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br Ubiquitin Capture by the
2020-04-21
Ubiquitin Capture by the Mobile APC11 RING Domain Contributes to Processive Substrate Ubiquitylation Although the rules of Ub-mediated proteolysis are only beginning to emerge, the rate and order in which different APC/C substrates are degraded during the SecinH3 synthesis correlates with proces
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In glioblastoma methylation of pMGMT is predictive of
2020-04-21
In glioblastoma, methylation of pMGMT is predictive of the efficacy of temozolomide with an increased survival [22], [23], [24], [25]. As in glioblastoma [24], [26], [27], [28], pMGMT methylation assessed by pyrosequencing (with immunochemistry, IHC) is the most effective and reproducible technique
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br Discussion Our data demonstrate that the bicyclam AMD
2020-04-21
Discussion Our data demonstrate that the bicyclam AMD3100 strongly interacts with CXCR-4, whereas DS and AR177, two other compounds that also interfere with virus entry into the po1 (and interfere with virus binding), do not. AMD3100 is a unique compound in that it interferes with the chemokine r
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MLN 2480 synthesis Our structures also provide new insights
2020-04-21
Our structures also provide new insights into CRTH2 drug development. The ligand binding pocket revealed by our structures comprises many aromatic residues and a few polar residues at the distal end. Correspondingly, most CRTH2 antagonists share a similar structural feature characterized by an aceta
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The in vitro cytotoxicity of
2020-04-21
The in vitro cytotoxicity of the prodrugs was assessed in the LS174T human colon cell line (). The results were found to reflect the stability of the prodrugs, with the unstable urea compounds ( and ) giving relatively poor cytotoxicity differentials between prodrugs and parents (i.e., approximately
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br Materials and Methods br Results
2020-04-21
Materials and Methods Results Discussion Viral infection of eukaryotic 3-Bromopyruvic acid activate signaling pathways both via specific interaction with pattern recognition receptors (TLRs, RIG-I, MDA5) and more nonspecific mechanisms such as accumulation of newly synthesized viral glycop
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Since the aggregation of neurotoxic forms of A
2020-04-20
Since the aggregation of neurotoxic forms of Aβ plays a pivotal role in AD pathogenesis, an approach that using small molecules to bind Aβ monomers and prevent their assembly into cytotoxic oligomers attracts great interest for the development of AD drugs. Therefore, the potential inhibitory activit
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br Conflicts of interest br Financial support
2020-04-20
Conflicts of interest Financial support NZ is an Established Investigator of the Dutch Heart Foundation (2013T111) and is supported by an ERC Consolidator grant (617376) from the European Research Council and by a Vici grant from the Netherlands Organization for Scientific Research (NWO; 91818
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The BMP family comprises significant growth factors
2020-04-20
The BMP family comprises significant growth factors for the regeneration of bone and cartilage. Among these, BMP- has been known as an early marker during the proliferation of osteoblast cells, and one of the most potent stimulators of osteoblastic cells differentiation [40]. Studies with COX-2 knoc
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br Conclusion The role of DNA PK
2020-04-20
Conclusion The role of DNA-PK target in DNA DSB repair renders this 961 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 pote
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The fibrillogenesis process of collagen is understood to
2020-04-20
The fibrillogenesis process of collagen is understood to initiate in the extracellular space near the plasma membrane where secretory vesicles form regions of deep invagination. However, it is not clear how and when collagen-binding proteins interact with collagen molecules during fibrillogenesis or
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The cysteinyl leukotrienes cysLTs LTC LTD and LTE are increa
2020-04-20
The cysteinyl leukotrienes (cysLTs) LTC, LTD, and LTE are increased in the airways of asthmatic subjects, with the ability to induce bronchoconstriction, vascular permeability, and mucus secretion., , , , CysLTs are well established as mediators of allergic rhinitis and asthma on the basis of the e
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MAPKs are a family of phosphorylating
2020-04-20
MAPKs are a family of phosphorylating enzymes that orchestrate various cellular response in proliferation, apoptosis, inflammation, stress response, and energy metabolism [11]. There are at least four major members including extracellular signal-regulated kinase 1 and 2 (ERK1/2), p38 mitogen-activat
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The interface between the E ligase
2020-04-20
The interface between the E3 ligase and the E2 enzyme can vary, and ZNF451 and SP-RING ligases stabilize this interaction via noncovalent binding to a scaffold SUMO (SUMOB) on the backside of the E2 (Cappadocia et al., 2015; Eisenhardt et al., 2015; Streich & Lima, 2016). By contrast, RanBP2 does no
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PF-8380 mg Although many GPCR heteromers have been identifie
2020-04-20
Although many GPCR heteromers have been identified using heterologous cell lines, only very few fit all three criteria. This is mainly due to the difficulties to study these structures in native tissues because of the lack of sensitive and selective tools, not only capable of detecting in vivo evide
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