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br Acknowledgments We thank Jon Clardy Juan Manuel Dom
2019-09-16
Acknowledgments We thank Jon Clardy, Juan Manuel Domínguez, José Francisco García Bustos, and the GlaxoSmithKline (GSK) Plasmodium falciparum dihydroorotate dehydrogenase project team for their contributions, helpful advice, and discussions. Introduction Dihydroorotate dehydrogenase (DHODH) i
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We recently reported that the
2019-09-16
We recently reported that the information about the electronic density obtained from a QTAIM analysis is useful to describe the molecular interactions that stabilize and destabilize the different complexes L-R [13], [14], [15]. Specifically in our previous work reported for DHFR inhibitors, the QTAI
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The binding of collagen X to DDR differs from
2019-09-16
The binding of collagen X to DDR2 differs from the binding of collagen X to α2β1 integrin in that the triple helical conformation is essential for DDR2 binding. We previously reported that heat denatured pepsinised collagen X supported cell adhesion via α2β1, indicating that the triple-helical confo
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Discussion In this paper we present insights
2019-09-12
Discussion In this paper we present insights into the observed specificities of inhibitors targeting the ubiquitin-activating and related E1 Phenylbutyrate via crystal structures of the specific NEDD8-E1 inhibitor MLN4924, the dual NEDD8/Ub E1 inhibitor ABPA3, and the selective Ub-E1 inhibitor MLN7243 bound to yeast Uba1, and augment these structures with biochemical and computational studies.
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Astrocytes play a key role in the brain
2019-09-11
Astrocytes play a key role in the brain, as these cells are involved in fluid, ion, pH, and neurotransmitter homeostasis, synapse function, energy and metabolism and blood-brain barrier (BBB) maintenance (Sofroniew and Vinters, 2010).
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Concholepas concholepas our model species
2019-09-10
Concholepas concholepas, our model species for this study, is a marine gastropod found along the Chilean coast that has become commercially important [25], [26], [27].
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Our earlier experimental studies showed
2019-09-09
Our earlier experimental studies showed neutral i.e. non-proliferative, effects of progesterone but a large increase in proliferation using certain progestins; however, this was only in the presence of PGRMC1 [[13], [14], [15], [16], [17], [18], [19]].
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Conclusion We have constructed a series
2019-09-07
Conclusion We have constructed a series of potent and greatly selective DPP-4 inhibitors with pyrazolo[1,5-a]pyrimidin-7(4H)-one core surrogates. The modification of the core led us to b2 which has IC50 of 80 nM and > 1000 fold selectivity over DPP-8 and DPP-9.
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In conclusion we designed novel E1 inhibitors
2019-09-06
In conclusion, we designed novel E1 inhibitors based on the three-dimensional structure of E1 in complex with ubiquitin. Following an enzymatic assay evaluating synthetic compounds and we identified compound as a novel E1 inhibitor.
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Among the high value compounds derived from
2019-09-05
Among the high value compounds derived from agricultural residues there are enzymes with industrial application. The extraction processes have been focused on the development of new strategies that guarantee high recovery rates with maximum activity (Nadar et al., 2017).
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In summary our data demonstrated a biological
2019-09-04
In summary, our data demonstrated a biological function of cpt1a gene from large yellow croaker. In particular, we indicated the effects of fasting on free carnitine status, CPT1 kinetics, and cpt1a mRNA expression in liver of large yellow croaker. During short-term fasting, the fish liver may have a strong capacity for ensuring the optimal catalytic efficiency through regulating carnitine-dependent Km rather than gene transcription and enzyme avtivity.
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In sum although it is reasonable to assume that the
2019-09-03
In sum, although it is reasonable to assume that the activities of an enzyme on alternative (metabolically available) substrates may often depend on neutral drift, the point is difficult to prove because various types of selective pressures can be at play, and these will be different in different organismal lineages 57, 58.
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After repeated intermittent exposure
2019-09-02
After repeated, intermittent exposure to a psychostimulant an augmentation of drug response to motor activity is commonly observed, a phenomenon known as behavioral sensitization (Kalivas and Stewart, 1991, Steketee and Kalivas, 2011).
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These studies established IAP proteins as
2019-08-30
These studies established IAP proteins as dimeric RING E3 ligases, but did not account for the essential role of dimerization.
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Primases are classified into two major groups
2019-08-29
Primases are classified into two major groups: first, the DnaG primases, found in bacteria and bacteriophages, and second, the archaeoeukaryotic primases.
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