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caspofungin mass The results of bisaryl ether linker study a
2019-09-19

The results of bisaryl ether linker study are shown in . It was found that the methylene linker () moderately improved the binding to the DP receptor. The increased binding potency was also diminished in the presence of plasma, possibly due to higher plasma protein binding. Other linkers, such as th
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br Acknowledgements This work was supported by
2019-09-19

Acknowledgements This work was supported by the European Committee Fifth Framework Project QLK5-1999-01360. We are grateful to Dr. T.T. Hoang for the provision of plasmids pEX18Tc, pPS858 and pFLP2, Prof. B.L. Wanner for providing us with the plasmid pKD4 and related strains, and Prof. P. Soucail
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How does an increase in E affinity for the RING
2019-09-18

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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It is of interest to consider an
2019-09-18

It is of interest to consider an explanation for the apparent phosphorylation of hSSB1 in undamaged cells. One such may be that in order to execute a rapid response to replication inhibition, basal S134 phosphorylation could function to keep hSSB1 in a ‘primed’ state prior to stress. Such an arrange
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DGK is classified into the
2019-09-18

DGKη is classified into the type II DGK subfamily [12], [13], [14], [15]. As described above, DGKη has the splice variants η1 and η2 [10]. DGKs η1 and η2 possess in common a pleckstrin homology domain at the N-terminus and a catalytic domain that is divided into two subdomains (catalytic subdomain-a
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br Experimental procedures br Introduction Protein kinases r
2019-09-18

Experimental procedures Introduction Protein kinases represent one of the largest enzyme ccr5 antagonist in the human genome and act as signaling mediators in a variety of cellular processes (Manning et al., 2002). Because many diseases are associated with aberrant protein kinase activity, ta
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Ligand independent constitutively active variants have
2019-09-18

Ligand-independent, constitutively active variants have also been found in receptors with associated tyrosine kinases. In approximately 60% of patients harboring inflammatory hepatocellular adenomas (IHCAs), these adenomas have been caused by small in-frame deletions in the cytokine-binding domain o
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To assess which export pathway is
2019-09-18

To assess which export pathway is used by the iNOS mRNA, we inhibited CRM1 activity by incubation of DLD-1 PSB 0777 ammonium salt with LMB. Since LMB covalently and exclusively binds to CRM1, it represents a potent and specific inhibitor of the CRM1 transport activity [38]. Inhibition of CRM1 activi
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br Study br Study meta
2019-09-17

Study 1 Study 2: meta-analyses Discussion Ten studies have examined the associations of 5-HTTLPR and COMT Val158Met with alexithymia. However, the findings were mixed. In this study, we found that neither the 5-HTTLPR nor COMT Val158Met is associated with alexithymia. The previous findings
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br Discussion The present study
2019-09-17

Discussion The present study found cholinesterase activity in Saccostrea sp. to vary significantly among three tissue types (digestive gland, gills, adductor muscle) and to respond differentially to four toxicants, three of which were non-organophosphates. Furthermore, a comparison of enzyme acti
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MAPKs are a family of phosphorylating enzymes that
2019-09-17

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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br Chemistry The test compounds listed in Table Table Table
2019-09-17

Chemistry The test compounds listed in Table 1, Table 2, Table 3, Table 4, Table 5, were synthesized as outlined in Scheme 1, Scheme 2, Scheme 3, Scheme 4, Scheme 5. Synthesis of 2–5 is described in Scheme 1. N-Sulfonylation of the aniline 26 with benzenesulfonyl chloride afforded the sulfonamide
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Besides by substrate and product KSTDs
2019-09-17

Besides by substrate and product, Δ1-KSTDs may also be inhibited by other steroids. N. simplex ATCC 6946 Δ1-KSTD was strongly inhibited non-competitively by dicortinone (60), a steroidal dimer, and by bis-1-dehydrodicortinone, with values of 0.7 and 0.75 μM, respectively. This enzyme was also inhib
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DDR is characterized by an N terminal discoidin
2019-09-17

DDR2 is characterized by an N-terminal discoidin domain and a C-terminal kinase domain [7]. Characteristics of DDR1, which is a homologue of DDR2, have been extensively investigated in terms of expression level in cancer tissues and biological functions in normal and cancer cell conditions, but char
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KPT-335 Findings from the present study indicate
2019-09-17

Findings from the present study indicate that CRF1 receptors are especially important in fear acquisition. CP154,526 given before acquisition training, at least partly, reinstated the fear-potentiated startle response and blocked the development of contextual conditioned fear in SERT−/− rats. CP154,
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