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androgen receptor inhibitor First of all two assumptions jus
2020-11-27

First of all, two assumptions just as in Ref. [30] are need to simplify the penetration process: (1) The crater phases is short and the androgen receptor inhibitor of EFP is consumed little; thus, the influence of crater on penetration can be ignored; (2) the initial stagnation radial pressure is e
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br Materials and methods br Results br
2020-11-27

Materials and methods Results Discussion PKA and Epac are two principal effector proteins involved in cAMP signaling; they are expressed in a wide range of tissues and control diverse biological functions [10]. The existence of two cAMP effectors provides more precise regulation of cAMP sig
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Preliminary studies suggest that dimerization of the
2020-11-27

Preliminary studies suggest that dimerization of the AT1 receptor occurred during the biosynthesis in the endoplasmic reticulum before surface expression [27,40], which may explain the presenece of these Droxinostat before the addition of any ligand. Our results showed that the presence of Ang II d
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Several studies on the collagen
2020-11-27

Several studies on the collagen receptor DDR1 have revealed a defined collagen signaling pathway that causes cell scattering and cadherin switching. As mentioned earlier, DDR MM-102 receptor on collagens are distinct from integrin binding sites; therefore, the same collagen protein can bind to DDR
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Results from experiments in model systems have suggested
2020-11-27

Results from experiments in model systems have suggested that the DPRs translated from the HRE of C9ORF72 are toxic and play a role in disease pathogenesis (reviewed in Taylor et al. (2016)). Although the DPRs are present in neurons and glia in various regions of the central nervous system (CNS) ear
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In our study the TIP P model is applied for
2020-11-27

In our study, the TIP3P model is applied for water, AMBER99sb force field [24] is used to describe three types of EGFR, including the wild type (PDB: 2ITY) [25], its mutant G719S (PDB: 2ITO) [25] and mutant T790M (PDB: 3IKA) [26]. The force field of Tubemoside molecule is parameterized with optimize
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br Materials and methods br Results and discussion br Confli
2020-11-27

Materials and methods Results and discussion Conflict of interest Acknowledgments This work was supported by grants from National 973 Project (2015CB755700) and the Doctoral Starting up Foundation of Henan University of Science and Technology (13480033). Introduction Progression thro
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EPZ015666 synthesis br Results br Discussion Our UbV library
2020-11-27

Results Discussion Our UbV library was originally designed to develop inhibitors of deubiquitinases (Ernst et al., 2013). Recently, we showed that UbVs could exhibit multiple binding modes and mechanisms to modulate HECT E3 activity (Zhang et al., 2016)—one set occupied the HECT domain E2-bind
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br Materials and methods br Results br Discussion
2020-11-27

Materials and methods Results Discussion Structural analysis of dnmt3 sequences of different ploidy fish cloned in this study showed high similarities to zebrafish sequences, which also contained a unique N-terminal motif and a calponin homology (CH) domain, a conserved proline-tryptophan-t
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Of the acidic hydroxyazoles involved hydroxypyrazole had the
2020-11-27

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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The compounds were ranked based on the Glide
2020-11-26

The compounds were ranked based on the Glide XP Score, as shown in . All 15 compounds were subject to a radiometric assay previously used in our lab to evaluate their ability to inhibit DHFR steady-state activity in recombinant TS-DHFR (A). Compound demonstrated greater than 50% inhibition of DHFR
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CYP s are heme containing monooxygenases constituting a
2020-11-26

CYP450s are heme-containing monooxygenases constituting a conserved gene superfamily of heme-thiolate proteins, and are found in prokaryotes and eukaryotes (Martignoni et al., 2006). They play a key role in detoxification of endogenous (e.g., steroids) and exogenous compounds (e.g., drug, insecticid
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Deregulated Wnt signaling either due
2020-11-26

Deregulated Wnt signaling, either due to pathway mutations or otherwise aberrant pathway activity, is common in CLL [81], [82]. In addition to targets described above, alvocidib also inhibits glycogen synthase kinase 3 (GSK3)-β at higher nanomolar concentrations [37]. Despite intuition and experimen
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R co localizes Golgi marker GM Fig Our metabolic pulse
2020-11-26

R co-localizes Golgi marker GM130 (Fig. 5). Our metabolic pulse-chase studies carried out in the presence of CSF-1 exposed the newly synthesized CSF-1R to its ligand, which promoted its rapid degradation. While this was clearly seen in control BMDMs, the mature band of CSF-1R remained intact for the
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Based on the ability of CRF to modulate
2020-11-26

Based on the ability of CRF to modulate nociception, we hypothesized that stress leads to hyperalgesia by the activation of CRF1 and/or CRF2 receptors in the spinal cord. We tested this hypothesis using an acute forced swim as a widely used and easily reproducible stressor and grip force as a measur
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