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Studies have focused on a hydrophobic cage at the CULT
2020-01-22

Studies have focused on a hydrophobic cage at the CULT domain, conserved from bacteria to mammals, as it binds to substrates and IMiDs (Chamberlain et al., 2014, Lupas et al., 2015). In addition, CRBN ligand-mediated protein degradation was highly conserved, which was confirmed in vertebrates by foc
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In humans several different small ubiquitin
2020-01-22

In humans, several different small ubiquitin-related modifier (SUMO) paralogs can be conjugated to cellular proteins. The human genome codes for five SUMO paralogs (SUMO1–5); of these, SUMO1 and the almost identical SUMO2 and SUMO3 are ubiquitously expressed. Sumoylation is executed by an enzymatic
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Herein we explored by docking studies the effectiveness of r
2020-01-21

Herein, we explored by docking studies the effectiveness of replacing the dimethyl substitution at C (6) of dihydrotriazine with a folded azaspiro-containing substituent, along with the introduction of differently substituted phenyl- and benzyl-rings or alkyl chains, linked at the position 1 of the
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As for antiviral activity eight out of synthesized compounds
2020-01-21

As for antiviral activity, eight out of 23 synthesized compounds were active against influenza B virus with EC50 values in the range of 0.19–39 μM. Four of the eight influenza B hits were active against influenza A and two were also active against RSV (4 and 6, EC50 = 0.40 and 1.8 μM, respectively).
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Multiple protein species are known to naturally exist for th
2020-01-21

Multiple protein species are known to naturally exist for the transmembrane receptors DDR1 and DDR2. Five splice variants have been characterized for DDR1 (“a” through “e”). The d and e isoforms lack the intracellular kinase domain of DDR1. The splicing of DDR1 to various extents has been reported i
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DDR expression is upregulated in the glomeruli and
2020-01-21

DDR1 expression is upregulated in the glomeruli and tubules of injured kidneys [7], [8], [19]; however, what role this receptor plays in kidney resident AS8351 is unclear. A plausible hypothesis is that DDR1 might contribute to kidney injury by directly exerting a pro-fibrotic action. In favor to t
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The molecular mechanism by which CRM regulates IEC
2020-01-21

The molecular mechanism by which CRM1 regulates IEC apoptosis in CD remains to be explored. As an inhibitor of cyclin E-Cdk2, p27kip1 plays a pivotal role in controlling cell proliferation, S phase entry, and G1 phase exit during development and tumorigenesis [38]. As previously reported, p27kip1 i
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So what can we glean from this illuminative foray
2020-01-21

So what can we glean from this illuminative foray into how Chk1 and MK2 participate in checkpoint control? First and foremost, this work reveals that Isochlorogenic acid A australia deficient in the tumor suppressor p53 contain two spatially distinct G2/M phase checkpoint control kinase networks. T
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Schaftoside synthesis Another potential source of variable a
2020-01-21

Another potential source of variable affinities is inherent in the method of RBA determination. While several reports simply use relative IC50 values as RBAs [11], [12], [13], [14], [15], these are only an approximate measure of relative affinity since IC50 varies due to experimental and biological
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br Disclosure statement br Acknowledgment
2020-01-21

Disclosure statement Acknowledgment This work was supported by the National Natural Science Foundation of China (81270704, 81330018). Background Over-expression of cyclooxygenase-2 (COX-2) is common in many malignancies including non-small cell lung cancer (NSCLC) and is associated with po
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At the therapeutic level the logical
2020-01-21

At the therapeutic level, the logical approach to address the cooperation between FGFR4 and EGFR was the combined inhibition of both receptors. To explore the potential efficacy and specificity of this approach, we tested the effect of FGFR and EGFR inhibitors in monotherapy or in combination in syn
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An important role for the
2020-01-21

An important role for the precursor molecule of the main EBI2 ligand, 25-OHC, in the inhibition of inflammation was recently shown. 25-OHC was demonstrated to inhibit inflammasome induction in mouse macrophages [28]. Inflammasome assemblies are the sites of caspase 1 activation and lead to the gener
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The LNX ligand of numb protein X or
2020-01-21

The LNX (ligand of numb protein-X) or PDZRN (PDZ and RING) family of proteins consists of five members (LNX1–LNX5), the first four of which act as E3‐ubiquitin ligases in various roles, as reviewed elsewhere [14]. LNX proteins comprise a RING domain and two to four PDZ (PSD-95, DlgA, ZO-1) domains [
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EphB promotes tumor growth by stimulating angiogenesis
2020-01-21

EphB4 promotes tumor growth by stimulating angiogenesis through EphrinB2 [18]. However, the distinct and specifically involvement of Golgicide A and veins in the tumor angiogenesis of all tumor grades is unclear. Our results indicate that the relation between EphrinB2 and EphB4 stained blood vessel
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LY335979 australia It should also be noted that remarkable i
2020-01-21

It should also be noted that remarkable individual differences in extinguished fear bradycardia (i.e., CS+E vs. CS−E) during initial Day 2 recall test were observed, particularly within Met carriers. Exploratory analyses revealed that these individual differences were partly driven by the level of r
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