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Introduction DHFR is an important enzyme in both
2020-07-29

Introduction DHFR is an important enzyme in both mammals and microorganism including Mycobacterium tuberculosis (Mtb). It catalyzes folic BCTC conversion to dihydro and tetrahydro folic acid which is a crucial step in folate pathway [1]. Inhibition of folate pathway leads to interruption of thymid
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We have previously shown that the receptor
2020-07-29

We have previously shown that the receptor for advanced glycation end products (RAGE) is expressed by JW 55 in-vitro and in-vivo and that a RAGE ligand interferes with calvarial bone healing [53]. Combined with the current study, an understanding emerges that AGE-modification of collagen inhibits bi
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The role of DDR in glomerular injury
2020-07-29

The role of DDR1 in glomerular injury has been then further studied by the Chatziantoniou group in experimentally-induced crescentic glomerulonephritis, by injection of alloimmune sheep nephrotoxic serum (NTS) [54]. Glomerulonephritis produced a 17-fold increase of DDR1 expression, predominantly in
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Udenafil is a novel PDE inhibitor that has an established
2020-07-29

Udenafil is a novel PDE5 inhibitor that has an established record of safety and efficacy in adult males for the indication of erectile dysfunction., , In that population, the pharmacokinetics (PK) of udenafil (molecular weight 516 g/mol) and the major circulating metabolite, DA-8164 (molecular weigh
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What are the molecular signals that guide
2020-07-28

What are the molecular signals that guide Tfh cells as they navigate around the lymph node in the course of the immune response? It was recently reported that Tfh cells inside GCs have high expression of SIPR2, which acts to repel them from the S1P-rich lymph in the SCS and promote their retention i
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A structural model for the unprecedented interactions
2020-07-28

A structural model for the unprecedented interactions between UBE2S, its target (i.e., a Ub that has been linked already to an APC/C substrate), and APC/C was generated by hybrid structural studies merging information from NMR, crosslinking, and mutational data with a low-resolution cryo-EM map of A
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DCPIB In the case of high fidelity polymerases
2020-07-28

In the case of high-fidelity polymerases, we propose that water is used to achieve negative selection against nucleotide binding. With specialized DNA polymerases, we propose that nucleobase desolvation plays a different yet important role in allowing these enzymes to replicate damaged DNA. In this
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The reduced DNA stability at RH
2020-07-28

The reduced DNA stability at 100% RH confirms previous results for incubates at these conditions, although in the present study amplifiable DNA still survived for months. The crucial point appears to be the onset of microbial growth, which happened at room temperature and at 35 °C. In the biological
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br Mammalian alkyladenine DNA glycosylase
2020-07-28

Mammalian 3-alkyladenine-DNA glycosylase (MAG or AAG) Whilst some bacteria contain two or more distinct DNA glycosylases that catalyze the excision of 3meA from DNA, mammalian cells have only one (MAG, also called AAG for 3-alkyladenine-DNA glycosylase) (Fig. 2). Interestingly, mammalian AAG sho
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The prokaryotic DgkB from Staphylococcus
2020-07-28

The prokaryotic DgkB from Staphylococcus aureus is essential for lipoteichoic NSC 207895 synthesis (Matsuoka et al., 2011) and its solubility makes it particularly interesting with respect to its relevance to mammalian DGKs. Importantly, this is the first bona fide DGK with a solved structure (Mill
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DHODH is the only enzyme in the pyrimidine
2020-07-28

DHODH is the only enzyme in the pyrimidine biosynthesis that is located in the mitochondria rather than the cytosol. Mitochondria are intracellular organelles that are mainly associated with the electron transport chain (ETC) and generation of cellular energy. Mitochondrial bioenergetics plays a sig
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br Conclusion Further optimization of a
2020-07-28

Conclusion Further optimization of a 7-azaindole-3-acetic Sal 003 chemotype derived from HTS delivered a new sub-series of selective CRTh2 receptor antagonists. Exploiting observations from the earlier sulfonamide sub-series, where lipophilicity reduction led to improved eosinophil SC potency, c
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br Experimental br Acknowledgements The
2020-07-28

Experimental Acknowledgements The authors thank Dr. Takanobu Kuroita for helpful discussions during the preparation of the manuscript. The authors also thank Dr. Katsumi Kobayashi, Mr. Takuto Kojima and Mr. Yoshirou Tomimatsu for helpful discussions during the preparation of the research repor
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Those effects seem to be associated with COMT activity
2020-07-28

Those effects seem to be associated with COMT activity, itself related to COMT genetic polymorphisms. The levels of COMT activity vary not only between individuals but also between the tissues of the same person. Val158Met seems to be the most important SNP showing an impact on COMT function. The co
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br Discussion In this paper we have explored the
2020-07-28

Discussion In this paper, we have explored the phosphorylation of human and murine p53 by the protein kinase CK1 in vitro. The most striking observation which is evident from our data is that prior phosphorylation of serine 15 in vitro can create a potent recognition determinant for subsequent ph
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