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Prostaglandin E receptor subtype EP is a
2020-12-17
Prostaglandin E receptor subtype 4 (EP4) is a transmembrane G-coupled protein receptor activated by prostaglandin E2 (PGE2). EP4 activation exerts anti-inflammatory effects in adipose tissue by dampening the levels of inflammatory chemokines [12]. In the mouse, EP4 deficiency aggravates fragmentatio
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The Liver X Receptor and LXRs NR H and
2020-12-17
The Liver X Receptor-α and -β (LXRs, NR1H3 and NR1H2, respectively) are members of the nuclear receptor superfamily that play a central role in controlling cholesterol homeostasis [9], [10]. In macrophages, LXRs can decrease the cellular sterol burden by inducing expression of the cholesterol efflux
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Eptifibatide br Transparency document br Acknowledgements We
2020-12-17
Transparency document Acknowledgements We thank Prof. Barbara Brodsky for valuable comments and discussion. We thank the support of the Tufts start-up fund and the Knez Family Faculty Investment Fund for Y.-S. L, and the Tufts Summer Scholar program for E.C. Introduction Discoidin domain r
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br Materials and methods br Results
2020-12-17
Materials and methods Results Discussion Studies have suggested that the Hh signaling pathway, which plays as an essential autocrine viability factor for MFBs [10], [11], is a potential therapeutic target for liver fibrosis. Previously reported works have proven the effectiveness of the Hh
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EBI and its ligand s EBI
2020-12-16
EBI2 and its ligand(s) EBI2 was found in a screen of upregulated genes in human B cells upon infection with EBV [1]. EBI2 is a G-protein (Gαi type) coupled receptor [2] but as long as 18 years after its discovery the nature of its ligand remained undisclosed. With the help of transfected cell lines
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Because of the important role
2020-12-16
Because of the important role of the DDB1-CUL4B interaction for CUL4B-based E3 ligases, disruption of the DDB1-CUL4B interaction could be an effective approach to treat cancer. Therefore, we developed an in vitro HTS assay based on yeast cell growth inhibition to identify compounds that could disrup
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Intriguingly one E residue may serve as
2020-12-16
Intriguingly, one E2 residue may serve as a molecular ‘gate’ to allow the C-terminus of ubiquitin to access the closed E2~Ub conformations favorable for ubiquitin transfer. This residue, Asp87 in UbcH5 family members, resides on one side of the opening that leads to the active site Cys (Fig. 4D). In
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br Conclusion In the last year significant advances in our
2020-12-16
Conclusion In the last year, significant advances in our understanding of ubiquitin transfer by IAPs and related E3 ligases have been made. The three crystal structures of the RING-bound E2~Ub show that the conjugate is bound by the RING domain in the closed conformation, where the I44-centered f
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The first hint that GLP might not be
2020-12-16
The first hint that GLP-1 might not be completely stable came from a meeting abstract in 1992, reporting that GLP-1 could be degraded in plasma incubations [16], although the enzyme(s) involved was not identified. A year later, Mentlein and colleagues [17], in a search for peptide substrates of the
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br Conclusion The role of DNA
2020-12-16
Conclusion The role of DNA-PK target in DNA DSB repair renders this Oleandrin kinase of great medicinal interest in cancer chemotherapy especially the cancer types of linked to DNA defects. Due to the absence of 3D DNA-PK target structure, different ligand-based methods were applied for design of
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In this paper we describe a facile and universal method
2020-12-16
In this paper, we describe a facile and universal method for in situ crosslinking of DNA micelles, using spherically directed reduction of metal ions. As shown in Scheme 1A, a single-stranded DNA (ssDNA) consisting of a ligand domain, a template domain, and a lipid domain was designed as a monomer t
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The overall shape of p
2020-12-16
The overall shape of p110α/iSH2 is dramatically different from DGKB or SK1, instead of forming a homodimer, p110α/iSH2 heterodimer has a triangular shape with iSH2 laying on the top and ABD, RBD, helical and kinase domain of p110α sitting in the bottom (Fig. 2B) (Gabelli et al., 2010; Huang et al.,
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The preferences for source of FAs for DGAT and DGAT
2020-12-16
The preferences for source of FAs for DGAT1 and DGAT2 are related to their membrane topologies, subcellular locations, interactions with other proteins or organelles (discussed in the former section), and their differential expression, substrate specificities, and enzyme kinetics. According to UniPr
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The death associated protein kinase DAPK is an
2020-12-16
The death-associated protein kinase (DAPK) is an actin-associated, calcium/calmodulin-dependent enzyme with serine/threonine kinase activity [11], [12]. DAPK is a pro-apoptotic gene and participates in various apoptotic systems, such as TNF-α- and Fas-triggered apoptosis [10], IFN-γ-induced cell dea
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br Acknowledgement This research was supported by a grant fr
2020-12-16
Acknowledgement This research was supported by a grant from the National Research Foundation of Korea (NRF-2013R1A1A2011238) funded to Young-Mi Lee. Introduction Stroke is considered a serious disease with high morbidity and high mortality. More than 6 million deaths are reported each year wo
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