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This structure guided the variation
2019-09-02

This structure guided the variation of the compounds aiming either at enhanced interaction with CK1 or to exclude interaction with CK1 (R=Me, 15). We chose the 5-cloro substituted oxoindole as backbone as it is supposed to show enhanced metabolic stability, which is commonly used in medicinal chemis
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Many studies have shown that curcumin delays the
2019-09-02

Many studies have shown that curcumin delays the progression of atherosclerosis in different atherosclerotic animal models [18], [19], [20], [37] and the risk of atherosclerosis in human studies [15], [38], [39]. Curcumin also has many properties that contribute to combat atherosclerosis, such as an
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In humans several different small ubiquitin related
2019-09-02

In humans, several different small ubiquitin-related modifier (SUMO) paralogs can be conjugated to cellular proteins. The human genome codes for five SUMO paralogs (SUMO1–5); of these, SUMO1 and the almost identical SUMO2 and SUMO3 are ubiquitously expressed. Sumoylation is executed by an enzymatic
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br Criteria for ER targeted
2019-09-02

Criteria for ER-targeted fluorescent probes Survey of fluorescent probes Proposed approach to high affinity fluorescent steroidal ER probes Our proposed approach to the development of a new generation of fluorescent estrogen receptor imaging agents employs many of the elements present in th
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The potent estrogen EE induced a decrease
2019-09-02

The potent 5z EE2 induced a decrease in CYP2C11 activity (reduction in 2α-OH and 16α-OH testosterone) and protein at the 200 ppb dose and in this respect was similar to nonylphenol and genistein. This result agrees qualitatively with the results of Hallstrom et al. (1996) who exposed male rats to h
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5-Iodotubercidin and Importantly in genetic studies Saccharo
2019-09-02

Importantly, in genetic studies, Saccharomyces cerevisiae Pif1, a member of the SF1 family of helicases, has been implicated in BIR in conjunction with Pol δ (Chung et al., 2010, Saini et al., 2013, Wilson et al., 2013). Using highly purified S. cerevisiae proteins, a system that permits dissection
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br Acknowledgement br Introduction Human dihydroorotate
2019-09-02

Acknowledgement Introduction Human dihydroorotate dehydrogenase (hDHODH), a flavin-dependent mitochondrial enzyme involved in de novo nigericin clinical biosynthesis, is a validated therapeutic target for the treatment of autoimmune diseases such as rheumatoid arthritis and cancer [1], [2], [3
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br Acknowledgments br Introduction Heterocyclic chemistry
2019-09-02

Acknowledgments Introduction Heterocyclic chemistry has become one of the most important fields of research in pharmaceutical industry due to their many fold applications. Amongst all, heterocyclic lipid metabolism pathway containing nitrogen and oxygen have shown most potent biological activ
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cetp inhibitor Some studies have been conducted on the activ
2019-09-02

Some studies have been conducted on the activities of CYP450 [[28], [29], [30], [31]]. For example, Chen et al. reported that low-dose aspirin induced the in vivo activity of CYP2C19 in healthy subjects [30], Krasniqi et al. reported that CYP2C8*3 and CYP2C9*2*3 variants correlated with ibuprofen-in
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Testosterone is inactivated through hydroxylation and conjug
2019-09-02

Testosterone is inactivated through hydroxylation and conjugation pathways [3], [4]. 6β-Hydroxylation is the main pathway among testosterone hydroxylation processes in the liver microsome. Testosterone 6β-hydroxylation is mainly catalyzed by cytochrome P450 3A (CYP3A) [5], [6], which is expressed in
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Ethyl naphthoates a h were successfully
2019-09-02

Ethyl 1-naphthoates (10a–h) were successfully reduced to 1-naphthylmethanols (12a–h) by using LiAlH4 with 8–87% yields. Then PCC was used to convert the alcohols into the corresponding 4-alkyl-1-naphthaldehyde derivatives (13a–h) with relatively higher yields (58–90%) as represented in Scheme 2. The
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DDX belongs to the DEAD box
2019-09-02

DDX3 belongs to the DEAD-box family of proteins, ATP-dependent RNA helicases characterized by the presence of a highly conserved helicase core domain [13]. This catalytic core is composed of two RecA-like domains containing motifs involved in ATP binding/hydrolysis, RNA binding and helicase activity
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br Introduction Proteins therapeutic can be defined as prote
2019-09-02

Introduction Proteins therapeutic can be defined as proteins that are either naturally produced in the body or created in the laboratory and introduced into the patient with the aim of improving or curing a pathological condition. They are usually acquired from either microbial Apicidin and or b
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Two major mechanisms including apoptosis and oxidative
2019-09-02

Two major mechanisms including apoptosis and oxidative stress have been suggested for MTX-induced cytotoxicity (Hafez et al., 2015; Neuman et al., 1999; El-Sheikh et al., 2015). It has been reported that MTX promotes cell death via apoptosis in both cancerous and non-transformed cells (Mazur et al.,
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There was a measurable worsening but not a
2019-09-02

There was a measurable worsening, but not a statistically significant change in the baseline and follow-up best ear hearing scores, where the mean worsening change was 11.9 dB (95% CI: −1.11–24.86, p-value = 0.070). However, of the 16 patients, 14 (87.5%) were found to have clinically significant wo
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