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In addition to PGC transcriptional co
2021-02-26

In addition to PGC1α, transcriptional co-repressors such as NCOR and RIP140 participate in oxidative muscle remodeling induced by exercise, whereby reductions in their expression and the resulting de-repression of downstream TFs activates oxidative gene expression (Seth et al., 2007, Yamamoto et al.
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A set of small molecule LigI
2021-02-25

A set of small molecule LigI inhibitors were identified through an in silico structure-based screen, using the atomic resolution structure of LigI complexed with nicked DNA [[18], [26]]. This screen yielded inhibitors that were selective for LigI (L82), inhibited both LigI and LigIII (L67) and inhib
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This pathway appears to have importance in
2021-02-25

This pathway appears to have importance in epilepsy. DGKε(−/−) mice had significantly fewer motor seizure and epileptic events compared with DGKε(+/+) mice [18]. This could be explained by the fact that in the knockout mice a greater fraction of the SAG would be converted to 2-AG. 2-AG itself is kno
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Previous studies from our lab looked
2021-02-25

Previous studies from our lab looked at the effect of interfering with crossover helix interactions in TS-DHFR. One study utilized peptide mimetics of the crossover helix to inhibit wild-type TS-DHFR noncompetitively, and with an IC of 230 μM. A second study used a virtual screening approach to iden
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chk1 inhibitor br Phylogenetic analysis KSTDs have rather
2021-02-25

Phylogenetic analysis — Δ1-KSTDs have rather diverse amino chk1 inhibitor sequences. A sequence distance analysis using the program MEGA6 [75] of all currently biochemically characterized Δ1-KSTDs yielded a largest p-distance [76] of 0.67 (on a scale of 0-1) for the Δ1-KSTDs from the actinobacter
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HEK cells stably transfected with CysLT were
2021-02-25

HEK-293 TNKS 49 receptor stably transfected with CysLT1 were stimulated with LTD and internalization was studied by confocal microscopy, FACS or cell-surface ELISA. Cells were co-transfected with wildtype and dominant negative (DN) mutants of arrestin and dynamin. Clathrin-mediated endocytosis was i
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Among the CYP enzymes CYP D has
2021-02-25

Among the CYP450 enzymes, CYP2D has been considered a crucial protein that involves in the metabolism of xenobiotics and drugs (Zanger and Schwab, 2013). Some isoforms of the CYP2D subfamily have been well characterized, such as CYP2D6 due to its clinical importance and CYP2D14 in black cattle (Hama
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Ung et al examined a
2021-02-25

Ung et al. examined a variety of structural features based upon the location of the DFG-motif and the αC-helix to define the conformational space of the catalytic domain of protein kinases [75]. They reported that the DFG motif can move from its active DFG-Din location to the inactive DFG-Dout locat
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Grapiprant is a selective antagonist for prostaglandin
2021-02-25

Grapiprant () is a selective antagonist for prostaglandin E (PGE) receptor subtype 4 (EP4) identified as a clinical candidate for the treatment of inflammatory pain associated with osteoarthritis (OA). It is currently under development for use in humans and dogs. The projected dosing regimen of grap
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Recoverin is a kDa retinal
2021-02-25

Recoverin is a 23-kDa retinal protein that binds to calcium. It regulates the Cytochalasin J of rhodopsin during visual transduction within photoreceptor cells. Since the pathogenicity of anti-recoverin antibody is potent, anti-recoverin CAR patients often have progressive visual impairments, chara
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br Materials and methods br Results br Discussion Approximat
2021-02-25

Materials and methods Results Discussion Approximately 90% of pulmonary emphysema causes are related to smoking and its progression in patients and are characterized by severity levels [5]. Experimental models using CS to induce emphysema are widely used because they resemble the emphysema
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br Results br Discussion The origin
2021-02-25

Results Discussion The origin and fate of Tfh cells has been intensely studied since their first description 14 years ago (Breitfeld et al., 2000, Schaerli et al., 2000). Although mice engineered to report BCL6 (Kitano et al., 2011, Liu et al., 2012) and interleukin-21 (IL-21) (Lüthje et al.,
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One of the most fundamental distinctions
2021-02-25

One of the most fundamental distinctions between Ub signals is substrate monoubiquitination versus polyubiquitination. With the exception of the E2, UBE2W, which represents a special case because it Epigenetics Compound Library only ubiquitinates the flexible N-termini of substrates [5], [6], [20],
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COH inhibited global SUMOylation in cells and blocked the
2021-02-25

COH000 inhibited global SUMOylation in Parthenolide and blocked the E1 catalyzed attachment of SUMO to the corresponding conjugating enzyme Ubc9, but not the attachment of ubiquitin or NEDD8 to their respective E2s, confirming inhibition and specificity in cellulo. Consistent with previous studies
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The activity of chromenones bearing heteroaryl groups
2021-02-25

The activity of chromenones bearing heteroaryl groups at the 8-position is summarised in . Replacement of the 8-phenyl substituent of by a thiophen-2-yl group ( and ) did not improve DNA-PK inhibitory activity, although the 4-phenylthiophen-2-yl derivative (), together with the bithiophene analogue
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