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BMS 309403 In the context of E ligase drug discovery it
2020-06-29
In the context of E3 ligase drug discovery, it is critical to identify the appropriate E2/E3 substrate pairing to ensure the development and use of the most physiologically relevant screening assay. There have been many reports of limited E2/E3 activity profiling with a small number of E2 and E3 BMS
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Introduction The number of patients with type
2020-06-29
Introduction The number of patients with type 2 diabetes is increasing globally, and has become a serious public health problem. Type 2 diabetic patients exhibit a higher risk of bone fracture [1]. In addition, clinical studies have indicated that increased fracture risk is associated with long-ter
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However one major challenge will be to understand how the
2020-06-29
However, one major challenge will be to understand how the diverse actions of D2Rs in multipartite, dopamine-sensitive circuits are coordinated to produce specific behaviors across species. It is possible that emerging techniques for imaging neuronal activity in different neuronal population in beha
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During the past three decades platinum
2020-06-29
During the past three decades, platinum-based DNA-alkylating agents have been employed in the treatment of various cancers [14]. Oxaliplatin is currently used as a first-line treatment for colorectal cancer (CRC) [15]. Unfortunately, a large portion of CRC patients receiving oxaliplatin-based chemot
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Collectively the results presented here provide new
2020-06-28
Collectively, the results presented here provide new insights into ligand binding, clustering, spatial distribution, and phosphorylation of DDR1b and DDR2 in response to soluble collagen I. As depicted in the cartoon of Scheme 1, we postulate a model in which the spatial distribution and assembly of
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Some mechanistic experiments performed in
2020-06-28
Some mechanistic experiments performed in the early 2000s by Ongusaha et al. [78], suggest that DDR1 induction protects Physcion from apoptosis in a p53-dependent manner, and that impairment of DDR1 expression or function leads to a pronounced increase of DNA damage-induced apoptosis. This evidence
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The authentic PPase was purified from B subtilis as
2020-06-28
The authentic PPase was purified from B. subtilis as described previously [21], whereas the recombinant enzyme was purified to homogeneity from E. coli by a simplified procedure including only phenyl-Sepharose CL-4B column chromatography and DEAE-HPLC [21]. About 26 mg of pure enzyme was obtained fr
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Although the crystal structures of Atg C
2020-06-28
Although the crystal structures of Atg4C and Atg4D are not available, their three dimensional structures can be acquired by homology modeling, using the structure of Atg4B as a template (Zhang, Li, Ouyang, Liu, & Cheng, 2016). In that model, the catalytic triad is conserved (Cys110/Asp345/His347 for
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br Disclosure and conflicts of interest br Acknowledgements
2020-06-28
Disclosure and conflicts of interest Acknowledgements This research was supported by grant (BT/PR/11293/BRB/10/849/2008) from Department of Biotechnology (DBT), Government of India and a DST YOS Chair Professorship to PB. The mass spectrometry facility is supported by an institutional program
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It should be noted that the long lifetime
2020-06-28
It should be noted that the long-lifetime binding-responsive luminescence of ARC-1528 and ARC-1530 becomes evident only upon illumination with radiation at near-UV range where the excitation of ATB or ASB moiety is possible. At higher wavelength range (visible light), the fluorophore (5-TAMRA) can b
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br Materials and methods br Results br Discussion The
2020-06-28
Materials and methods Results Discussion The main finding of the present study is that selective ETA and dual ETA/ETB receptor blockade markedly improve endothelium-dependent vasodilatation in patients with type 2 diabetes and vascular complications. The magnitude of improvement did not dif
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br Criteria for ER targeted fluorescent probes
2020-06-28
Criteria for ER-targeted fluorescent probes Survey of fluorescent probes Proposed approach to high affinity fluorescent steroidal ER probes Our proposed approach to the development of a new generation of fluorescent estrogen receptor imaging agents employs many of the elements present in th
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It is well established that a number of intracellular signal
2020-06-28
It is well established that a number of intracellular signaling pathways mediate sensitization of sensory neurons (Gold and Gebhart, 2010, Richardson and Vasko, 2002). This redundancy could be advantageous since it provides diversity in initiating and maintaining hypersensitivity in response to inju
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We continued to investigate the contribution of
2020-06-28
We continued to investigate the contribution of the EP1 AG957 to nociceptive sensitization by utilizing its natural ligand PGE and tested the effect of local subcutaneous injection of PGE (5nmol in 5μl) into one hindpaw on mechanical and heat pain thresholds. Wild-type mice displayed maximum sensit
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Docking experiments showed that Me MeGlcA Xyl and
2020-06-28
Docking experiments showed that Me-MeGlcA3Xyl4 and MeGlc3Xyl4 were bound to EcXyn30A and the R293A variant in the same way as MeGlcA3Xyl4, having MeGlcA or its modified forms accommodated in the -2b subsite. All ligands were coordinated by the same bradykinin receptor antagonist and no new interact
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