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The ACC receptor family appear to be attractive targets for
2021-01-21
The ACC receptor family appear to be attractive targets for the development of novel anthelmintics. With this in mind we also tested the activity of the anthelmintics levamisole and pyrantel which activate the nematode nAChR (Martin and Robertson, 2007). We found both molecules were partial agonists
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Although in vitro and in vivo immunosuppressive effects
2021-01-21
Although, in vitro and in vivo immunosuppressive effects of female steroids have been described in fish (Yamaguchi et al., 2001, Law et al., 2001), their mode of action was not evaluated in detail. Consequently, it is of considerable interest to investigate the intracellular pathways that regulate t
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Synthetic progestogens also known as synthetic gestagens
2021-01-21
Synthetic progestogens (also known as ‘synthetic gestagens’, ‘synthetic progestins’ or simply ‘progestins’) are designed to mimic the effects of progesterone (P4) and are the active pharmaceutical ingredient in many contraceptives and hormone replacement therapies. Since most progestins are derived
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br Role of ERK signaling in preventive and
2021-01-21
Role of ERK signaling in preventive and therapeutic potential of flavonoids in neurodegenerative diseases ERK is one of the main pharmacological targets of natural phenolic compounds and contributes to several therapeutic approaches including anti-atherogenic, anti-cancer, anti-colitis, anti-arth
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The ADME profile of AAT was very promising
2021-01-21
The ADME profile of AAT-008 () was very promising, with high stability in HLM. The pre-clinical pharmacokinetic properties of AAT-008 were also assessed in rats (Sprague-Dawley, male), dogs (beagle, male), and monkeys (cynomolgus, male). The experimentally determined parameters are summarized in .
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While showing that deletion of EP
2021-01-21
While showing that deletion of EP1 maintains femur bone volume fraction and trabecular bone parameters during aging, perhaps more importantly we have also demonstrated that increased initial BV/TV in EP1 is protective against OVX-induced bone loss. That is, while mice lose an approximately equal pe
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CYP contributes to the metabolism of more
2021-01-21
CYP450 contributes to the metabolism of more than 90% of currently available drugs (Shapiro and Shear, 2002). Currently, CYP1A is the most studied xenobiotic-metabolizing isoform in fish and is often used as a biomarker for early effects of pollutants in aquatic organisms (Havelkova et al., 2007). T
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The purpose of this study is to investigate KDM B
2021-01-21
The purpose of this study is to investigate KDM1B expression and its functional significance in PC. We used lentivirus-mediated shRNA to down-regulate KDM1B expression in PC cell lines in vitro and detected the changes of cell proliferation and apoptosis. These studies provided a novel insight into
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br Discussion and conclusion Ubiquitination
2021-01-21
Discussion and conclusion Ubiquitination and deubiquitination have emerged as important mechanisms involved in p53 management. This review revealed that various DUBs can regulate p53 or p53-Mdm2-MdmX networks. Herein, we reviewed the current progress made toward elucidating the complexities in th
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br Materials and methods br Results br
2021-01-20
Materials and methods Results Discussion The first DGAT1 gene was described in the mouse in 1998 [28], and a few years later DGAT2 was identified from the oleaginous fungus Mortierella ramanniana[29]. Although both of them are known as the primary enzymes for de novo TAG biosynthesis, they
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We neither observed changes in
2021-01-20
We neither observed changes in midazolam eCLmet indicative of significant inhibition of CYP3A4/5 during both experiments, despite the in vitro evidence for CYP3A4/5 inhibition (Theile et al., 2017). The observed increase in CYP3A dependent midazolam clearance after chronic ingestion of clementines/c
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br Introduction Analyses of genomic
2021-01-20
Introduction Analyses of genomic alterations in cancer have identified epidermal growth factor receptor (EGFR) as one of the most potent “oncogenic driver” kinases that is present in many epithelial tumors including endometrial, breast, prostate, skin, esophagus, lung, stomach, colorectal, and re
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AVE-1625 A variety of fused membered ring chemotypes have
2021-01-20
A variety of fused 6–5-membered ring chemotypes have arisen such as 7-azaindole acetic acids, benzimidazolyl acetic acids, spiro-indolinone acetic acids, and indolizine acetic acids, however, to the best of our knowledge, fused 5,5-membered ring systems have not been reported. Prostaglandin D (P
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br Conflict of interest br Acknowledgments Dr Hauger was
2021-01-20
Conflict of interest Acknowledgments Dr. Hauger was supported by a BLR&D Merit Review grant from the Department of Veterans Affairs, Veterans Health Administration, Office of Research and Development. Dr. Hauger also received support from the VA Center of Excellence for Stress and Mental Healt
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This approach is similar to that suggested by the previous
2021-01-20
This approach is similar to that suggested by the previous edition of the GL [6]. Not surprisingly, the questions to be answered are the same (i.e., was the event TLOC? In cases of TLOC, is this SP 600125 of syncopal or non-syncopal origin? In cases of suspected syncope, is there a clear aetiologica
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