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To study systemic potential of the selected
2020-12-14
To study systemic potential of the selected compounds as EP1 receptor antagonist, they were evaluated with regard to the sulprostane-induced increase of intravesical bladder pressure in rats. Some of the analogs, 13 and 15–17, which were selected on the basis of their in vitro EP1 receptor affinity,
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br Conclusions Two chemical coupling agents BTDE
2020-12-14
Conclusions Two chemical coupling agents, BTDE and CDI, were used to activate the free hydroxyl groups of plant cellulose powder and OPH from Flavobacterium ATCC 27551 immobilized on modified carriers by covalent linkages. The highest immobilization yields obtained in optimum conditions of effect
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Generally glycines and other small residues
2020-12-12
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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wnt signaling Given the link between E s
2020-12-12
Given the link between E3s, autoimmunity, and antitumor immunity, it wnt signaling is reasonable to assume that, similar to other ICBs, IRAEs may limit the clinical use of E3-targeting therapies – further stressing the need to better understand the underlying mechanisms of these unwanted effects. D
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FOX proteins constitute a large class of transcription facto
2020-12-12
FOX proteins constitute a large class of transcription factors with multiple functions, from development and organogenesis to regulation of metabolic and immune functions. The Fox transcription factor is characterized by a 100-amino-acid wing helix or forkhead DNA-binding domain. In addition, the FO
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br Results The AR genotype frequencies are
2020-12-12
Results The AR genotype frequencies are shown in Table 1. Alleles at the two loci are in linkage disequilibrium, as expected for such closely linked loci and consistent with previous findings (Kittles et al., 2001). The genotype frequency for the DBH 1021 polymorphism is similar to previous find
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br Acknowledgments Studies in the Tomkinson laboratory on
2020-12-12
Acknowledgments Studies in the Tomkinson laboratory on DNA ligase III are supported by research grants from the National Institutes of Health (P01 CA92584 and ES12512 to AET), a grant from the V Foundation and the University of New Mexico Cancer Center. Introduction Ionizing radiation (IR) as
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br DGKs inhibition and signaling Local DAG levels are strict
2020-12-12
DGKs inhibition and signaling Local DAG levels are strictly controlled by a balance between synthesis and degradation rates. Both receptor controlled PLC-mediated production and DGK-mediated degradation are classically implicated in the control of “signaling” DAG. However, this dogma is starting
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To determine direct DDR binding
2020-12-12
To determine direct DDR1-binding partners and to further connect to Akt and mTOR signaling, we performed mass spectrometry on DDR1 immunoprecipitates and found various candidates of the Akt and mTOR pathway such as LARP1 (La-related protein 1) and RPS6 (40S ribosomal protein S6/ S6). Most intriguing
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Moreover recent structural studies of VEEV nsP pro in
2020-12-12
Moreover, recent structural studies of VEEV nsP2pro in complex with E-64d revealed an important molecular interaction at the interface of two subdomains. In this structure, Asn475 which is in polar contact with carbonyl oxygen of Asp507 of the protease subdomain makes an H-bond with Arg662 of the MT
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br Materials and methods br Results Metabolic stability of
2020-12-11
Materials and methods Results Metabolic stability of compounds was studied by incubation with pooled human liver microsomes. Piperine was the metabolically most stable compound, with a t1/2 of 141min (Fig. 2, and Table 1). SCT-29 and LAU 397 showed t1/2 of approx. 45min, whereas a t1/2 of only
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It was recently reported that
2020-12-11
It was recently reported that a functional single nucleotide polymorphism (rs75932628) within Triggering receptor expressed on myeloid nicotinic receptor agonist 2 (TREM2) is associated with AD (Guerreiro et al., 2013). Homozygous loss of function mutations in TREM2 are also associated with an auto
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Since protein kinase CK has over known substrates
2020-12-11
Since protein kinase CK2 has over 300 known substrates we examined if the inhibitory effects described above could also be detected using another substrate. Therefore, we employed the synthetic peptide RRRADDSDDDDD which is often used in CK2 inhibitory studies. Quite contrary to the phosphorylation
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EP receptors belong to the family of
2020-12-11
EP1–4 receptors belong to the family of G protein-coupled receptor (GPCR). Trafficking events such as externalization, internalization, recycling and degradation dynamically regulate GPCR cell surface density. A fast-rate of internalization and degradation reduces GPCR surface density to desensitize
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Given that CE plays an
2020-12-11
Given that CE plays an essential role in schistosome invasion, its immunoreactivity and protective potential is of significant interest. The native form of SmCE was found to be poorly immunogenic in immunized mice. An earlier study found that sera from S. mansoni patients have shown the presence of
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