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br Acknowledgments This work was supported by Grants from
2020-03-27

Acknowledgments This work was supported by Grants from the National Research Foundation (2010-0000782) and the National Center for GM Crops (PJ008152) of the Next Generation BioGreen 21 Program funded by the Rural Development Administration, Republic of Korea, to W.T.K. Introduction Ubiquityl
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br Materials and methods br Results br Discussion PYR inhibi
2020-03-27

Materials and methods Results Discussion PYR-41 inhibits UBE1 activity that catalyses an initial step in the ubiquitination reaction. In the present study, we examined the role of this enzyme in sperm-egg fusion by inhibiting UBE1 enzymatic activity in eggs. Our results suggest that PYR-41
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The authors identified inhibitors of SUMOylation using two
2020-03-27

The authors identified inhibitors of SUMOylation using two assays to monitor the conjugation of SUMO1 to RanGAP1 by E1 and E2 enzymes: a fluorescence resonance energy transfer (FRET) primary screen that evaluated over 250,000 compounds and a chemiluminescence secondary screen. A counter screen was u
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N acetylation by N acetyltransferase NAT is an important met
2020-03-27

N-acetylation by N-acetyltransferase (NAT) is an important metabolic pathway for some substances, and there are 2 functional NAT isoforms in humans—NAT1 and NAT2. Studies of etamicastat in healthy subjects showed an extensive N-acetylation of etamicastat to the inactive metabolite BIA 5-961, and a l
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PF-06447475 The field of synthetic cytokine biology continue
2020-03-27

The field of synthetic cytokine biology continues to grow through molecular, physiological and pathophysiological insights, as well as via new methodical advances. The approval of chimeric antigen receptor (CAR) T cell immunotherapy by the US Food and Drug administration (FDA) in August 2017 for rel
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Functional studies suggested the presence of
2020-03-27

Functional studies suggested the presence of a cysLT1 receptor. We observed an LTD4-induced cytosolic calcium response, albeit one that was very weak by most standards. The magnitude of the average response was partially explained by the low percentage of Bax inhibitor peptide P5 showing a very tra
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SCH 727965 Introduction Quassinoids are natural products for
2020-03-27

Introduction Quassinoids are natural products formed through the oxidative degradation of triterpene derivatives with anti-inflammatory, antimicrobial, antineoplastic, and antiplasmodial effects (Chakraborty and Pal, 2013; Houël et al., 2013). They are characteristic ingredients of the family Simar
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AMPK is a master regulator of metabolic homeostasis its broa
2020-03-27

AMPK is a master regulator of metabolic homeostasis, its broad spectrum of metabolic activities makes it an attractive target for treatment of metabolic and related disorders including Diabetes and Obesity (Madhavi et al., 2018). It controls lipid metabolism through its target genes PPAR-γ, C/EBP-α
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Stable isotope studies applied to skeletal remains of early
2020-03-27

Stable isotope studies, applied to skeletal remains of early Pacific populations, have shown a trend toward a horticultural diet with temporal variation in response to local environmental conditions (Field et al., 2009; Kinaston and Buckley, 2013; Valentin et al., 2010, Valentin et al., 2014; Kinast
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The repair pathway of DNA DSBs through HR
2020-03-26

The repair pathway of DNA-DSBs through HR and the role of BRCA1 in repair kinetics by HR is also an important factor to unravel the radiation sensitization of novel small molecule inhibitors. The involvement of the breast cancer susceptibility gene 1 (BRCA1) in tumorigenesis and its role in facilita
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Of the acidic hydroxyazoles involved hydroxypyrazole had the
2020-03-26

Of the acidic hydroxyazoles involved, hydroxypyrazole had the weakest acidic profile (pKa in the range of 6–7), although highly deprotonated at physiological pH. During hit optimization, the two pyrazole ring positions available for substitution provide an opportunity for a better exploration of the
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For LAU extracted ion chromatograms of the
2020-03-26

For LAU 399, extracted Lapatinib chromatograms of the blank, t0, and t120 samples for the diagnostic product ion m/z 163.0216 are provided in Fig. S11, and extracted ion chromatograms of the t120 sample for m/z 163.0216 (diagnostic product ion), and m/z 308.1677 and 306.1522 (metabolites) are shown
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A growing number of other post
2020-03-25

A growing number of other post-translational modifications are implicated in regulation of the ubiquitin system, including substrate modification by hydroxylation, glycosylation, acetylation, methylation, modification by poly(ADP-ribose) (PAR), and attachment of ubiquitin-like modifiers. The HIF1-α
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salbutamol sulfate Extracellular uridine can be transported
2020-03-25

Extracellular uridine can be transported across the cell membrane to enter the nucleotide salvage pathway. A colon cancer cell line supplemented with uridine was capable of growing normally in the presence of 1 μM brequinar (Peters et al., 1992). The supplemented uridine may be transported into the
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br Acknowledgments br Casein kinases
2020-03-25

Acknowledgments Casein kinases (CK) are serine/threonine-specific enzymes and can be divided two subtypes: casein kinase 1 (CK1) and casein kinase 2 (CK2). CK1 contains at least seven isoforms (α, β, γ1, γ2, γ3, δ and ε) expressed in eukaryotic organisms, CK1 is involved in various cellular pro
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