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QSAR based on the D
2020-03-24
QSAR based on the 3D structures of ligands plays an important role in the ligand-based drug discovery and design [12]. Comparative molecular field analysis, CoMFA [11], and comparative molecular similarity index analysis, CoMSIA [12] are among the most popular QSAR models. They focus on changes in 3
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br Introduction As a serine proteinase
2020-03-24
Introduction As a serine proteinase and a sub-family of the chymotrypsin-like proteinase, Glutamyl endopeptidase (GE), which is mainly found in Bacillus species, specifically cleaves negatively charged amino Spironolactone mg residues (Glu/Asp) (Yokoi et al., 2001). Madsen et al. (Madsen & Qvist
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The roles of ginsenoside in E and S
2020-03-24
The roles of ginsenoside in E1 and 26S proteasome inhibition are shown in Table 2. The nitro substitute on the furan ring may be important for PYR-41 inhibition of the E1 enzyme (Yang et al., 2007). The macrocycle core and aliphatic tail of Largazole are responsible for inhibiting E1 activity (Unger
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There have been attempts to stimulate the dopaminergic syste
2020-03-24
There have been attempts to stimulate the dopaminergic system to influence cognition in women around menopause who have subjective complaints about their cognition by Epperson et al. (Epperson et al., 2011, Epperson et al., 2015). In perimenopausal and postmenopausal women, Epperson et al. found tha
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In S cerevisiae Mek a paralog of the checkpoint
2020-03-24
In S. cerevisiae, Mek1, a paralog of the checkpoint kinase Chk2, mediates cell-cycle arrest in response to meiotic defects (Bailis and Roeder, 2000, Xu et al., 1997). Mek1 is associated with meiotic chromosome axes, where its activation requires interactions with two other axis proteins, Hop1 and Re
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In this study we reported that over expressed endogenous cen
2020-03-24
In this study, we reported that over-expressed endogenous central ET-1 exerted anti-allodynic and anti-hyperalgesic effects on SNL-induced NP for the first time. Furthermore, we showed that ETA-R mRNA Urolithin A together with the level of ET-1 was increased in the CNS up to 21days after SNL surger
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Previous synthetic lethal screening efforts Cox et al
2020-03-23
Previous synthetic lethal screening efforts (Cox et al., 2014) have mainly used RNAi as a means of identifying potential targets (Barbie et al., 2009, Kim et al., 2016, Luo et al., 2009, Scholl et al., 2009), although a few screens (Shaw et al., 2011, Steckel et al., 2012) have been performed with s
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Proteolysis by CPs is crucially important for
2020-03-23
Proteolysis by CPs is crucially important for cereal seed development and germination. However, these enzymes must be tightly controlled. Pre-harvest sprouting is a phenomenon in which the control of CPs is disrupted. This disruption manifests in the premature synthesis and activation of CPs, leadin
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In this review we first introduce the in vivo metabolism
2020-03-23
In this review, we first introduce the in vivo metabolism profile of VD3, and the mediation of Cyp3a gene transcription by PXR and CAR in humans, mice and rats. We then focus on the species-specific VDR-dependent regulation of human (CYP3A4, CYP3A5 and CYP3A7), mouse (mainly CYP3A11 and CYP3A13), an
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FSLLRY-NH2 We did not observe inhibition of vCPH by any
2020-03-23
We did not observe inhibition of vCPH by any of the TCA cycle intermediates (apart from the metal chelators citrate and isocitrate), nor by the factor inhibiting HIF (FIH; a 2OG-dependent asparaginyl hydroxylase) inhibitor N-oxalyl d-phenylalanine (NOF) or the γ-butyrobetaine dioxygenase inhibitor m
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Materials and methods br Results br Discussion Hydroxylation
2020-03-23
Materials and methods Results Discussion Hydroxylation of proline in bacterial dna synthesis is one of the oxygen-requiring metabolic reactions, which needs efficient oxygen. Oxygen supply is always a rate-limiting step for tyrosinase production even though pure oxygen is purged in a bioreac
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Egr together with catecholamine biosynthetic enzymes such as
2020-03-23
Egr1, together with catecholamine biosynthetic enzymes, such as tyrosine hydroxylase (TH), dopamine β-hydroxylase (DBH), and phenylethanolamine N-methyltransferase (PNMT), is induced in adrenal medulla by different types of stress (Liu et al., 2005, Morita et al., 1996, Nankova et al., 1993, Papanik
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The Lysine mutant is located in the tail region of
2020-03-23
The Lysine429 mutant is located in the tail region of 5-HT2A, which is predicted to be unstructured. This region has been shown to interact, in vitro, with PSD95 and leads to differences in signaling (Xia et al., 2003). The ASK motif, a component of the tail region, is also important for regulation
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Furthermore the determination of downstream
2020-03-23
Furthermore, the determination of downstream target genes induced by CdCl2 is noteworthy and can help to define its underlying carcinogenesis mechanism. Therefore, we evaluated c-fos and c-jun expression which are stimulated by estrogen through ERK/MAPK pathway. These are not only proto-oncogenes wh
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3230 The upregulation of PTGS and
2020-03-23
The upregulation of PTGS1 and PTGS2 in late gestation in mares could be linked to the high levels of estrogens produced by the fetoplacental unit. Estrogens are thought to be effective stimulators of prostaglandin production by potentially up regulating PTGS2 expression. Although a recent publicatio
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