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p38 pathway Historically covalent drugs have had great succe
2019-08-28
Historically, covalent drugs have had great success (e.g., aspirin and penicillin), and covalent drugs have become a focus in anticancer and antiviral drug discovery (Kalgutkar and Dalvie, 2012, Singh et al., 2011). These compounds contain low reactivity warheads that allow covalent adducts to form
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In summary we hypothesize that
2019-08-28
In summary, we hypothesize that targeting the A1R–D1R heterotetramer with heteromer-selective drugs might improve safety and efficacy of the pharmacological therapy for RLS and other motor diseases, resulting in fewer side effects than classical drugs developed for targeting monomeric A1R or D1R.
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Ligand independent constitutively active variants have
2019-08-28
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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Given the importance of cysteine
2019-08-28
Given the importance of cysteine cathepsin inhibitors as putative therapeutic molecules and microbial virulence factors, we chose to investigate whether Yersinia enterocolitica may be a potent producer of such inhibitors. Y. enterocolitica is the most heterogeneous species within the genus Yersinia.
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For the first time the V carinata transcriptome was
2019-08-28
For the first time, the V. carinata transcriptome was analyzed and its transcript coding sequences comprehensively characterized. The non-redundant contigs encoding putative CysPs were identified and their dna methyltransferase patterns in different tissues were investigated. Our study show that fo
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br Materials and methods br Results
2019-08-28
Materials and methods Results Discussion CDK4 has been identified recently as a potential therapeutic target in human breast cancer, liposarcoma, melanoma, and glioblastoma [[37], [38], [39]]. Due to the importance of CDK4 activity in cancer cells, CDK4 inhibitors have emerged as promising
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In this study we further
2019-08-28
In this study, we further investigated the involvement of CRF1 and CRF2 receptors of the dPAG in the regulation of panic-related responses. For this, we used two animal models that associate escape behavior with panic attacks: the elevated T maze and the electrical stimulation of the dPAG (for a ful
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quercetine br Materials and methods br Results
2019-08-28
Materials and methods Results Discussion Intra-BNST injections of NOC-9 (at all doses) were able to produce freezing and anxiogenic-like effects. Freezing was observed immediately after the NO donor injection and lasted about 2–3min (data not shown). When exposed to the EPM 5min after intra
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br Experimental section br Results br Discussion In
2019-08-28
Experimental section Results Discussion In our previous work (Rashidi et al., 2018) we isolated a novel glucarpidase whose raised Spadin did not cross-react with the one in clinical use. In principle, therefore, it would be possible to delay the production of antibodies in a patient by alte
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The final test that was performed was to
2019-08-28
The final test that was performed was to determine whether the trigger points of the current limiters are stable across a wide temperature range. This test was performed within a thermal-vacuum chamber on each current limiter individually. All the current limiter trip currents were set to approximat
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br Disclosure statement br Acknowledgment This work was
2019-08-27
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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br General mechanism of NHEJ NHEJ
2019-08-27
General mechanism of NHEJ NHEJ is an amazingly versatile pathway that can select specific enzymes which bind to, process, and finally mediate the direct re-ligation of a wide range of DSBs including those that are complex, have incompatible ends, and contain mobile game damages [7], [8], [9], [10
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br Experimental br Results and discussion br Conclusions In
2019-08-27
Experimental Results and discussion Conclusions In this work we presented the direct electrochemical behaviour of the Mo containing formate dehydrogenase, purified from D. desulfuricans, where the Mo centre redox features were observed. The results allowed to calculate the reduction potenti
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Our finding that activating DDR variants are a cause of
2019-08-27
Our finding that activating DDR2 variants are a cause of this disease suggested that the ABL inhibitor dasatinib, a leukemia drug that also inhibits DDR2, could be used for treatment of affected individuals.10, 11 To examine the effect of dasatinib on p.Leu610Pro- and p.Tyr740Cys-induced autophospho
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Recently it was reported that Crm is linked to spindle
2019-08-27
Recently, it was reported that Crm1 is linked to spindle pole body (SPB) by Spc72 in LY2606368 HCl yeast [9]. Spc72 and Spc110 are two specific receptors of γ-tubulin complex (Tub4), which target Tub4 to SPB and mediate the nucleation of microtubules from SPB [20]. It was found that disrupting the
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