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Magnetic interactions between metal ions are usually describ
2020-04-02

Magnetic interactions between metal ions are usually described by superexchange via intermediate ligands. Although the general principles of the superexchange mechanism are essentially the same for d and f ions, calculations of exchange parameters for lanthanides are more difficult than for transiti
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We found that E and
2020-04-02

We found that E2 and GEN each has mostly similar effects on recruitment of the epigenetic modulators to the MB-COMT distal promoter (summarized in Table 2). These effects are associated with increased promoter methylation and gene suppression of COMT. It is noted that the array of epigenetic modulat
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br Introduction Vein graft implantation into the arterial en
2020-04-02

Introduction Vein graft implantation into the arterial environment for surgical bypass is the gold standard to treat severe cardiovascular occlusive disease. After placement of a vein into the higher pressure, flow, and oxygen tension of the arterial circulation, the vein adapts to the arterial e
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We next turned our attention to the position
2020-04-02

We next turned our attention to the 6-position of the indole (). It was found that the chlorine atom present in was extremely important. The des-chloro analogue showed nearly 30-fold less affinity for the EP receptor in the binding assay and was nearly 30-fold lower in activity in the functional a
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What are the molecular signals that guide Tfh
2020-04-02

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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br The classical ubiquitination pathway Ubiquitination is an
2020-04-02

The classical ubiquitination pathway Ubiquitination is an enzymatic process that involves the addition of an ubiquitin protein to a substrate that usually becomes inactivated followed by degradation in the proteasome; however, several other functions have also been described. For the discovery of
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Intriguingly one E residue may serve as
2020-04-02

Intriguingly, one E2 residue may serve as a molecular ‘gate’ to allow the C-terminus of ubiquitin to access the closed E2~Ub conformations favorable for ubiquitin transfer. This residue, Asp87 in UbcH5 family members, resides on one side of the opening that leads to the active site Cys (Fig. 4D). In
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DUBs are involved in cell cycle regulation and DNA
2020-04-02

DUBs are involved in axl inhibitor regulation and DNA damage pathways and since, in cancer and different stress conditions all the proteins which regulate cell cycle and DNA damage/repair are either up/down regulated (Singh et al., 2013, Singh et al., 2011, Kumar and de Massy, 2010, Gupta et al., 2
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A second advance came with the discovery that conformational
2020-04-02

A second advance came with the discovery that conformationally-flexible benzamide analogs having an N-phenylpiperazine moiety possessed good affinity and modest selectivity for D3 versus D2 receptors [3,[14], [15], [16]]. This observation spawned a significant effort by medicinal chemists to develop
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Also important in binding of E to the
2020-04-02

Also important in binding of E2 to the ER is the hydroxyl on the D ring, which has a stabilizing contact with His-524 in ERα (Fig. 7) and with His-475 in ERβ (Fig. S1) [8,9,36,37]. The spatial relationship of the functional groups on the A and D rings on E2 has been used to develop chemicals contai
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Hepatocyte proliferation is accompanied by changing gene exp
2020-04-02

Hepatocyte proliferation is accompanied by changing gene expression [1,2]. as two of the three estrogen receptors are transcription factors: Estrogen Receptor alpha (ERα) and ERβ [[3], [4], [5]]. The most potent ligand estradiol, binds to ERα/ERβ and exerts changing cognate gene transcription [5]. O
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Our present data show that neuroleptics can affect
2020-04-01

Our present data show that neuroleptics can affect CYP3A via a direct interaction with the enzyme and a significant indirect mechanism (enzyme regulation) produced in vivo. The obtained results revealed interactions of the neuroleptics (added in vitro to control liver microsomes, Model I) with rat C
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Cy3-UTP mg Published results have revealed relationships bet
2020-04-01

Published results have revealed relationships between serine 81 in AR and some CDKs, especially CDKs 1, 5 and 9 [12], [13], [14], [15], [16]. These results are often supported by pharmacological inhibition of a certain CDK. An effect of CDK1 inhibition on suppression of S81-phosphorylation was previ
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As described above we designed and
2020-04-01

As described above, we designed and synthesized a new 1,4-di-substituted isoquinoline lead compound, and was identified as a ligand with moderate potency for the CRTH2 receptor. We initially we examined the effects of the steric factor of R group on the CRTH2 binding potency (). When the methyl gro
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Crystal structures of various CRM
2020-04-01

Crystal structures of various CRM1 complexes have provided insight into molecular details of the interactions between CRM1 and its interaction partners during the transport cycle. CRM1 cooperatively binds RanGTP and cargo in the nucleus (Paraskeva et al., 1999). In this ternary complex, RanGTP is lo
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