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In order to evaluate the
2020-06-15
In order to evaluate the in vivo pharmacology associated with EP receptor antagonism, we wished to discover antagonists presenting a higher degree of selectivity over the other prostanoid receptors. We also wanted to increase the brain–blood ratio since it is probable that centrally mediated EP agon
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While oxysterols were most extensively studied for its poten
2020-06-15
While oxysterols were most extensively studied for its potent ability to mediate feedback regulation of cholesterol biosynthesis, some early investigations showed that the enzymes involved in its syntheses were highly upregulated in macrophages and dendritic cells—an indication of possible roles in
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All components of the UPP
2020-06-15
All components of the UPP were predicted to be susceptible to oxidative stress due to the cysteine residues in their active sites [36]. Curcusone D inhibits DUBs but has no significant effect on the action of E1, E2s, E3s, or the proteasome, which indicates that the targets of the ROS induced by cur
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CC-223 mg br Author Contributions br Acknowledgments br Intr
2020-06-15
Author Contributions Acknowledgments Introduction Many anticancer agents bind covalently to DNA, introduce bulky adducts, and inhibit DNA metabolic processes including repair, replication and transcription.1., 2., 3. Frequently, the first enzymes to encounter DNA adducts are DNA helicases.
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One possible explanation for differences in the binding
2020-06-15
One possible explanation for differences in the binding ability of monomeric versus dimeric forms of DDR2 ECD to collagen could be that the monomeric form only binds to the primary GVMGFO site, whereas dimeric (and oligomeric) DDR2 ECD binds to additional sites on the collagen triple-helical molecul
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In conclusion DDR ECD was
2020-06-15
In conclusion, DDR1 ECD was shown to be sufficient for collagen mediated DDR1 oligomerization, and the oligomerized form binds to collagen with increased affinity. In full length receptors expressed on live cells, DDR1 oligomerization occurred on the cell surface in agreement with the role of DDR1 E
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br Acknowledgements br This work
2020-06-15
Acknowledgements This work was supported by grants from the National Natural Science Foundation of China (Grant No.: 30260088) and the prophase research for National “973” Project of China (Grant No.: 2007CB116203). The DNA sequences of Hbvp1 and the Hbvp1 promoter were deposited in GenBank, an
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The early serologic response of infants to infection with
2020-06-15
The early serologic response of infants to infection with HIV-1 is obscured by the presence of transplacentally acquired maternal HIV antibody. However, the HIV PTC209 HBr mg produced in vitro by peripheral blood from infants has been studied (Pollack et al., 1993) and it has been shown that neonat
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CPG a metalloenzyme derived from sp was the elected
2020-06-15
CPG2, a metalloenzyme derived from sp., was the elected enzyme for the first pilot-scale clinical trial of ADEPT. This enzyme has no mammalian homologue and activates glutamic CGRP (rat) prodrug derivatives of several nitrogen mustards alkylating agents., , , , , A bond cleavable by CPG2 is essen
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Materials and methods Construction of the Chk YB
2020-06-15
Materials and methods Construction of the Chk-YB-1b-Neo vector. Approximately 107 plaques from a chicken genomic library established in EMBL3 vector (Clontech Palo Alto, CA) was screened and one clone containing a 12kb insert was selected. Digestion of this clone with SalI and EcoRI restriction enz
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Introduction Neuropathic pain occurs in approximately one
2020-06-15
Introduction Neuropathic pain occurs in approximately one-third of patients with diabetes and is refractory to currently available analgesic drugs (Abbott et al., 2011). This painful diabetic neuropathy (PDN) is associated with elevated levels of methylglyoxal (MG; a reactive glucose metabolite) an
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TraM is one of two transfer proteins from pIP T
2020-06-15
TraM is one of two transfer proteins from pIP501 T4SS that have structural similarity to the A. tumefaciens VirB8 protein (Fercher et al., 2016, Goessweiner-Mohr et al., 2013), a central member of the inner membrane complex (Bailey et al., 2006, Guglielmini et al., 2014, Trokter et al., 2014). VirB8
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The imbalance that renders greater lipid uptake toxic
2020-06-15
The imbalance that renders greater lipid uptake toxic is unclear, but the comparison of our in vitro studies with those in mice illustrates the importance of TAG storage versus accumulation of less non-polar molecules. Protective effects of ACSL1 and PPARγ have been reported in other cell types. Par
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A structural explanation for how RBR RING s handle
2020-06-15
A structural explanation for how RBR RING1s handle their bound E2~Ubs differently from canonical RINGs has not been readily apparent. Only a few residue positions are strongly conserved in RING and RING1 domains, most of which are zinc-coordinating Cys and histidine residues. A key position in canon
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Many studies reporting on discoveries of DUBs in the TGF
2020-06-15
Many studies reporting on discoveries of DUBs in the TGFβ and BMP pathways have relied on RNAi strategies to investigate loss-of-function impact. While RNAi strategies are useful tools, there are limitations ranging from limited knockdowns of targets to potential off-target effects. New and better t
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