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A set of small molecule
2021-08-25
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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To understand more clearly how these
2021-08-25
To understand more clearly how these activities are combined in the heterotrimeric enzyme and to understand more clearly how DNA alkylation might effect DNA helicase activity, we summarize the relevant features of the structure of RecBCD determined in the presence of DNA. The RecB and RecC subunits
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br Acknowledgements br Introduction Lung cancer treatment st
2021-08-25
Acknowledgements Introduction Lung cancer treatment strategies, especially molecular targeted therapy, have progressed rapidly. However, most established treatments are for adenocarcinoma of the lung, not for squamous cell carcinoma (SQCC). SQCC constitutes approximately 30% of lung cancers, w
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SAR131675 During host cell interactions G intestinalis
2021-08-25
During host-cell interactions, G. intestinalis trophozoites up-regulate several cell-associated proteins, including high-cysteine membrane proteins (HCMPs) and variant surface proteins (VSPs) [8]. The parasite also releases around 200 proteins upon host-cell contact, including many proteases [9,10].
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The sex dimorphic expression of mouse CYP A
2021-08-25
The sex-dimorphic hyPerFUsion™ high-fidelity PCR Kit of mouse CYP3A is partially due to sex-dimorphic plasma GH profile which is a decisive factor in the regulation of sexspecific CYP isoforms [14]. Nevertheless, in our study we did not observe any changes in plasma GH levels in either mouse sex wit
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The observed increase in Bdnf
2021-08-25
The observed increase in Bdnf1 mRNA occurred 1 h after treatment indicates participation of BDNF in early plasticity and subsequently mnemonic processes. Most of the evidence regarding the importance of BDNF for memory formation derived from electrophysiological studies that utilized the molecular c
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Constitutive activity of Ras Raf MEK
2021-08-24
Constitutive activity of Ras/Raf/MEK/ERK pathway plays a critical role on melanoma growth, thus inhibition of activity of Ras, Raf and MEK can reduce ERK activity, leading to a decrease in melanoma cell proliferation, survival and invasion (Burotto et al., 2014; Paluncic et al., 2016). Our results a
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While showing that deletion of EP maintains
2021-08-24
While showing that deletion of EP1 maintains femur bone volume fraction and trabecular bone parameters during aging, perhaps more importantly we have also demonstrated that increased initial BV/TV in EP1 is protective against OVX-induced bone loss. That is, while mice lose an approximately equal per
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Synthesis of and is described
2021-08-24
Synthesis of 5–7, 12–14, and 18 is described in Scheme 3. Compounds 5–7 and 18 were prepared as outlined in Scheme 3a. Reaction of 4-bromomethylbenzoic Prednisone (36) with thionyl chloride yielded the corresponding acid chloride, which was converted to the corresponding amide 40a by the usual ammo
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A decrease in heme levels enables
2021-08-24
A decrease in heme levels enables the phosphorylation of eIF2α by HRI and thereby inhibition of eIF2α activity. Indeed, the relatively small change in cytosolic heme levels in SZ Walrycin B showed downstream functional consequences manifested by almost 50% elevation in the phosphorylation of eIF2α
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Generally glycines and other small residues such as alanine
2021-08-24
Generally, glycines (and other small residues such as alanine) present in a helical GxxxG-motif that are facing the same side of the helix form a uniform surface that enables direct contact with a second helix. Crystal structures of multipass membrane proteins have demonstrated that GxxxG-motifs are
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In plants SUMOylation has been shown to
2021-08-24
In plants, SUMOylation has been shown to modulate plant hormone signaling (Lois et al., 2003, Miura et al., 2009, Conti et al., 2014), root stem cell maintenance (Xu et al., 2013), and responses to abiotic and biotic stress (Lois, 2010). Many of the plant biological processes regulated by SUMOylatio
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UBA belongs to the non canonical E enzymes
2021-08-24
UBA5 belongs to the non-canonical E1 enzymes that lack a defined Cys domain but have the active-site Cys within the adenylation domain [24]. Similar to other E1 enzymes, UBA5's adenylation domain comprises an eight-stranded beta sheet that is surrounded by helices [21]. Moreover, like the ancestral
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br Results br Discussion Thus the
2021-08-23
Results Discussion Thus, the biochemical and structural studies of six Maf proteins from different organisms have revealed two subfamilies of new enzymes with the metal-dependent nucleoside triphosphate pyrophosphatase activity against both canonical and noncanonical pyrimidine nucleotides (Yh
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AMD is equally active against
2021-08-23
AMD3100 is equally active against a broad range of HIV-1 and HIV-2 strains, but not against simian immunodeficiency virus (SIV) strains in human PBMC (De Clercq et al., 1994). At this moment it is not clear what coreceptor SIV is using in human PBMC, but it does not seem to be CXCR-4 (Feng et al., 1
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