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Besides chemopreventive effects against oxidative DNA damage
2020-04-01
Besides chemopreventive effects against oxidative DNA damage we evaluated the protective effects of the three Hypericum sp. and isolated compounds against alkylating DNA damage induced by MMS in HT29 cells. Human exposure to alkylating agents, from different sources, occurs in a continuous way and i
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A novel series of DHODH inhibitors was
2020-04-01
A novel series of DHODH inhibitors was developed by us based on a lead that was discovered during a docking procedure and medicinal chemistry exploration. The activity of the initial lead was improved by a QSAR method and yielded low nanomolar inhibitors. Introduction The most common metabolic h
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br Introduction Acylglycerol acyltransferases AGATs are pred
2020-04-01
Introduction Acylglycerol acyltransferases (AGATs) are predominantly responsible for triglyceride synthesis in the body, via two major pathways: the glycerol phosphate (GP) pathway (Kennedy, 1957) and the monoacylglycerol (MG) pathway (see Coleman and Lee, 2004, Yen et al., 2008). The final step
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eletriptan br Acknowledgments This research was supported by
2020-04-01
Acknowledgments This research was supported by grants from the Ministerio de Ciencia e Innovación (Grants SAF/FEDER 2010-17907; 2013-49076-P), Spain, Red de trastornos adictivos (RETICS RD12/0028//0003, Instituto de Salud Carlos III, Spain) and Fundación Séneca (15405/PI/10, Región de Murcia, Spa
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BMS-509744 australia Previous studies have shown the
2020-04-01
Previous studies have shown the harmful effects of NEFA on ovarian functionality, such as inhibition of bovine granulosa cell survival and proliferation, steroidogenesis, and follicular development and alteration in oocyte development [36,45,46]. Therefore, the higher levels of NEFA found in the fo
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Although several genomic technologies including the generati
2020-04-01
Although several genomic technologies, including the generation of ERRγ-specific knockout mice, have revealed that ERRγ plays a pivotal role in cellular bioenergetics [1], its involvement in other metabolic pathways has been appreciated only recently. Therefore, we highlight recent findings on the r
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Introduction Obesity constitutes a global healthcare problem
2020-04-01
Introduction Obesity constitutes a global healthcare problem and has many adverse effects on the cardiovascular function [1,2]. Recently, the perivascular adipose tissue (PVAT) has emerged as a relevant fat depot for cardiovascular risk and as a potential trigger in vascular dysfunction. Indeed, PV
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The data from drug screening in P berghei
2020-03-31
The data from drug screening in P. berghei (Fig. 3D) provide proof of concept that chemogenomic profiling can be accomplished in P. berghei in the same manner as P. falciparum, in that significant increases in the EC50 ratio were found only for antifolate drugs in the parasite with attenuated TgDHFR
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br Anti inflammatory effects of MTX In addition to cytotoxic
2020-03-31
Anti-inflammatory effects of MTX In addition to cytotoxic and cytostatic effects, the anti-inflammatory activity of MTX was also described by several studies. Inhibition of ATIC by MTX has been found to result in the accumulation of 5-aminoimidazole-4-carboxamide-1-β-d-ribofuranosyl 5′-monophosph
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9-cis-Retinoic Acid Naringenin is the one of
2020-03-31
Naringenin is the one of the many components in grapefruit juice. It was assumed that administration of 20mL grapefruit juice per kilogram of body weight is completely glucuronidated in the hepatic or gut wall for first pass metabolism [38]. It has been detected that one liter of grapefruit juice co
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br Advantages of modified proteins over unmodified ones In c
2020-03-31
Advantages of modified proteins over unmodified ones In contrast to small-molecule drugs, proteins are readily amenable to site-specific alterations through genetic engineering. In principle, therefore, it is possible to build in features that allow them to remain active for longer in the body an
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Phenylbenzofurans are a very important molecule skeleton
2020-03-31
Phenylbenzofurans are a very important molecule skeleton due to their synthetic versatility and their proved pharmacological properties [2]. They are synthetic compounds in which an additional phenyl ring is present in any position of the benzofuran nucleus. This could be easily obtained possible by
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Nociceptive and hyperalgesic actions of
2020-03-31
Nociceptive and hyperalgesic actions of ET-1 are produced through ETA and ETB receptors. Previous reports indicate that ETA receptor antagonists in peripheral tissues are effective in inhibiting ET-1 induced hyperalgesia, and attenuation of neuropathic pain in rats [16]. Studies have also shown that
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Phylogenetically three related CXC chemokines are
2020-03-30
Phylogenetically three related CXC chemokines are classified as the possible ligands for the teleost CXCR1 and CXCR2. They are referred to as CXCL8_L1 (CXCL8/IL-8/CXCa), CXCL8_L2 (CXCc) and CXCL8_L3 (Alejo and Tafalla, 2011, Chen et al., 2013, Laing et al., 2002, Laing and Secombes, 2004, Nomiyama e
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Levonorgestrel Interestingly ASV infusion in the dRN
2020-03-30
Interestingly, ASV-30 infusion in the dRN of saline pre-treated rats had no effect on anxiety-like behaviors. This result may be due to the saline pre-treated group exhibiting relatively low levels of anxiety-like behaviors (when compared to saline pre-treated rat of the first experiment that were n
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