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br APC C Uses a Dynamic Cullin RING
2019-12-14

APC/C Uses a Dynamic Cullin–RING Mechanism to Elongate Polyubiquitin Chains Human APC/C generates Lys11-linked poly-Ub chains through an entirely different mechanism, via the distinctive E2 enzyme, UBE2S 30, 31, 32. Although APC2 and APC11 are necessary and sufficient to activate UBE2S, the mecha
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The UPP broadly involves proteolysis in
2019-12-14

The UPP broadly involves proteolysis in biochemical processes and is a potential target for cancer therapy. The UPP degrades unfolding or damaged proteins by an ATP-dependent mechanism (Ciechanover, Elias, Heller, Ferber, & Hershko, 1980). It also plays an important role in RGDS peptide regulation,
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Boc-MLF We also discovered important clues to domain binding
2019-12-14

We also discovered important clues to domain Boc-MLF of DGKs and how to exploit these regions for development of DGKα-selective inhibitors. The identification of a probe-modified site at the C1 domain provided the first evidence of a ligand binding site remote from the ATP binding region of DGKs. A
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Cultured cells or mouse lung tissues
2019-12-14

Cultured cells or mouse lung tissues were harvested and lysed in Radio-Immunoprecipitation Assay (RIPA) buffer (0.05 mol/l Tris–HCl pH 7.4, 0.15 mol/l NaCl, 0.25% deoxycholic acid, 1% NP-40, 1 mmol/l ethylenediamine tetraacetic WIN 18446 (EDTA), 1 mmol/l phenylmethylsulfonyl fuoride, 1 μg/ml aprot
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br E intracellular localization br Regulation of E
2019-12-13

E1 intracellular localization Regulation of E1 by other post-translational modifications Concluding remarks Acknowledgments We apologize to those whose work was not included because of space considerations or whose papers were unintentionally omitted. We thank Dr Peter Bullock (Tufts Uni
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m-3M3FBS Even though Et modification of DNA delayed the prog
2019-12-13

Even though Et743 modification of DNA delayed the progress of the translocating enzyme significantly, it did not trap RecBCD on DNA, nor did it alter the activity of the enzyme significantly. Under catalytic conditions, no loss of enzyme activity was observed (Table 2), nor were stable unwinding int
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Interestingly some drugs have been shown to be
2019-12-13

Interestingly, some drugs have been shown to be effective in the regulation of cytokine production (such as IL-2, IL-10, IL-27, IL-35, IL-37 and transforming growth factor-β, TGF-β) and, therefore, having a key role in the management of certain inflammatory-based clinical conditions (Banchereau et a
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N6-Methyl-ATP br ET Antagonist for the Future Macitentan and
2019-12-13

ET Antagonist for the Future: Macitentan and Atresentan Macitentan is an insurmountable antagonist, resulting from structure-activity studies to improve the efficacy and tolerability of bosentan, and gained approval in the United States in 2013 for the treatment of PAH. Actelion describes the com
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Quercetin competitively inhibited BFC activity in human reco
2019-12-13

Quercetin competitively inhibited BFC activity in human recombinant cDNA-expressed CYP3A4 with Ki=15.4±1.52μM, and myricetin noncompetitively with Ki=74.6±7.99μM (Fig. 4). The degree of inhibition by quercetin was not affected by a pre-incubation step and was similar in the microsomes from both gend
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Here we show that cpg is expressed only in the
2019-12-13

Here, we show that cpg2 is expressed only in the auda synthesis and encodes a protein that localizes specifically to the postsynaptic endocytic zone of excitatory synapses. We present evidence that CPG2 is a critical component of the postsynaptic endocytic pathway that mediates both constitutive an
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A French cohort study reported that micronized progesterone
2019-12-13

A French cohort study reported that micronized progesterone or didrogesterone used with oral or percutaneous estradiol showed no increase or decrease in the risk of breast cancer compared to synthetic progestins for at least 4 years of treatment [22] and even after 8 years [23]. Although the results
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Finally it is possible that also species
2019-12-13

Finally, it is possible that also species differences (rat primary preadipocytes vs mouse 3T3-L1 cells) could contribute to these discrepancies. A recent study suggested that 3T3-L1 SMIP004 may contain adipocyte precursors with multiple cell lineage characteristics which may contribute to different
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br Future directions The proposed membrane topology model
2019-12-12

Future directions The proposed membrane topology model of DGAT1 has only three TMDs, with the N-terminus oriented toward the cytosol and the C-terminus in the ER lumen. The catalytic activity is exclusively on the luminal side of the ER membrane. The second and third TM domains are only about 10
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br Four active site residues of KSTD
2019-12-12

Four active site residues of Δ1-KSTD1 are fully conserved in Δ1-KSTDs from different species (Supplementary Figure S2). These residues are Tyr-119, Tyr-487, and Gly-491 from the FAD-binding domain and Tyr-318 from the catalytic domain. The structure of the Δ1-KSTD1•ADD complex revealed that the hy
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Widely expressed mammalian adhesion receptors for
2019-12-12

Widely expressed mammalian adhesion receptors for fibrillar collagens include the α2β1- and α11β1-integrins and the discoidin domain receptors (DDRs), DDR1 and DDR2 (Leitinger, 2011). Integrins and DDRs bind distinct and separate motifs in native fibrillar collagen (Curat et al., 2001, Vogel et al.,
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