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Besides EGFR other tyrosine kinase receptors are
2021-02-01

Besides EGFR, other tyrosine kinase receptors are currently gaining attention as potential therapeutic targets. Included among these is the fibroblast growth factor receptor (FGFR) family, which is involved in the progression of a variety of cancers.7, 8, 9, 10, 11 In lung cancer, fibroblast growth
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The loss of secondary mutation T
2021-02-01

The loss of secondary mutation T790M mutation after AR and SCLC transformation was also reported for Rociletinib. Piotrowska et al. using the MGH NGS platform recently reported in 13 biopsies among 12 EGFR T790M+ patients progressing after treatment with Rociletinib the loss of EGFR T790M mutation i
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Currently two approaches can be used individually
2021-02-01

Currently, two approaches can be used individually or combinedly to overcome weak immunogenicity of subunit sars-cov (Bookstaver et al., 2018; Moyle, 2017; Vartak and Sucheck, 2016). The first is to design particulate antigens. Virus-like particles (VLPs), for example—mainly derived from the capsid
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Intriguingly one E residue may serve
2021-02-01

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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br Materials and methods br
2021-02-01

Materials and methods Results Discussion We recently detected phosphorylation of tyrosine Y102 in BPV-1 E2 and reported that FGFR3 binds to E2 and limits E1 dependent viral DNA replication (Culleton et al., 2017, Xie et al., 2017). In the current study, we addressed the potential role of ot
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The lack of effective strategies aiming to
2021-02-01

The lack of effective strategies, aiming to directly increase the neuronal survival, is reflected by the fact that the only available therapeutic interventions are indirect. They consist of acute therapeutic interventions involving chemical and/or surgical removal of the thrombotic clot (Taqi et al.
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bmn This pathway appears to have importance in
2021-02-01

This pathway appears to have importance in epilepsy. DGKε(−/−) mice had significantly fewer motor seizure and epileptic events compared with DGKε(+/+) mice [18]. This could be explained by the fact that in the knockout mice a greater fraction of the SAG would be converted to 2-AG. 2-AG itself is kno
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Previous studies showed that many steroidogenic enzymes act
2021-02-01

Previous studies showed that many steroidogenic enzymes act when the enzyme binds to the cofactor first [30]. In the present study, we showed that HPTE inhibited both AKR1C14 and RDH2 in a mixed mode when cofactor was used. This indicates that HPTE interferes with cofactor-binding residues although
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Various domains of DDR have been shown to be
2021-02-01

Various domains of DDR1 have been shown to be important for receptor clustering and its oligomeric status. It is now understood that (i) dimerization [7] and higher-order oligomerization [12], [18] of the DDR1 extracellular domain (ECD) enhance its binding to collagen; (ii) DDR1 exists as non-covale
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br Fragment based drug discovery FBDD
2021-02-01

Fragment-based drug discovery (FBDD) is a powerful method to discover drug leads and has been widely adopted in both academia and industry. FBDD can be used to explore chemical PF 04418948 space with libraries which are smaller in size, producing drug leads with high ligand-binding efficiency. It
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LTD and LTC cause contraction in the rat stomach and
2021-02-01

LTD4 and LTC4 cause contraction in the rat stomach and these contractions are sensitive to CysLT1 receptor antagonists (Goldenberg and Subers, 1983, Miura et al., 1992, Miyata et al., 1995). However, effects of other leukotrienes in the gastric contraction and inhibitory effects of potent, selective
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To determine the time course of ZD P CPG
2021-02-01

To determine the time course of ZD2767P+CPG2 DNA–DNA interstrand cross-link formation, HT29 and LS174T colorectal tumour BIBW 2992 were exposed to the drug for 10, 30 or 60 min. The levels of DNA interstrand cross-links in HT29 or LS174T cells did not increase with exposure time, suggesting that ZD
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The two SNPs rs rs presented above are part of
2021-01-30

The two SNPs rs4818-rs4680 presented above are part of the haploblock (rs6269, rs4633, rs4818, rs4680) presenting the 3 major haplotypes which influence the enzymatic activity of COMT. This activity is inversely related to the sensitivity of pain in a chronic pain syndrome; so the haplotype (GCGG) h
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Evidence for interactions between the endothelin
2021-01-30

Evidence for interactions between the endothelin and the angiotensin system has also become plentiful. It has become clear that the two systems, in addition to acting independently, can act synergistically (Emori et al., 1989, Imai et al., 1992) as well as promote the peptide mRNA expression in endo
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In conclusion our findings suggested that EP receptor activa
2021-01-30

In conclusion, our findings suggested that EP4 receptor activation triggers apoptosis in B-cell lymphoblasts. Our results also showed that EP4 receptor engagement inactivates NF-κB, which, in turn, sensitizes Ramos 98 2 sale to apoptosis induced by chemotherapeutic agents. EP4 receptor agonists are
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