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Several main strategies for targeting
2019-10-12
Several main strategies for targeting E3s described in the literature include: in vitro screening using functional assays [86]; computer programs for predicting potential druggable pockets, including those at protein-protein interfaces, and subsequent docking-based in silico ligand screening [87]; f
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Predictions of enzyme topology for
2019-10-12
Predictions of enzyme topology for DGAT2 are more difficult since the DGAT2 polypeptide sequences are more diverse across species than those of DGAT1. The length and function of the hydrophilic N-terminus preceding the first hydrophobic segment varies with species – for example, segments in fungi ar
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br Experimental br Results and discussion br Conclusions In
2019-10-12
Experimental Results and discussion Conclusions In this work we presented the direct electrochemical behaviour of the Mo containing formate dehydrogenase, purified from D. desulfuricans, where the Mo centre redox features were observed. The results allowed to calculate the reduction potenti
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Introduction The term myeloproliferative disorders was first
2019-10-12
Introduction The term “myeloproliferative disorders” was first proposed by William Dameshek in 1951. With the discovery of the Philadelphia chromosome, myeloproliferative disorders were classified into two groups: BCR-ABL positive chronic myeloid leukemia (CML) and BCR-ABL negative chronic myelopr
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br Materials and methods br Results br
2019-10-12
Materials and methods Results Discussion In our tissue array, we demonstrated that 14-3-3 tau mRNA and protein expression levels decreased in the preeclamptic placentas. 14-3-3 proteins are considered to be important in the functional regulation of trophoblasts and maybe associated with adv
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The collagen field undoubtedly regains attractiveness with t
2019-10-12
The collagen field undoubtedly regains attractiveness with the emergence of new concepts (cell niche, regulation of growth factor bioavailability, mechanotransduction, cell microenvironment sensing) and new tools to investigate their in vivo functions (atomic force microscopy (AFM), second harmonic
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br Introduction Cell transplantation therapies using
2019-10-12
Introduction Cell transplantation therapies using embryonic stem cell (ESC) and induced pluripotent stem cell (iPSC)-derived retinal tissue (ESC/iPSC retina) or fluorescent probes have emerged as therapeutic options for retinal degeneration following recent breakthroughs. A number of groups have
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Given the potency enhancing effect of
2019-10-12
Given the potency enhancing effect of the 4--butyl group, this substitution was incorporated into the Eastern portion of the molecule for further SAR investigations (). Removal of the phenol group (SR19822) or moving it from the -position to the -position (SR19552) or led to significant loss of acti
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In mammals ribonucleotide reductase RNR
2019-10-12
In mammals, ribonucleotide reductase (RNR) is a unique enzyme that catalyzes the rate-limiting step of de novo synthesis of deoxyribonucleoside triphosphates (dNTPs).7, 8 Mammalian RNR consists of two homodimer subunits: the large catalytic dimer RRM1 and the small regulatory dimer RRM2 or RRM2B. An
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br Materials and Methods br Results br Discussion
2019-10-12
Materials and Methods Results Discussion The spatial properties of receptor-ligand interactions can influence receptor activation and signal propagation, but studying this phenomenon requires the development of systems capable of recapitulating complex biophysical traits. In this study, we
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To study systemic potential of the
2019-10-12
To study systemic potential of the selected compounds as EP1 receptor antagonist, they were evaluated with regard to the sulprostane-induced increase of intravesical bladder pressure in rats. Some of the analogs, 13 and 15–17, which were selected on the basis of their in vitro EP1 receptor affinity,
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In some cases more than one CYP enzyme may
2019-10-12
In some cases, more than one CYP450 enzyme may be involved in the metabolism of a drug, and an Eadie–Hofstee plot is usually more reliable for assessing the involvement of multiple Bromhexine HCl (Bu, 2006). Therefore, we first plotted the Eadie–Hofstee curves and observed their shape to determine
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In all available E E structures the RING type
2019-10-12
In all available E2:E3 structures, the RING-type domain binds the E2 on a surface that is remote from the active site Cys (and therefore from the ubiquitin thioester) (Fig. 2). The non-contiguous E3-binding and active sites on the E2 imply that the role played by a RING to facilitate ubiquitin trans
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Programmed cellular death or apoptosis is a process genetica
2019-10-12
Programmed cellular death or apoptosis is a process genetically controlled that plays an important role in cellular homeostasis, being an important defense mechanism to remove cells that have been infected, damaged or mutated (Smith and Smith, 2012, Wlodkowic et al., 2011). Nevertheless, apoptosis s
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MoAbs targeting the tumourigenic pathways such as
2019-10-11
MoAbs targeting the tumourigenic pathways, such as IGF-1R may theoretically have a dual working mechanism. On the one hand they block pathways having an anti-tumour working mechanism, and on the other hand they may also stimulate an immunological response inducing a reaction of the patients own immu
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