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In our preliminary evaluation of this series we
2020-06-03
In our preliminary evaluation of this series, we were surprised to discover that arginase inhibitor was found to bind CSF-1R in a classical DFG-in binding mode (a). Dramatic conformational differences in the juxtamembrane domain and activation loops are apparent when this DFG-in structure is compa
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The mammalian two hybrid results
2020-06-03
The mammalian two-hybrid results described above were all obtained in 293T cells, and thus the higher RLU observed specific to the hCrm1 fusion could be consistent with human AS 101 having an unknown activator that interacts with hCrm1 HEAT repeat 9A and somehow facilitates Crm1-Rev/RRE function. Al
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br Introduction Breast cancer is the most common cancer in
2020-06-03
Introduction Breast cancer is the most common cancer in women and one of the leading causes of death worldwide. Estrogen receptor alpha (ERα, “wild-type” estrogen receptor), encoded by the estrogen receptor1 (ESR1) gene, is expressed in approximately 70% of all breast cancers. Hormonal therapy ha
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br Materials and methods br Results and discussion br
2020-06-03
Materials and methods Results and discussion Conclusions The fabrication and characterization of AMCs reinforced with SiC and RHA was done in this study. Following conclusions are drawn from the above study: Conflict of interest Authors\' contributions Introduction Industrialisati
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Similarly in the EAE model Chalmin et al previously demonstr
2020-06-03
Similarly in the EAE model, Chalmin et al. previously demonstrated that EBI2 and CH25H might be responsible for the efficient egress of differentiated Th17 cells from the draining lymph nodes [31]. As discussed above, in active EAE we did not find differences in EAE development and only the transfer
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GLP also showed cardioprotective effects i
2020-06-03
GLP-1 also showed cardioprotective effects (i.e., infarct size reduction and ejection fraction improvement) in experimental models of myocardial ischemia-reperfusion injury by suppressing caspase-3 activation and preventing apoptosis of cardiomyocytes [[50], [51]]. Of note, such a cardioprotection w
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For example nM MTX markedly stimulates the differentiation o
2020-06-03
For example, 200nM MTX markedly stimulates the differentiation of the monocytic U937 Riociguat [39], but only 10nM MTX is sufficient for the inhibition of clonogenicity in the ALL and APL cell lines [22]. Furthermore, an even lower concentration of MTX (2nM) selectively induces the expression of p2
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DDR is one of two non integrin tyrosine
2020-06-02
DDR1 is one of two, non-integrin tyrosine kinase receptors activated by collagen. Although DDR1 has five isoforms (1a, 1b, 1c, 1d, 1e) generated by alternative splicing, only DDR1a and 1b have active kinase domains, whereas DDR2, encoded by a distinct gene, has one isoform (Vogel et al., 2006). Coll
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Of the acidic hydroxyazoles involved hydroxypyrazole had
2020-06-02
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 thank Dr Hongqiang Qin at Dalian Institute of
2020-06-02
We thank Dr. Hongqiang Qin at Dalian Institute of Chemical Physics, Chinese Academy of Sciences for technical assistance in mass-spectrometric analysis. We thank Prof. Quentin Liu at Dalian Medical University and Prof. Qiang Shen at M.D. Anderson Cancer Center for helpful discussion and comments. Dr
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Hymenialdisine the most potent inhibitor of parasite TgCK en
2020-06-02
Hymenialdisine, the most potent inhibitor of parasite TgCK1 enzymes in vitro has no whole cell anti-parasitic activity (Table 2). Like purvalanol B however, this AZD2858 also displays poor activity against target enzymes in cultured cells. For example, in vitro IC50 values for inhibition of CDK5/cy
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ERR and ERR share high sequence
2020-06-02
ERRα and ERRγ share high sequence homology at their DNA binding domain (98% identity) and bind response elements in a similar fashion (Fig. 3 and Liu et al., 2005), yet ERRγ shows high variability in its capacity to stimulate the different response elements, whereas ERRα does not (Fig. 6A). For exam
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br Material and Methods br Results and Discussion br Conclus
2020-06-02
Material and Methods Results and Discussion Conclusions Two chemical coupling agents, BTDE and CDI, were used to activate the free hydroxyl groups of plant cellulose powder and OPH from Flavobacterium ATCC 27551 immobilized on modified carriers by covalent linkages. The highest immobilizati
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The question arises as to
2020-06-02
The question arises as to how the massive conformational changes determining whether APC/CCDC20–MCC is inhibited or able to catalyze MCC ubiquitylation are naturally controlled? This transition likely involves APC/C regions near the subunit APC15, because reducing cellular APC15 levels stabilizes MC
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The other scenario pertaining to the significance of H AX
2020-06-02
The other scenario pertaining to the significance of H2AX phosphorylation is based on the fact that the initiation of DNA fragmentation by CAD facilitates the chromatin condensation that occurs concurrently [15]. Apoptotic DNA fragmentation and chromatin condensation are important for the efficient
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