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With respect to the muscle compartment only
2019-12-16
With respect to the muscle compartment, only low protein expression of ASB9 has been detected in healthy human skeletal muscle [as reported in the Human Protein Atlas (HPA)], whereas high levels of Asb5 protein expression are detected in mammalian skeletal muscle, which appears to be important in th
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Preparation of the regioisomeric pyridooxazepinones and was
2019-12-16
Preparation of the regioisomeric pyridooxazepinones 10 and 11 was accomplished utilizing the synthetic sequence depicted in Scheme 3. Amide coupling of 63 and PD 151746 chloride 64 afforded amide 65. Removal of the alcohol protecting group, followed by base catalyzed cyclization afforded a 1:2.4 mi
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Soluble receptors have been shown
2019-12-16
Soluble receptors have been shown to be important and common regulators of many cytokines within the immune system, including IL-1, IL-6, IFNγ, TNF-α, GM-CSF, G-CSF and others (Fernandez-Botran, 1991, Heaney, Golde, 1998). We previously described a novel soluble receptor, sCSF-1R, that to date has o
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These evidence prompted us to
2019-12-16
These evidence prompted us to investigate the effectiveness of CT-133, a newly discovered, well-tolerated, selective and potent CRTH2 antagonist, as a treatment of ALI. CT-133 has shown a potential response in treating chronic obstructive pulmonary disease (COPD), allergic rhinitis and KU57788 (Guo
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Our previous high throughput screening HTS campaign using au
2019-12-14
Our previous high-throughput screening (HTS) campaign using automated, robust, and sensitive fluorescence based IMD 0354 assay [10], [11] led to the identification of several EPAC specific inhibitors (ESIs), and was subsequently followed by extensive hit-to-lead optimizations [20], [21], [22], [23]
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br Physiological roles for EPAC isoforms
2019-12-14
Physiological roles for EPAC isoforms: vascular function The effects of cAMP on limiting vascular endothelial cell (VEC) inflammation and vascular smooth muscle cell (VSMC) proliferation have been well documented 36, 37, 38. However, recent work has demonstrated that several key effects of cAMP i
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NBI 27914 hydrochloride br Materials and methods br
2019-12-14
Materials and methods Results Discussion Schistosome cercarial elastase secreted from the acetabular glands of cercariae is recognized to play a critical role in mammalian host skin penetration upon infection. The present study extends the understanding of biochemical and immunological prop
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Multiple protein species are known to naturally
2019-12-14
Multiple protein species are known to naturally exist for the transmembrane receptors DDR1 and DDR2. Five splice variants have been characterized for DDR1 (“a” through “e”). The d and e isoforms lack the intracellular kinase domain of DDR1. The splicing of DDR1 to various extents has been reported i
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ACY-241 Through an unknown mechanism RING Ubox
2019-12-13
Through an unknown mechanism, RING/Ubox-type E3 dimers and the N-terminal tail have been shown to function as a modulator of full E3 ubiquitin ligase activity [27]. LRSAM1 promotes a significant enhancement in the formation of the high-molecular-weight products or E3 activity when the RING domain is
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As demonstrated by Mak and colleagues ER is
2019-12-13
As demonstrated by Mak and colleagues, ERβ is known to be a part of the NFκB-HIF-1α signaling pathway during hypoxia as well as chronic inflammation of prostate (Mak et al., 2015), therefore in the next part of the study, we evaluated whether ZEA-induced ROS production is also associated with NFκB-
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Furthermore elastase might not be the only regulator of CBG
2019-12-13
Furthermore, elastase might not be the only regulator of CBG on cleaved and uncleaved form. In a study by Nenke et al. [85] α1-AT deficient subjects, who lack this native neutrophil elastase inhibitor, paradoxically have higher levels of uncleaved CBG and lower levels of CBG* [85]. Gender differenc
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The Kaempferia parviflora extract met the criteria for a non
2019-12-13
The Kaempferia parviflora extract met the criteria for a non-competitive interaction with CYP1A1 based on the decrease of Vmax and unchanged Km. The high Ki value and low IC50, as well as the high Km value was indicative of the weakness of the interaction between the Kaempferia parviflora extract an
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br Discussion Nowadays data of uncommon EGFR
2019-12-13
Discussion Nowadays, data of uncommon EGFR mutations are limited, considering that patients carrying these rare alterations are usually excluded from clinical trials. Available survival data of activity of EGFR TKIs on this class of mutations, coming from a small number of usually retrospective s
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To investigate the role of DPP inhibition in
2019-12-13
To investigate the role of DPP-4 inhibition in inflammation-induced bone resorption, we evaluated the effect of a DPP-4 inhibitor on LPS-induced osteoclast formation and bone-resorption in vivo. Our results showed that the DPP-4 inhibitor inhibited LPS-induced osteoclast formation and bone resorptio
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guanylyl cyclase br DNA end processing enzymes
2019-12-13
DNA end processing enzymes The simplest DSB is one that consists of two blunt DNA ends as these termini can be re-joined without processing. However, DSBs induced by ionizing radiation and reactive oxygen species are notorious for producing DNA ends which are non-ligatable (“dirty ends”) and thus
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