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Previously we have reported that magnitude of
2021-04-27
Previously, we have reported that magnitude of the disruption of the blood–aqueous barrier after paracentesis was reduced by 82% in EP4 receptor knockout mice (Biswas et al., 2006). In the present study, we observed that pretreatment of EP1 receptor knockout mice with EP4 receptor antagonist, reduc
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biotin products br O GlcNAcase Human OGA is a multidomain
2021-04-27
O-GlcNAcase Human OGA is a multidomain protein with an N-terminal domain similar to glycoside hydrolase family 84 (GH84) enzymes, a stalk domain, a C-terminal pseudo histone acetyltransferase (HAT) domain, and several low-complexity regions (Figure 1f) [43]. A splice variant that lacks the HAT do
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Compared to ET all agonists tested showed a fold
2021-04-27
Compared to ET-1, all agonists tested showed a 2–4 fold bias for the G protein constrictor assay compared to the β-arrestin assay (Table 1). This preliminary analysis indicated that at least modest pathway bias for endogenous ET peptides is possible, however the physiological significance of this, i
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EBI and its ligand s EBI was found in
2021-04-27
EBI2 and its ligand(s) EBI2 was found in a screen of upregulated genes in human B cells upon infection with EBV [1]. EBI2 is a G-protein (Gαi type) coupled receptor [2] but as long as 18 years after its discovery the nature of its ligand remained undisclosed. With the help of transfected cell lines
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Among the Ub interactions observed in
2021-04-27
Among the ~Ub interactions observed in the HOIP structure is one that involves a RING2 domain (from the non-cognate HOIP) [47]. A similar binding interaction was defined between HHARI RING2 and the hydrophobic patch on Ub by NMR [54]. HHARI RING2 mutations that ablate the interaction inhibit formati
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A role for the E E interface in
2021-04-27
A role for the E2–E3 interface in governing mono- versus polyubiquitination is not mutually exclusive with that of the E2 backside, which has previously been shown to mediate polyubiquitination through its ability to bind to Ub [21], [25], [33]. Brzovic and colleagues first demonstrated the importan
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Analysis of Table shows that compound b in which
2021-04-26
Analysis of Table 1 shows that compound 7b, in which the biphenyl scaffold does not bear any substituent, displays its inhibitory potency in the micromolar range (IC50 = 11 μM). If the amide bridge is moved from position 1 to 3 of the biphenyl system, product 7c is yielded, whose potency is about 4
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In this study we have developed and investigated three
2021-04-26
In this study we have developed and investigated three NADPH-regenerating fusion partners with two different enzyme systems: a BVMO and an ADH. With the exception of one fusion construct (StGDH with LbADH), all fusion Aprepitant resulted in good soluble expression as well as fully functional as self
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It is well established that Shp can
2021-04-26
It is well established that Shp-2 can function as a substrate for several RTK, such as PDGF or EGFR [23], [36]. To test whether DDR1 recognizes Shp-2 as its substrate, we overexpressed a catalytically inactive Shp-2 mutant together with DDR1b in 293 cells [31]. Immunoprecipitation of Shp-2 followed
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Keratin K has been identified as the first
2021-04-26
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 ol
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Previous studies from our laboratory have
2021-04-26
Previous studies from our laboratory have demonstrated that CysLT1R mRNA and protein expression can be upregulated by T2-type cytokines (IL-13, IL-4, and IL-5) in monocytes, macrophages, and eosinophilic HL-60 cells., To our knowledge, however, there are no studies on interactions of cytokines (suc
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Here we describe a novel series of arylazoderivatives develo
2021-04-26
Here, we describe a novel series of arylazoderivatives developed from CAN508, one of the first known selective CDK9 inhibitors. We focused on modification of both ends of parental molecule, CAN508, in order to improve cytotoxicity and CDK activity. We therefore analyzed how changes in molecules will
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Finally unilateral microinjection of CP
2021-04-26
Finally, unilateral microinjection of CP-376395, Astressin 2B, CP-376395 + CRF or ASTR 2B + CRF into the BLA (Fig. 3A) or CeA (Fig. 3B) did not significantly alter spontaneous motor activity in the open field test (F4,24 = 0.148, P > 0.05; F4,29 = 0.290, P > 0.05 in the BLA and CeA, respectively, AN
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br Acknowledgements This work was supported in part by JSPS
2021-04-26
Acknowledgements This work was supported in part by JSPS KAKENHI Grant Number 26292031. Introduction The Cys-loop receptors constitute an important superfamily of ligand-gated ion AG 013736 synthesis (LGICs) and mediate synaptic transmission in both invertebrate and vertebrate nervous system
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br Materials and methods br Results br Discussion DAS
2021-04-26
Materials and methods Results Discussion DAS and nilotinib, as the second potent, oral generation TKIs, bind to both the active and inactive conformation of the ABL1 kinase domain, have been found to be effective in treating patients with IM resistant or intolerant CML-CP, and inhibit all t
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