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Epigenetic silencing of genes that
2020-08-20
Epigenetic silencing of genes that determine tumor invasiveness, growth patterns of tumors, and tumor-cell apoptosis12, 29 may also affect the expression of drug-metabolizing enzymes, thereby providing an additional genetic mechanism in pharmacogenomics. Trisomy 8 that contains wild-type GGH could b
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br The modulation of ER
2020-08-20
The modulation of ERα: from SERMs to TSECs Continued efforts to provide women with efficacious menopausal therapies have generated interest in the development of selective DPP4 Activity Fluorometric Assay Kit receptor receptor modulators (SERMs). Similar to estrogens, SERMs have been shown to bin
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ATP binding cassette transporters such as ABCA and
2020-08-20
ATP-binding cassette transporters such as ABCA1 and ABCG1 are expressed on cell membranes to transport cholesterol from biotin 100 mg to HDL. These transporters help to improve RCT and reduce atherosclerosis. ABCA1 and ABCG1 gene expression are primarily induced by the stimulation of liver X recept
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Given the important regulatory roles Ub signaling pathways p
2020-08-20
Given the important regulatory roles Ub signaling pathways play in eukaryotes, bacterial pathogens and viruses have evolved elaborate mechanisms to hijack host Ub signaling pathways and evade the immune response. This is highlighted by the numerous E3 Ub ligases and spectrum of DUBs encoded by bacte
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DNMT is the dominating enzyme responsible for maintenance of
2020-08-19
DNMT1is the dominating enzyme responsible for maintenance of the DNA methylation pattern and the primary enzyme responsible for copying methylation patterns following DNA replication (Moore et al., 2013). DNMT1 maintains the mitotic inheritance of the original methylation pattern in a cell lineage d
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Indeed the alkyl group is not seen in the
2020-08-19
Indeed, the -alkyl group is not seen in the original crystallographic electron density omit map prior to positioning either inhibitor in DHODH, nor can it be found in the final maps. Rather, the electron density maps are consistent with hydrolysis of the amide to the acid. Once the scaffold was clea
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MTX and MTXPGs block the
2020-08-19
MTX and MTXPGs block the activity of the key enzyme DHFR (Fig. 1), which converts folates to their active forms – dihydrofolate (DHF) and tetrahydrofolate (THF). MTXPGs also potently inhibit thymidylate synthase (TS). Furthermore, during dTMP synthesis, TS utilizes the cofactor 5,10-methylene THF, w
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Kuo et al Have shown that DAPK function in
2020-08-19
Kuo et al. (2006) Have shown that DAPK1 function in inhibiting microtubule (MT) assembly is through the activation of microtubule affinity-regulating kinases (MARK)/PAR-1 family kinases MARK1/2, which destabilize MT by phosphorylating tau and related MAP2/4. This relation with DAPK1 has demonstrated
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Compounds and administered orally to fasted
2020-08-19
Compounds , , and administered orally to fasted Harlan Sprague-Dawley rats 1h prior to trigeminal stimulation, decreased extravasation in this model in a dose-related manner, with an estimated ID of 1, 10 and 100μg/kg, respectively (determined 15min after stimulation, ). For comparison, the clinica
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Stable carbon and nitrogen isotope
2020-08-19
Stable carbon and nitrogen isotope ratios in bone collagen and carbon isotope ratios in bone apatite data were obtained by the means of the techniques described in supplementary data (SD1). For collagen, standard indicators have been used to assess its preservation, such as collagen yield, carbon an
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Introduction Safety critical systems are defined as those sy
2020-08-19
Introduction Safety-critical systems are defined as those systems where failure could result in the loss of life or injury to people, damage to equipment or to the environment [9]. Safety standards, e.g., [41], [17], [18], [6], [38], expect appropriate safety analysis tasks to be integrated within
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br Materials and methods br Results br Discussion The
2020-08-19
Materials and methods Results Discussion The oestrogen agonist properties and androgen antagonist activities of parabens have been well documented by a variety of in vitro and in vivo assay systems over the past decade (Chen et al., 2007, Darbre and Harvey, 2008, Golden et al., 2005). To th
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Cantharidin is a natural element extracted
2020-08-19
Cantharidin is a natural element extracted from blister beetles, and has been proven to be effective in cancer [16]. NCTD, the demethylated analog of cantharidin, has been synthesized and been shown to have an equal anti-cancer effect with fewer side effects than cantharidin [39]. It was confirmed t
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Accumulating evidence suggests that certain abnormal emotion
2020-08-19
Accumulating evidence suggests that certain abnormal emotional traits, such as impulsive aggression and cluster B personality, are associated with suicidal behaviors (Currier and Mann, 2008, Mann et al., 2009, Rujescu et al., 2007, Turecki, 2005). Impulsive aggression appeared to be associated with
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br Results br Discussion In this
2020-08-19
Results Discussion In this paper we present insights into the observed specificities of inhibitors targeting the ubiquitin-activating and related E1 Fmoc-Gln(Trt)-OPfp via crystal structures of the specific NEDD8-E1 inhibitor MLN4924, the dual NEDD8/Ub E1 inhibitor ABPA3, and the selective Ub
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