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EBI remains an orphan GPCR and the identity
2020-02-10
EBI2 remains an orphan GPCR and the identity and source of its ligand are yet to be described. Molecular studies of EBI2 have suggested that this receptor has constitutive activity, similar to that observed for many herpesvirus-encoded 7TM receptors (Benned-Jensen and Rosenkilde, 2008, Rosenkilde et
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br Materials and Methods br Acknowledgements We thank the st
2020-02-10
Materials and Methods Acknowledgements We thank the staff of beamlines ID29 and ID30A-1 of the European Synchrotron Radiation Facility. This work was supported by, the Marie Curie Career Integration Grant (PCIG13-GA-2013-630755), the Israel Science Foundation (Grant 1383/17) and the Israeli Ca
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Verapamil a calcium channel blocker used clinically as
2020-02-10
Verapamil, a calcium channel blocker used clinically as a coronary vasodilator, was amongst the first compounds identified that could reverse MDR and potentiate the effects of MDR1 substrates such as vincristine [15], [16]. Verapamil, along with a number of other MDR1 blockers, have proved largely u
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Traditionally serum triglycerides have been measured in the
2020-02-10
Traditionally, serum triglycerides have been measured in the clinic in the fasted state in order to reduce variability and also to facilitate the calculation of LDL-cholesterol via the Friedewald equation, which was derived using fasted samples (Warnick and Nakajima, 2008). We have previously report
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Each of the CYP enzymes
2020-02-10
Each of the CYP450 enzymes alluded to above are highly selective catalysts, in that, the three aryl coupling reactions en route the biosynthesis of 1 are catalyzed by three different CYP450 enzymes in a sequential manner (Fig. 1). In sharp Cy5 NHS ester (non-sulfonated) is the recently described ma
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Furthermore in silico physicochemical characters
2020-02-08
Furthermore, in silico physicochemical characters and pharmacokinetic parameters for the synthesized compounds were predicted using dedicated computer software [34], [35], [36] to ensure successful in vivo therapeutic activity. Practical logP testing was performed and compared to the theoretical val
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Both the kK and kK mediated ubiquitination
2020-02-08
Both, the kK3 and kK5-mediated ubiquitination leads to rapid internalisation of target proteins followed by lysosomal degradation, similar to that seen for MARCH-1/8 [77]. Ubiquitination activity of kK3 and kK5 depends on the positioning of the targeted lysine (or cysteine) residues [22]. The positi
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It has been reported that vernolic
2020-02-07
It has been reported that vernolic Avasimibe accumulation in transgenic Arabidopsis seeds expressing a Δ12-epoxygenase often resulted in failure of germination and impaired growth and development (Singh et al., 2001). Similar phenomena were also reported for transgenic Arabidopsis seeds with accumu
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One of the therapeutic proteins used in cancer therapy is
2020-02-07
One of the therapeutic proteins used in cancer therapy is glucarpidase, also known as Carboxypeptidase G2, CPG2, which originates from the bacterium Variovorax paradoxus (old name, Pseudomonas sp. strain RS-16). It has no mammalian equivalent (Thompson et al., 1994; Kamlage, 1994) and is a zinc-depe
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Recently a method for in vivo photoactivation of cells expre
2020-02-07
Recently, a method for in vivo photoactivation of Epibrassinolide expressing PA-GFP in precise microanatomical compartments was described (Victora et al., 2010), which makes it possible to optically mark Tfh cells and track them 20 hr later (Shulman et al., 2013). Unexpectedly, it was reported that
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The second DDR binding partner identified here
2020-02-06
The second DDR1-binding partner identified here, Shp-2, which was not found in the two-hybrid screen but using a bioinformatics approach, is also a mediator of cell migration. Since Shp-2 has two SH2 domains, as well as phosphotyrosine phosphatase enzymatic activity and two C-terminal tyrosines targ
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Lately using receptor TM peptides BiFC and PLA experiments
2020-02-06
Lately, using receptor TM peptides, BiFC and PLA experiments, we have also obtained experimental evidence for the tetrameric structure of A1R–D1R, which explains the canonical interaction on Gi and Gs, respectively (Fig. 2). We have demonstrated for the first time the presence of this heterotetramer
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Therefore HNE is an attractive therapeutic target and
2020-02-05
Therefore, HNE is an attractive therapeutic target and the design of new HNE inhibitors is a demanding field that has been extensively investigated in order to provide inhibitors with new molecular architectures, including the potent oxo-β-lactam class [14]. In the present work, a coumarin-based oxo
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RO 4929097 Muscle Ring Fingers MuRFs comprising TRIM MuRF TR
2020-02-05
Muscle Ring Fingers (MuRFs) comprising TRIM63 (MuRF1), TRIM55 (MuRF2) and TRIM54 (MuRF3) are the most studied TRIMs in the heart. However, with increasing knowledge of E3 ligases and recent advancements in the field, many other TRIMs such as TRIM8, TRIM21, TRIM24, TRIM32, TRIM45, TRIM69 and TRIM72 w
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It is conceivable however that the distortion induced by ado
2020-02-05
It is conceivable, however, that the distortion induced by adozelesin in dsDNA may decrease the processivity of the translocating RecBCD enzyme so that it dissociates more frequently from adducted DNA relative to unmodified DNA. Premature termination from the DNA would also produce partially unwound
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