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In the course of our program which was aimed at
2020-11-03

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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P H is a nonheme iron II dioxygenase that uses
2020-11-03

P4H is a nonheme iron(II) dioxygenase that uses O2 and α-ketoglutarate as co-substrates (Fig. 1A). The three-dimensional structure of mammalian P4H is unknown. We reasoned that an electrophilic analog of α-ketoglutarate could serve as an irreversible inhibitor of the enzyme and, hence, a useful prob
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NPC L NPC Niemann Pick C like
2020-11-03

NPC1L1 (NPC1 [Niemann-Pick C-like-1]-like intracellular cholesterol transporter) is the rate-limiting transmembrane transporter for cholesterol L-α-Aminoadipic Acid from the intestinal lumen, and it mediates the absorption of both dietary and biliary cholesterol., , NPC1L1 is the target of the cho
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Introduction Angiotensin II Ang II and
2020-11-03

Introduction Angiotensin II (Ang II) and Endothelin 1 (ET-1) are potent vasoconstrictive peptides recognized as key players in many cardiovascular diseases [1]. Cardiac hypertrophy, ischemic arrhythmia, and stroke have been associated to an overstimulation of the angiotensin II type 1 (AT1) recepto
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Estrogen receptors ERs belong to the
2020-11-03

Estrogen receptors (ERs) belong to the third class of nuclear receptors (NR3) [23]. Two different forms of ER have been described, ERα and ERβ. They are coded by two distinct genes (ESR1 and ESR2, respectively) containing 8 transcribed exons that give rise to six conserved protein domains: domains A
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br Acknowledgements Professor Olli A J nne
2020-11-03

Acknowledgements Professor Olli A. Jänne is warmly thanked for support and for providing excellent research facilities. Professor Patrik Finne is acknowledged for his help with statistical analyses. Drs Ronald Evans, Vincent Giguère, Jorma Palvimo, Malcolm Parker, and Anastasia Kralli are acknowl
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The importance of AAE in enhancing the
2020-11-03

The importance of AAE3 in enhancing the survival of plants and yeast when confronted with certain environmental stresses has been documented in recent reports. In response to biotic stress such as oxalate-secreting micro-organisms, AAE3 was found to reduce the inhibitory growth effects of the secret
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br Protein protein interactions of
2020-11-03

Protein-protein interactions of LEI/L-DNase II and the control of cell death Evolutionary tips The serpin inhibitory mechanism is extremely well adapted to evolutionary changes because a single amino colorimetric assay substitution in the RSL can led to the inhibition of a totally different p
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br Ubiquitin Capture by the Mobile APC RING
2020-11-03

Ubiquitin Capture by the Mobile APC11 RING Domain Contributes to Processive Substrate Ubiquitylation Although the rules of Ub-mediated proteolysis are only beginning to emerge, the rate and order in which different APC/C substrates are degraded during the Sobetirome correlates with processivity
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br Acknowledgments br Introduction Ubiquitin
2020-11-03

Acknowledgments Introduction Ubiquitin ligases limit the stability and activity of substrates by targeting them for proteasomal-dependent degradation. Siah is a two-member family of ubiquitin ligases implicated in control of key cellular processes. Among those, Siah ligases control prolyl hydr
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DDR distribution in healthy fibrotic
2020-11-03

DDR1 distribution in healthy, fibrotic and inflamed tissues Whereas we can easily mine publicly available databases to infer DDR1 expression profile in different tissues (as reported in Fig. 1), fine comprehension of DDR1 biology has been hampered by the absence of a commercially available specific
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In addition we investigated if the
2020-11-03

In addition, we investigated if the previously reported papain inhibitor can inhibit rhodesain, and found that it was not active at inhibiting rhodesain. The vinyl sulfone analogue of () was then synthesized and tested, and it was also inactive towards rhodesain. We then determined the time depend
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br Introduction Benzanthrone BNZ is a
2020-11-03

Introduction Benzanthrone (BNZ) is a dye intermediate used in the synthesis of number of polycyclic vat and disperse dyes. It has been detected as an environmental pollutant in urban ambient air particulates, originating from furnace effluents, municipal refuge, wood and coal combustion and autom
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br Experimental procedures br Introduction
2020-11-02

Experimental procedures Introduction Perfluorooctane sulfonate (PFOS) is an anthropogenic compound with high thermal, chemical and biological stability, which makes it a perfect ingredient for many industrial applications (Kissa, 2001). Nevertheless, these characteristics also mean that PFOS i
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pka kinase We and others have previously found
2020-11-02

We and others have previously found that supplementation of old rats with ALCAR remediates the age-related decay in mitochondrial bioenergetics in liver (Hagen et al., 1998a, Hagen et al., 1998b), heart (Paradies et al., 1994, Paradies et al., 1999), muscle (Pesce et al., 2010) and pka kinase (Liu
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