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In conclusion the data suggest
2020-06-30
In conclusion, the data suggest that doses of COX-2 inhibitors and EP1 receptor antagonists which have previously been reported to exert disease modulating or antiepileptic drug potentiating effects do not negatively affect seizure control in temporal lobe epilepsy. The contrasting impact of the EP1
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br O GlcNAcase Human OGA
2020-06-30
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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It has been reported that
2020-06-30
It has been reported that the ECD of DDRs require dimerization and/or oligomerization for binding to collagen.,, Here, we have established using SPR that antibody-mediated oligomerization of DDR2-Fc significantly enhances its binding to immobilized collagen type 1. Our results are consistent with ea
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The cytoplasmic domain of classical cadherins is highly cons
2020-06-30
The cytoplasmic domain of classical cadherins is highly conserved and can interact with different cytosolic proteins. Typically this domain is associated with catenin family members, including p120 catenin, β-catenin, and α-catenin, which form a cadherin-catenin complex (Fig. 1). The catenin family
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br Rationale and hypothesis To discover an allosteric inhibi
2020-06-30
Rationale and hypothesis To discover an allosteric inhibitor of EGFR, Jia et al. (2016) screened a library of 2.5 million compounds at 1 μM ATP concentration in opposition the purified EGFR L858R/T790M mutant enzyme. 1322 best hits were found from this round of screening. The pinnacle hits had be
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The question arises as to how
2020-06-30
The question arises as to how the massive conformational changes determining whether APC/CCDC20–MCC is inhibited or able to catalyze MCC ubiquitylation are naturally controlled? This transition likely involves APC/C regions near the subunit APC15, because reducing cellular APC15 levels stabilizes MC
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UBA belongs to the non canonical E enzymes that
2020-06-30
UBA5 belongs to the non-canonical E1 enzymes that lack a defined Cys domain but have the active-site Cys within the adenylation domain [24]. Similar to other E1 enzymes, UBA5\'s adenylation domain comprises an eight-stranded beta sheet that is surrounded by helices [21]. Moreover, like the ancestral
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In contrast to the methylation that is catalyzed exclusively
2020-06-30
In contrast to the methylation that is catalyzed exclusively by DNMTs, there have been suggested several pathways that could induce demethylation (Watt & Molloy, 1988). However, the existence and influencing of enzymes that promote active demethylation remains elusive. Studies aiming to gain more in
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Kisspeptin 234 Our previous studies have demonstrated that t
2020-06-30
Our previous studies have demonstrated that the DDR2 discoidin domain fully contains the binding site(s) for the fibrillar collagens I and II (Leitinger, 2003, Leitinger et al., 2004). The binding site for collagen I was mapped to three spatially adjacent surface loops within the DDR2 discoidin doma
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Similarly LTD concentration dependently enhanced AQP express
2020-06-30
Similarly, LTD4 concentration-dependently enhanced AQP4 expression in astrocytes (Fig. 3). The LTD4-enhanced AQP4 expression was not affected by pranlukast but inhibited by Bay u9773, a non-selective CysLT1/CysLT2 receptor antagonist [33]. Because no selective CysLT2 receptor antagonists are current
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Verteporfin br Introduction Accounting educators and profess
2020-06-30
Introduction Accounting educators and professional accounting organizations have speculated that advanced placement (AP) may be an effective tool for recruiting high-quality students into accounting education programs (Deines, Bittner, & Eichman, 2012; The Pathways Commission, 2012), and it is no
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DNA hypomethylation has been found in
2020-06-29
DNA hypomethylation has been found in liver tumor and other tumors of humans, such as laryngeal cancer, KPT-9274 mg tumors, tongue squamous cell carcinoma and uterine leiomyomas [[20], [21], [22], [23], [24]]. Then, we mainly sought to confirm whether TCA could induce DNA hypomethylation in vitro an
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BI-7273 br Introduction br Sphingolipid metabolism Sphingoli
2020-06-29
Introduction Sphingolipid metabolism Sphingolipids, are fundamental constituents of all eukaryotic membranes and their metabolism is carried out by a broad array of anabolic and BI-7273 with ceramide as their hub (for a review, (Hannun and Obeid, 2018)). Ceramide can be formed by multiple pat
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In the course of our
2020-06-29
In the course of our program, which was aimed at developing CRTH2 antagonists for the treatment of allergic diseases, we have been pursuing a new class of potent and selective CRTH2 antagonist lead based on the structures of CRTH2 antagonists known to date (, , ). Using a fused 6–6-membered ring sys
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The synthesis of tricyclic analogs is described in
2020-06-29
The synthesis of tricyclic analogs 28–33 is described in Scheme 3. Oxidative C–C bond cleavage of the terminal olefin of 39i afforded a tricyclic product 52 without isolation of an aldehyde expected as an intermediate. Aminolysis of the chloride 52 with optionally substituted anilines afforded 28–30
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