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What are the molecular signals that
2020-03-07

What are the molecular signals that guide Tfh cells as they navigate around the lymph node in the course of the immune response? It was recently reported that Tfh cells inside GCs have high expression of SIPR2, which acts to repel them from the S1P-rich lymph in the SCS and promote their retention i
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Among the Ub interactions observed in the HOIP structure
2020-03-07

Among the ~Ub interactions observed in the HOIP structure is one that involves a RING2 domain (from the non-cognate HOIP) [47]. A similar binding interaction was defined between HHARI RING2 and the hydrophobic patch on Ub by NMR [54]. HHARI RING2 mutations that ablate the interaction inhibit formati
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Through an unknown mechanism RING Ubox type E
2020-03-07

Through an unknown mechanism, RING/Ubox-type E3 dimers and the N-terminal tail have been shown to function as a modulator of full E3 ubiquitin ligase activity [27]. LRSAM1 promotes a significant enhancement in the formation of the high-molecular-weight products or E3 activity when the RING domain is
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E protein was studied using specific anti E antibodies
2020-03-07

E1 protein was studied using specific anti-E1 FK 866 hydrochloride in wild type cells and in transfected cells overexpressing the enzyme. The results revealed several unusual characteristics, which are unique to this ubiquitin-activating enzyme. The E1 was translated as a full-length protein and th
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CaneCPI showed strong inhibitory activity against
2020-03-07

CaneCPI-4 showed strong inhibitory activity against recombinant falcipain-2 and falcipain-3, with IC values of 11.9±0.4nM and 42.3±0.8nM, respectively (Table 1, Supplementary material). Falcipains are involved in hemoglobin cleavage, with generation of two fractions: the heme and the globin. The hem
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A phenylacetic acid derivative discovered in
2020-03-07

A phenylacetic Azidobutyric acid NHS ester derivative (), discovered in a high throughput screen for CRTH2, inhibited the binding of H-PGD to CRTH2 receptors on 293 cells with an IC of 0.010μM, and inhibited the binding of H-PGD to DP receptors with an IC of only 8.3μM (). Compound also inhibited
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br Materials and methods br
2020-03-07

Materials and methods Results Discussion In this study, we investigated two novel candidate therapeutics, the related CRM1-inhibiting SINEs KPT-185 and KPT-276, in treatment of NHL. The results showed that KPT-185 induced growth inhibition, cell-cycle arrest, and apoptosis in tumor BYL-719
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The only reported synthesis of the aminobicyclic core
2020-03-06

The only reported synthesis of the aminobicyclic core of is based on bis-alkylation of a 4-amino-5,6-dihydroxypyrmidine with dibromoethane. The likelihood of poor regiocontrol/reactivity in utilizing such a transformation for the synthesis of compounds with a substituent on the dioxinyl ring led us
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br Dienogest DNG Dienogest is a nortestosterone derivative
2020-03-06

Dienogest (DNG) Dienogest is a 19-nortestosterone derivative with two special structural changes [Fig. 1a]: [a] At the cabon-17 position there is a cyanomethyl group instead of an ethinyl group; [b] A double bond is present between carbons 9 and 10. DNG is the only progestogen that combines prope
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br Physiological roles for EPAC isoforms
2020-03-06

Physiological roles for EPAC isoforms: vascular function The effects of cAMP on limiting vascular endothelial cell (VEC) inflammation and vascular smooth muscle cell (VSMC) proliferation have been well documented 36, 37, 38. However, recent work has demonstrated that several key effects of cAMP i
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br Introduction Cerebral stroke causes an
2020-03-06

Introduction Cerebral stroke causes an efflux of various groups of progenitor and stem cells from bone marrow to bloodstream and the levels of these cells correlate with neurological status of stroke patients (Gójska-Grymajło et al., 2012, 2018). It is thought that paracrine factors produced by t
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Enterobacteriaceae are gram negative rods that include the E
2020-03-06

Enterobacteriaceae are gram negative rods that include the Escherichia coli and Shigella. There are several DNA ligases posted on the GenBank belong mostly to Enterobacteria phages, such as the T4 bacteriophage [30]. There are several protein markers used to differentiate between T4 phage superfamil
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Of the acidic hydroxyazoles involved
2020-03-06

Of the acidic hydroxyazoles involved, hydroxypyrazole had the weakest acidic profile (pKa in the range of 6–7), although highly deprotonated at physiological pH. During hit optimization, the two pyrazole ring positions available for substitution provide an opportunity for a better exploration of the
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We demonstrated that cells expressing less DHODH were
2020-03-06

We demonstrated that Dequalinium Chloride expressing less DHODH were less sensitive to DHODH inhibitors regardless of their oncogenic status. Based on the proliferation speed of cells, Kant et al. (1989), showed that slow-growing squamous cell carcinoma was more sensitive to BQR than fast-growing mu
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Fostamatinib br The DDR kinase domain The DDR intracellular
2020-03-06

The DDR1 kinase domain The DDR1 intracellular kinase domain shares the typical structure of other kinase domains (Fig. 1). However, how DDR1 kinase is activated upon collagen binding is poorly understood. It is thought that the process is fundamentally different from the accepted paradigm of liga
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