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Repulsive interactions towards undesirable substrates are ar
2019-07-13
Repulsive interactions towards undesirable substrates are arguably a very efficient means to implement specificity [8]. In particular, it could be assumed that discrimination against a substrate that is larger than the cognate substrate may be achieved easily by restricting the active site and explo
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Anaesthetized mice of one eNOS KO
2019-07-13
Anaesthetized mice of one eNOS-KO strain showed a paradoxical decrease in blood pressure (BP) in response to i.p. administration of the NOS-inhibitor L-NA suggesting a role for non-endothelial isoforms of NOS in maintaining BP [1]. Alternatively, diminution in the activity of the renin-angiotensin s
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br Concluding Remarks Recent studies have provided
2019-07-13
Concluding Remarks Recent studies have provided unprecedented details of APC/C structure and enzymology, which explain how the activity of this massive E3 ligase is controlled, and how ubiquitylation is achieved to temporally regulate cell division. Although one pervasive question has been why th
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Each of these substrate receptors
2019-07-13
Each of these substrate receptors belongs to a multigene family with tens, if not hundreds of members in plants, and with in part overlapping and in part differential substrate specificities [4]. The complexity of the system is nicely illustrated by the F-box protein and auxin receptor TRANSPORT INH
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Atipamezole hydrochloride Fig S an
2019-07-13
Atipamezole hydrochloride (Fig. S1), an α2-adrenoceptor antagonist, is commonly used by veterinarians to recover animals from sedation-anesthesia induced by α2-adrenoceptor agonists. Recent studies in animals suggest that atipamezole might have beneficial effects in AZD7545 weight damage repair, it
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The current study showed that the tested nonselective COX in
2019-07-13
The current study showed that the tested nonselective COX inhibitors potentiated the neuronal (EFS) and endothelial (ACh)-dependent relaxation of rat corpus cavernosum. Indomethacin was the most effective among them in potentiating EFS-induced relaxation. Diclofenac was the most effective in potenti
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The reference standards methyl difluoro dioxolo
2019-07-13
The reference standards methyl 3-((2,2-difluoro-5-[1,3]dioxolo[4′,5′:4,5]benzo[1,2-]imidazol-6-yl)carbamoyl)benzoate () and -(2,2-difluoro-5-[1,3]dioxolo[4′,5′:4,5]benzo[1,2-]imidazol-6-yl)-3-methoxybenzamide (), and their corresponding desmethylated precursors 3-((2,2-difluoro-5-[1,3]dioxolo[4′,5′:
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We showed for the first time that ivermectin significantly
2019-07-13
We showed for the first time that ivermectin significantly reduced the pH-induced response of the pHCl-A variant at 300nM, whereas fipronil and γ-BHC had no significant effects on the channel unlike in RDL and GluCl (Fig. 4). Such a concentration is similar to the threshold at which ivermectin activ
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Damage of PE HD due to both
2019-07-13
Damage of PE-HD due to both mechanisms is usually considered to emerge from a local stress concentration in the material, leading to the initiation of a crack, which subsequently propagates further through the material, and finally leads to macroscopic failure. In this process, crack growth occurs o
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br Introduction Cell transplantation therapies using embryon
2019-07-13
Introduction Cell transplantation therapies using embryonic stem cell (ESC) and induced pluripotent stem cell (iPSC)-derived retinal tissue (ESC/iPSC retina) or W146 have emerged as therapeutic options for retinal degeneration following recent breakthroughs. A number of groups have shown that tra
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Our previous high throughput screening HTS campaign using
2019-07-13
Our previous high-throughput screening (HTS) campaign using automated, robust, and sensitive fluorescence based bcr-abl inhibitor 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], [2
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br Chemistry The test compounds listed
2019-07-13
Chemistry The test compounds listed in Table 1, Table 2, Table 3, Table 4, Table 5, were synthesized as outlined in Scheme 1, Scheme 2, Scheme 3, Scheme 4, Scheme 5. Synthesis of 2–5 is described in Scheme 1. N-Sulfonylation of the aniline 26 with benzenesulfonyl chloride afforded the sulfonamide
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br Methods br Results br Discussion The findings of
2019-07-13
Methods Results Discussion The findings of this study indicate that an ET system including ET-1 and ET-2 as well as ET receptors are present in the retina and RPE/choroid, and are up-regulated by both hypertension and diabetes. Specifically, individual antagonism of the ETRA or ETRB delive
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E3330 molecular br Conflict of interest br Acknowledgments P
2019-07-12
Conflict of interest Acknowledgments Part of this work was supported by Institut Francais en Egypte, and the Academy of Scientific Research and Technology in Egypt under the frame of “Imhotep Project N°: 31681XL” and “STDF/IFE project N° 30630″ Introduction NSAIDs play an important role in
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br Involvement of p MAPK pathway
2019-07-12
Involvement of p38 MAPK pathway The NF-κB signal transduction cascade is a major stress response signaling pathway for the COX-2 gene expression. In mice and humans, the COX-2 promoter has BET bromodomain inhibitor what for many transcription factors, including NF-κB in the 5′ region of the COX-
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