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A set of small molecule LigI
2019-11-12
A set of small molecule LigI inhibitors were identified through an in silico structure-based screen, using the atomic resolution structure of LigI complexed with nicked DNA [[18], [26]]. This screen yielded inhibitors that were selective for LigI (L82), inhibited both LigI and LigIII (L67) and inhib
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aa dutp In summary our findings show
2019-11-11
In summary, our findings show that LPS can activate CysLT2R on microglial aa dutp to induce microglial inflammation and microglia-dependent neuronal death. Furthermore, pharmacological inhibition or knocking down of CysLT2R expression protects neurons against neurotoxicity via suppression of LPS-in
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Compounds and administered orally to fasted Harlan Sprague
2019-11-11
Compounds , , and administered orally to fasted Harlan Sprague-Dawley rats 1h prior to trigeminal stimulation, decreased extravasation in this model in a dose-related manner, with an estimated ID of 1, 10 and 100μg/kg, respectively (determined 15min after stimulation, ). For comparison, the clinical
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VLX600 receptor Nucleophosmin NPM which also plays a role on
2019-11-11
Nucleophosmin (NPM1), which also plays a role on the nuclear export of ribosomal proteins and subunits (Maggi et al., 2008), is also a relevant MYC target, presumably through an interaction with CRM1. Conversely, it has been recently reported that specific SINE compounds reduce the levels of MYC in
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br Materials and methods br Results Recently a quantitative
2019-11-11
Materials and methods Results Recently, a quantitative proteomic analysis of C2C12 mouse myoblasts cell line totally deprived of protein kinase CK2 catalytic subunits (CK2α/CK2α′(−/−)), suggested that the cellular expression of HSP27, a chaperone with multiple functions related to proteostasis
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E ligases provide substrate recognition specificity Ubiquiti
2019-11-11
E3 ligases provide substrate recognition specificity Ubiquitination raas inhibitors and substrate specificity in mammals is achieved by the existence of over six-hundred E3-ubiquitin ligases that catalyze the final step of ubiquitination, compared with only one E1 and very few E2 enzymes known til
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br Discussion The regulation of intracellular cholesterol le
2019-11-11
Discussion The regulation of intracellular cholesterol levels is a biological process of vital importance for cellular function and integrity, and involves robust transcriptional and post-transcriptional mechanisms that are sensitive to metabolic feedback control. Amongst post-transcriptional mec
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G DH has gained interest because of
2019-11-11
G3DH has gained interest because of its broad substrate specificity and site-selective oxidation properties [9,10]. The conversion product, 3-ketoglycoside, possesses potential as a starting material for the chemical industry such as in polymer and surfactants because the keto group becomes a specif
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Dehydrogenation by a KSTD is also a crucial step
2019-11-11
— 1(2)-Dehydrogenation by a Δ1-KSTD is also a crucial step during STF 083010 degradation of the steroid core. Several Δ1-KSTDs were shown to be active under either aerobic or anaerobic conditions [27,29,47,50,66]. Furthermore, the last common intermediate of both aerobic and anaerobic steroid degrad
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Furthermore the determination of downstream target genes ind
2019-11-11
Furthermore, the determination of downstream target genes induced by CdCl2 is noteworthy and can help to define its underlying carcinogenesis mechanism. Therefore, we evaluated c-fos and c-jun expression which are stimulated by estrogen through ERK/MAPK pathway. These are not only proto-oncogenes wh
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Previous studies demonstrated that cPLA translocates to the
2019-11-11
Previous studies demonstrated that cPLA2α translocates to the phagosomal membrane during macrophage phagocytosis through mechanisms that, in humans, involve phosphorylation of the enzyme by c-Jun N-terminal kinases and membrane association via the cationic cluster of four lysine residues present at
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Recoverin is a kDa retinal protein that binds
2019-11-11
Recoverin is a 23-kDa retinal protein that binds to calcium. It regulates the Gedunin of rhodopsin during visual transduction within photoreceptor cells. Since the pathogenicity of anti-recoverin antibody is potent, anti-recoverin CAR patients often have progressive visual impairments, characterized
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AMTB hydrochloride The current study demonstrates a link bet
2019-11-11
The current study demonstrates a link between heme metabolism and mitochondrial Co-I, which deficits instigate abnormalities in the metabolism of heme and its downstream targets both in-vitro in patients and healthy subjects derived LCLs and in-vivo in brains of SZ-rat model. A further study of the
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br DNA end processing enzymes The simplest DSB
2019-11-08
DNA end processing enzymes The simplest DSB is one that consists of two blunt DNA ends as these termini can be re-joined without processing. However, DSBs induced by ionizing radiation and reactive oxygen species are notorious for producing DNA ends which are non-ligatable (“dirty ends”) and thus
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etc Since the initial identification of
2019-11-08
Since the initial identification of DNA ligase inhibitors by a structure-based approach [[18], [26]], there have been several reports describing LigI inhibitors using computer modelling and derivatives of the original DNA ligase inhibitors [[49], [50], [51]]. While these studies have shown that the
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