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On the contrary the benzhydrol series showed modest
2021-12-09

On the contrary, the benzhydrol series showed modest activity with EC of two digit micromole. The bulkiness of the tetraethylammonium tail may be the reason for the low activity. Interestingly, introduction of H-bonding groups, such as OMe in and CF in , slightly improved the activity compared to
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In order to understand the
2021-12-09

In order to understand the determinants of high affinity of with amide side chain, an X-ray crystal structure of human liver FBPase in complex with was determined (). The position of phosphonate group and tricyclic scaffold of is similar to those of with no side chain, which suggests the formation o
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In non Hodgkin lymphoma the catalytic SET domain of
2021-12-09

In non-Hodgkin lymphoma the catalytic SET domain of the histone methyltransferase EZH2 is subject to recurrent heterozygous missense mutations . These alterations have been observed in ∼20% of patients with diffuse large B cell lymphoma (DLBCL) and ∼10% of patients with follicular lymphoma (FL). Th
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Figure shows the network of the persons with diagnosed
2021-12-09

Figure 2 shows the network of the 47 persons with diagnosed HIV and their 192 contacts. Of the contacts, 149 (78%) were first-generation contacts and 43 (22%) were second-generation contacts. Color and shape combinations used for network nodes (i.e., persons) allow one to simultaneously discern past
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Oxidative stress results from the
2021-12-08

Oxidative stress results from the disequilibrium between levels of prooxidant molecules produced and the ability of a biological system to detoxify and neutralize the reactive molecules [14]. OS is a chronic, self-perpetuating state of damage to cells and increased inflammation resulting from the co
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Several groups studied CTD mouse models which
2021-12-08

Several groups studied CTD mouse models, which largely mimicked the symptoms (i.e. impaired cognition and autistic-like behaviour) of the human disease (Kurosawa et al., 2012; Baroncelli et al., 2016; Stockebrand, 2018). The CRT-1 knockout mice showed a drastic deterioration in the GABAergic system,
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In vitro studies have shown that some antidepressant drugs b
2021-12-08

In vitro studies have shown that some antidepressant drugs bind to NMDA receptors and inhibit the binding of NMDA receptor ligands [18]. Similarly, several research teams have reported that tricyclic antidepressants can modulate the release and/or uptake of glutamate [19]. In this study, we found th
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br Materials and methods br Results br
2021-12-08

Materials and methods Results Discussion The glucose transporter GLUT1 can be acutely activated or inhibited in L929 fibroblast BMX-IN-1 by a wide variety of reagents or nutrient conditions [[9], [10], [11], [12],36,50]. This abrupt change in the activity of GLUT1 occurs within minutes and
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In conclusion we provided the
2021-12-08

In conclusion, we provided the first evidence of a modification and regulation of GCK by O-GlcNAc modification that until now was not explored. This discovery provides important clues in the prevention of hyperglycemia and development of novel therapeutic drugs to treat type 2 diabetes. Acknowled
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The bFGF induced upregulation of
2021-12-08

The bFGF-induced upregulation of both GR and MR levels observed in our study raises a question regarding whether the simultaneous augmentation of the two receptors has a physiological and/or medical significance. It has been suggested that MR stimulates intracellular signaling pathways to minimize s
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br Acknowledgments br Introduction Postmenopausal osteoporos
2021-12-08

Acknowledgments Introduction Postmenopausal osteoporosis, which is primarily caused by KN-92 deficiency, has been a worldwide health problem and threatens postmenopausal women of all races. An estimated 80% of osteoporosis patients in the United States are women, and approximately 30% of postm
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br Conflict of interest br Transparency document br
2021-12-08

Conflict of interest Transparency document Acknowledgements We acknowledge our funding sources from the American Heart Association (13EIA4480016) and the National Institute of Health/National Heart, Lung, and Blood Institute (RO1 HL094414). We are very grateful to Dr. Shaohua Xiao and Dr. S
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The overall decrease in consummatory drive seen in
2021-12-08

The overall decrease in consummatory drive seen in rodents treated with naltrexone in previous studies is in accordance with the effects seen with mice treated with SNAP 37889 in this study. While it may seem inappropriate to use a broad-acting drug like SNAP 37889 that suppresses overall consummat
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Current guidelines for thromboprophylaxis recommend the use
2021-12-08

Current guidelines for thromboprophylaxis recommend the use of vitamin K antagonists (eg, warfarin), low-molecular-weight heparin (LMWH), or indirect inhibitor of factor Xa . Aspirin is also used for thromboprophylaxis in patients undergoing orthopedic procedures , . The efficacy and safety of LMWH
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The progression of HIV varies
2021-12-07

The progression of HIV varies from patient to patient, with some who progress slowly and others who progress much faster. However, CD4+ and CD8+ cell counts are intimately linked in those that are able to suppress the HIV infection (Walker et al., 1986; Saez-Aninon et al., 2007). Depletion of these
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