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Molecular docking simulations were carried out for ligands i
2024-08-30
Molecular docking simulations were carried out for ligands – in the ACE crystal structure (1O86) and DPP4 crystal structure (2G5P). Comparison of the binding mode of – () with enalaprilat (a) in ACE shows that the phenethyl group (–, enalaprilat) occupies the S1 pocket and the adjacent carboxylic fi
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IC values were obtained for an expanded version of
2024-08-30
IC50 values were obtained for an expanded version of the fragment library using the previously described mobility shift assay. Subsequently, Ki values were estimated from IC50 values to allow better comparison of the activity against targets which were measured at different substrate concentrations
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Acl converts cytosolic citrate CoA and ATP into
2024-08-30
Acl converts cytosolic citrate, CoA and ATP into acetyl-CoA, ADP+Pi and oxaloacetate (Fig. 1). This cytosolic enzyme is present in few Prokaryotes and in all Eukaryotes, but not in non-oleaginous yeasts [14]. Thus, this enzyme was presumed to be essential for FA synthesis [1], [13], [15]. In most mi
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To the best of our knowledge only cases
2024-08-29
To the best of our knowledge, only 3 cases of an E196K mutation have been described since it was first identified in 2000 [15], [16], [17], although 5 cases, accounting for 1.1% of all genetic TSE cases, were reported with no precise data on the clinical phenotypes in the EUROCJD collaborative surve
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br Antifungal resistance what is in a name Antifungal
2024-08-29
Antifungal resistance, what is in a name? Antifungal resistance is an emerging and hot topic in the field of medical mycology. Microbiological resistance is identified by determining minimal inhibitory concentrations (MICs) in vitro for a given antifungal and interpreting this value according to
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br Conflict of interest br Acknowledgement We
2024-08-29
Conflict of interest Acknowledgement We wish to thank the Program of National Key R&D Program of China (2017YFD0200500) and the Fundamental Research Funds for the Central Universities (KYTZ201604) for partially funding this work. Introduction Chitosan ((1→4)-2-amino-2-deoxy-β-d-glucose) is
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N,N-Dimethylsphingosine and LO are members of
2024-08-29
5- and 12/15-LO are members of the lipoxygenase family that convert arachidonic N,N-Dimethylsphingosine into lipid mediators such as leukotriene B4 (LTB) and 12()-hydroxyeicosatetraenoic acid (HETE) and 15()-HETE, respectively. Evidence from several in vitro and in vivo studies has shown that activ
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br Concluding remarks Enhanced membrane
2024-08-29
Concluding remarks Enhanced membrane binding upon calcium stimulation in ro5 mg suggests a pre-requisite step that involves a conformational change in LOX. This might facilitate it to tether to the membrane and regulate enzyme activity. The calcium binding loops and the putative active site entr
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MD was the recipient of the Intergroupe Francophone de Canc
2024-08-29
MD was the recipient of the Intergroupe Francophone de Cancérologie Thoracique (IFCT) Alain Depierre Grant in 2014. JP was the recipient of the ARISTOT (Association de Recherche, d’Information Scientifique et Thérapeutique en Oncologie Thoracique) grant in 2016. Conflicts of interest statement
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Introduction Glaucoma consists of a group
2024-08-29
Introduction Glaucoma consists of a group of eye diseases showing a broad spectrum of clinical presentation and unknown aetiologies, that lead to a permanent loss of visual function due to the death of retinal ganglion N1-Methyl-ATP and damage of the optical nerve. It is well accepted that a criti
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Our previous work fails to show any
2024-08-29
Our previous work fails to show any maternal effect with blockade of 5-HT2A receptor, as acute and repeated treatment of MDL100907 does not alter maternal behavior at the behaviorally active doses (Chen et al., 2014). In the present study, MDL100907 pretreatment attenuated the maternal disruptive ef
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In terms of the full length
2024-08-29
In terms of the full-length proteins, it was noted early on that ACs have two cellular localizations: as integral proteins of the plasma membrane and as soluble proteins in the cytosol. Based on the distribution in mammalian sequences, it was initially proposed that subclass IIIa contains only membr
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br Acknowledgements MC and PD were funded
2024-08-28
Acknowledgements MC and PD were funded by the Michael J Fox Foundation (Grant ID 9969). We would like to thank Pierluigi Saba, Francesco Traccis and Barbara Tuveri for their technical assistance. Introduction In the prostate, androgens play a crucial role in normal, BPH and cancerous growth b
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Introduction Cytochrome P CYP aromatase catalyzes
2024-08-28
Introduction Cytochrome P450 19 (CYP19; aromatase) catalyzes the conversion of androgens to estrogens in a three-reaction sequence, where each step depends on NADPH and O2 [[1], [2], [3]]. The first two steps are accepted to be hydroxylations of the steroid C19 methyl group, whereas the final step
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br Conclusion br Acknowledgments The authors extend
2024-08-28
Conclusion Acknowledgments The authors extend their appreciation to Kayyali Chair for Pharmaceutical Industry, Department of Pharmaceutics, College of Pharmacy, King Saud University for funding this work through the research project Number (G-2016-2). Introduction L-ornithine is a natural
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