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BAN ORL 24 Recently several Pt IV complexes as prodrugs have
2020-11-03

Recently, several Pt(IV) complexes as prodrugs have been designed and studied to enhance anti-tumor efficacy of traditional Pt(II) drugs, improving their cellular uptake and blood-circulation time [26], [27], [28], [29]. Compared with their Pt(II) counterparts, six-coordinated Pt(IV) complexes with
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HA activates its receptor channels to cause an inward chlori
2020-11-03

HA activates its receptor channels to cause an inward chloride flux in the insect nervous system (Hardie, 1989). Two genes encoding the subunits of these channels were first identified in D. melanogaster: one previously known as ort (also differently named as hclA, DM-HisCl-α1, hisCl2 and Dm HA-Cl
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br When Does Activity with
2020-11-03

When Does Activity with Alternative Substrates Depend on Neutral Drift? In a final scenario, the alternative reaction catalyzed by an enzyme might have no significant (positive or negative) effects on the system fitness, and thus it would be invisible to natural selection and essentially subject
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Early diagnosis of CVS and DCI is a key
2020-11-03

Early diagnosis of CVS and DCI is a key issue in the management of SAH patients. In this regard, CT Perfusion (CTP) is the most accurate and sensitive method for noninvasive imaging assessment of cerebral ischemia with a great value for prediction and early diagnosis of CVS and DCI. CTP is a relativ
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Because of the important role of the DDB CUL B
2020-11-03

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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How does an increase in E affinity for the
2020-11-03

How does an increase in E2 affinity for the RING domain favor higher activity and polyubiquitination by the E2? Binding of the RING domain to the E2 positions the donor Ub in the E2~Ub conjugate in a closed complex [16], [17], [18] that increases the reactivity of the thioester [60]. A higher affini
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Pridinol Methanesulfonate br Methods br Results br
2020-11-03

Methods Results Discussion Preclinical data indicate that nepicastat modulates sympathetic drive to the Pridinol Methanesulfonate with a mild pressor effect in various animal models of hypertension (Stanney et al., 1998). However in this clinical study, the doses of nepicastat employed did
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br Mammalian DGKs current knowledge Despite our understandin
2020-11-03

Mammalian DGKs: current knowledge Despite our understanding of prokaryotic DGKs, our limited understanding of the structure of mammalian DGKs is a major gap in our knowledge. Importantly, major differences exist between prokaryotic and mammalian enzymes often revealing the fact that structural fe
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A putative SHBG receptor SHBG R has been postulated for
2020-11-02

A putative SHBG Tedizolid HCl receptor (SHBG-R) has been postulated for about thirty years [66], [69], [70]. The characterization of this receptor has been researched by several groups. There are different ideas on how this receptor works. On the one hand Fortunati et al. provide evidence that SHBG
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For this reason downstream components
2020-11-02

For this reason, downstream components of the inflammatory pathway have been investigated in the search for alternative targets. Targeting such downstream elements might result in safer and more tolerable analgesics. PGE mediates its effects through binding to four G-protein-coupled receptors (EP1-4
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br Iterative design approach overview An iterative design st
2020-11-02

Iterative design approach overview An iterative design strategy is used to identify a peptidase-resistant reporter that acts as an efficient substrate for kinases in cell lysates as well as intact cells (Fig. 1). In this process, small-scale, rationally designed libraries are used to screen pepti
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As a co factor CIITA lacks the ability
2020-11-02

As a co-factor, CIITA lacks the ability to recognize and directly bind to specific DNA elements to regulate transcription; instead, it relies on interaction with sequence-specific transcription factors (TFs) to be recruited to the chromatin. Therefore, the observation that CIITA binds to a specific
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The enantiomeric ratio ER of chiral compounds
2020-11-02

The enantiomeric ratio (ER) of chiral compounds accumulated in organisms has been found to be different among species (Borga and Bidleman, 2005, Harner et al., 1999, Warner et al., 2005, Wiberg et al., 2000), indicating enantioselective accumulation of chiral compounds are species-specific. The ER o
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br Conflict of Interest br Acknowledgements Marques F was
2020-11-02

Conflict of Interest Acknowledgements Marques F. was supported by the Foundation for Science and Technology (FCT), Portugal, Grant UMINHO/BI/35/2012. This work was supported by FCT by the Project PTDC/AGR-AAM/70418/2006. Introduction β-methylamino-l-alanine (BMAA) exposure has long been as
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It has been shown that DAPK induces cell
2020-11-02

It has been shown that DAPK induces cell death through an increase in DAPK catalytic activity and subsequent phosphorylation of target proteins (Shang et al., 2005, Yamamoto et al., 2002), but its multidomain structure enables also a close physical interaction with other proteins (Bialik and Kimchi,
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