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br Conclusion In this study
2021-07-21
Conclusion In this study, we investigated functional alterations of ECs following exposure to mechanical and/or physicochemical stimuli. Specifically, hypoxia induced phosphorylation with significant increases after 30 min and the maximum increase was after 180 min. Our data show that a combinati
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ARCA ER redox imbalance leads to the accumulation of misfold
2021-07-20
ER redox imbalance leads to the accumulation of misfolded proteins, which might trigger the unfolded protein response (UPR) [17]. In the initiation of UPR, GRP78 preferentially binds to unfolded proteins, shifting the binding equilibrium away from IRE-1, PERK, and ATF-6, the initiators of UPR [18].
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topoisomerase ii HOIP s ability to build linear
2021-07-20
HOIP's ability to build linear Ub chains arises from a unique domain that follows directly after the RING2 domain, the linear ubiquitin chain-determining domain (LDD) (Fig. 1). Structures have revealed that the LDD is structurally integrated into RING2, creating a single RING2–LDD unit (Fig. 2D) [40
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Based on the SUMO SIM interaction involved in SUMOD position
2021-07-20
Based on the SUMO–SIM interaction involved in SUMOD positioning, a SUMO2ΔSBD (SIM-binding domain; Q30A, F31A, I33A) mutant can be investigated that disrupts this important binding interface (Eisenhardt et al., 2015; Meulmeester, Kunze, Hsiao, Urlaub, & Melchior, 2008). In Fig. 4A, multiturnover assa
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Recent results from our group found that
2021-07-20
Recent results from our group found that SPMs, not only play a part in terminating inflammation, but also have a physiological role in conjunctival goblet KU-0060648 to maintain ocular surface health in the absence of disease. Amongst the SPMs that are effective in the conjunctiva are resolvin D1 (
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Carbazole could be recrystallised from ethyl acetate to prov
2021-07-20
Carbazole could be recrystallised from ethyl acetate to provide bright red crystals suitable for single crystal X-ray diffraction (see ). The first crop showed had crystallised preferentially as the ()-isomer (A). Examining the single crystal X-ray data of it was interesting to find that the N2C1
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br Introduction Lung cancer is the leading
2021-07-20
Introduction Lung cancer is the leading cause of cancer-related death worldwide, accounting for more than 1.5 million deaths in 2012. Non–small-cell lung cancers represent approximately 85% of lung neoplasms; among these, squamous cell carcinomas (SCC) account for approximately 30% of cases. The
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Our recent discovery M P H R A
2021-07-20
Our recent discovery (M.P., H.R., A.S.) of a highly selective and in vivo active DDR1 small-molecule inhibitor provides evidence that DDR1 is a druggable pharmaceutical target, and some details of our efforts are provided below. To avoid the repurposing of known kinase inhibitor structural motifs, w
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VU 0155069 br Fragment based drug discovery
2021-07-20
Fragment-based drug discovery (FBDD) is a powerful method to discover drug leads and has been widely adopted in both academia and industry. FBDD can be used to explore chemical VU 0155069 space with libraries which are smaller in size, producing drug leads with high ligand-binding efficiency. It a
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For human health risk assessment of chemicals
2021-07-20
For human health risk assessment of chemicals, a default uncertainty factor (UF) of 3.16 is used to capture inter individual variation in toxicokinetics (Dorne and Renwick, 2005). However, the scientific background for this default UF remains unsatisfactory., Several studies have reported that a fac
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The phenolic hydroxyl group of ezetimibe
2021-07-20
The phenolic hydroxyl group of ezetimibe tolerated various structural modifications (disaccharide, carboxyalkyl and glucuronide) that retained inhibitory activity.13, 14, 15 We conjugated glycylglycine to phenolic hydroxyl group and synthesized ten 1H-pyrrole-2,5-dione derivatives 14a-j successfully
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We first confirmed LPS induction of
2021-07-19
We first confirmed LPS-induction of markers known to induce NF-κB signaling in Caco2BB cells, as established for numerous other cell types [31]. We initially selected this approach to monitor NF-κB activation instead of directly monitoring p65 as it is technically straightforward and provides both u
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br Introduction The ubiquitination status
2021-07-19
Introduction The ubiquitination status of a target protein is achieved via a delicate balance between two opposing forces: ubiquitin E3 ligases and DUBs. It has been postulated that the majority of proteins in a cell are regulated and modified by ubiquitin at some point (Hershko and Ciechanover,
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Preparation of the regioisomeric pyridooxazepinones and
2021-07-19
Preparation of the regioisomeric pyridooxazepinones 10 and 11 was accomplished utilizing the synthetic sequence depicted in Scheme 3. Amide coupling of 63 and pkm2 chloride 64 afforded amide 65. Removal of the alcohol protecting group, followed by base catalyzed cyclization afforded a 1:2.4 mixture
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The purposes of this study are to investigate the molecular
2021-07-19
The purposes of this study are to investigate the molecular function of DDR2, especially in cellular proliferation in prechondrocytes, and to examine the relationship between the proliferation and differentiation of prechondrocytes through both in vitro and in vivo analysis. Materials and methods
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