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This structure guided the variation
2020-09-19
This structure guided the variation of the compounds aiming either at enhanced interaction with CK1 or to exclude interaction with CK1 (R=Me, 15). We chose the 5-cloro substituted oxoindole as backbone as it is supposed to show enhanced metabolic stability, which is commonly used in medicinal chemis
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It is not precisely known which of the intramolecular
2020-09-19
It is not precisely known which of the intramolecular interactions created by the SH2 domain, the SH3–SH2 linker and the SH2–kinase linker are essential for the catalytic activity of Csk or how these interactions regulate Csk activity. Thus far it has been shown that site-directed mutagenesis of SH3
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Colchicine br Acknowledgements br A subgroup
2020-09-19
Acknowledgements A subgroup of pediatric solid neoplasms, collectively referred to as small round cell tumors (SRCTs) of childhood, demonstrates undifferentiated small round cell morphological characteristics. The SRCTs include neuroblastomas, lymphomas, and several bone and soft tissue sarcoma
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br Introduction Phoenixin PNX is a
2020-09-19
Introduction Phoenixin (PNX) is a recently discovered peptide produced mainly in hypothalamus by proteolytic cleavage of a small integral membrane protein 20 (Smim20) [1]. The most important endogenous active isoforms of PNX are amided peptides, composed of 14 and 20 chem 8 [2]. Previous data pr
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Both receptors belong to the
2020-09-19
Both receptors belong to the large family of G protein-coupled receptors (GPCRs) [4,5], which often appeared as monomers, dimers and higher order aggregates [6,7]. There is evidence that these receptor-complexes can modulate the functionality and the pharmacology of the receptors [8,9] by sequesteri
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In regards to regional variation
2020-09-19
In regards to regional variation in metabolic behavior of adipose tissue, subcutaneous adipose tissue transplantation has been shown to reprogram visceral adipose tissue to have subcutaneous-like phenotypic behavior, whereas visceral-to-subcutaneous transplantation does not promote a more detrimenta
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br Experimental Procedures Further details
2020-09-18
Experimental Procedures Further details and an outline of resources used in this work can be found in Supplemental Experimental Procedures. Introduction In response to T cell-dependent (TD) antigen stimulation, antigen-specific 4μ8C migrate to the periphery of B cell follicles and interfolli
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br EBV BILF A Virus Encoded TM Receptor with
2020-09-18
EBV-BILF1—A Virus-Encoded 7TM Receptor with Immune Evasive Functions The EBV-encoded BILF1 receptor (EBV-BILF1) is thought to be implicated in the immune evasion strategy of EBV.56, 61, 62 This orphan 7TM receptor is expressed at significant levels during the early lytic phase of the virus infect
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Immunofluorescence assays were performed to localize
2020-09-18
Immunofluorescence assays were performed to localize the enzyme during growth and differentiation to further characterize Giardia E1. As stated before, the assays showed that the β-Pompilidotoxin generated recognized specific E1 forms (E1-114, E1-90 and E1-67 with anti-gNTE1; and E1-47 with anti-gE
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SIRT has deacetylated regulation on
2020-09-18
SIRT1 has deacetylated regulation on numerous nonhistone protein substrates [Atgs, Foxo1, Foxo3, PGC-1α, NF-kB, E2F1 and p53] (Conrad et al., 2016) to play a key role in protecting against cell stress. Therefore, the role of SIRT1 in fluorine-induced oxidative stress was explored. The results reveal
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RLS is a genetically complex
2020-09-18
RLS is a genetically complex disorder in which genetic and environmental factors contribute to the phenotype (Trenkwalder, Allen, Högl, Paulus, & Winkelmann, 2016). This disease is highly familial and six genetic variants with single nucleotide polymorphisms have been identified by genome-wide assoc
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Even though Et modification of DNA delayed the progress
2020-09-18
Even though Et743 modification of DNA delayed the progress of the translocating enzyme significantly, it did not trap RecBCD on DNA, nor did it alter the activity of the enzyme significantly. Under catalytic conditions, no loss of enzyme activity was observed (Table 2), nor were stable unwinding int
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MTX and MTXPGs block the activity
2020-09-18
MTX and MTXPGs block the activity of the key enzyme DHFR (Fig. 1), which converts folates to their active forms – dihydrofolate (DHF) and tetrahydrofolate (THF). MTXPGs also potently inhibit thymidylate synthase (TS). Furthermore, during dTMP synthesis, TS utilizes the cofactor 5,10-methylene THF, w
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Consistent with previous simulations on the DFG
2020-09-18
Consistent with previous simulations on the DFG-Asp-out/-in interconversion of Abl kinase, we only observe the DFG flip with protonated Asp747 (Shan et al., 2009). We showed previously that the pKa for the DFG-Asp in Abl is elevated at 6.5. Further “constant pH” simulations whereby protonation event
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These cytokines except for TGF can
2020-09-18
These cytokines, except for TGF-β can also increase CysLT1R mRNA expression. We further demonstrated that TGF-β and IL-13 were able to increase the proliferation of human BSMC in response to LTD4. BSMC proliferation was CysLT1R-dependent, given that Montelukast ablated this effect. Taken together, o
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