introduction Endothelin receptors Shortly after the discovery of ET‐1, two types of seven transmembrane G protein‐coupled receptors were cloned called endothelin receptor A (ETA) (Arai et al., 1990) and ETB (Sakurai et al., 1990). The affinity of the ETA receptor for ET-3 is
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The small intestine in addition to its primary role of
2020-07-16
The small intestine, in addition to its primary role of absorption, has the ability to metabolize drugs and other xenobiotics through phase 1 and phase 11 metabolisms [25] since almost all the cytochrome P450 GS967 australia present in the liver are also present in the small intestine although, in
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The development of novel approaches to study
2020-07-16
The development of novel approaches to study GPCR-mediated transactivation in live NVP 231 is important, and this study describes a unique BRET-based quantification of Grb2 recruitment to the EGFR as a direct readout of GPCR-mediated transactivation. We have previously used the recruitment of Grb2
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