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Ryoichi et al modified potent
2023-03-01

Ryoichi et al. modified potent clinical candidate VX-680 (6) with 3-cyano-6-(5-methyl-3-pyrazolamino)pyridine as Aurora kinase inhibitor. Substituted cyano pyridine derivative (7) inhibited proliferation of HCT-116 cells with an IC50 value of 115 nM. It showed tumor inhibition in mice model at a dos
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Ryoichi et al modified potent
2023-03-01

Ryoichi et al. modified potent clinical candidate VX-680 (6) with 3-cyano-6-(5-methyl-3-pyrazolamino)pyridine as Aurora kinase inhibitor. Substituted cyano pyridine derivative (7) inhibited proliferation of HCT-116 cells with an IC50 value of 115 nM. It showed tumor inhibition in mice model at a dos
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br Concluding remarks and future perspectives While the
2023-02-25

Concluding remarks and future perspectives While the rational engineering of protein-based switches has yet to be fully developed, emerging empirical rules facilitate the construction of tailor-engineered dpat with custom input and output parameters. Both in the context of molecular diagnostics a
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In addition unconventional mechanisms of internalization can
2023-02-25

In addition, unconventional mechanisms of internalization cannot be ignored. It is generally believed that the conventional homologous internalization of a GPCR depends on the activation of G proteins, since GRK activation requires the pre-activation of G proteins (Fig. 2). Feng et al. demonstrated
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WZ4003 The zinc transporter proteins are members of the
2023-02-25

The zinc transporter proteins are members of the SLC superfamily of metal transporters, and comprise two structurally and functionally different groups, the zinc-importer (ZIP; Zrt-, Irt-like proteins) family (SLC39A), which regulate zinc transport into the cytoplasm from outside the cell and from i
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br Conclusion br Conflicts of interest br
2023-02-25

Conclusion Conflicts of interest Introduction Alzheimer’s disease is the most common neurodegenerative condition known to cause dementia (Ferri et al., 2005). Alzheimer’s dementia typically presents with initial recent episodic memory deficits, word finding difficulty and later with apraxia
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br AHR mediates TCDD toxicity
2023-02-25

AHR mediates TCDD toxicity and wasting syndrome TCDD causes numerous toxicities in laboratory animals, including teratogenesis, hepatic steatosis, thymic atrophy, immune dysfunction and a lethal wasting syndrome [17]. The dose-dependent sensitivity to TCDD-induced toxicities varies widely among l
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As we previously observed in the
2023-02-25

As we previously observed in the NSFT (Fukumoto et al., 2014), the effect of LY341495 in the FST was also inhibited by a 5-HT1A receptor antagonist, indicating the role of the 5-HT1A receptor in the actions of LY341495. Among the 5-HT1A receptors, which exist both presynaptically and postsynapticall
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mdm2 p53 Tension within the network could be
2023-02-25

Tension within the network could be explained by two potential mechanisms: the more classical contractility that is dependent on motor proteins that are pulling mdm2 p53 filaments towards each other [10]; or contractility that is caused by disassembly of a crosslinked network of actin filaments [2]
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Sperm total motility and hyperactivated
2023-02-25

Sperm total motility and hyperactivated motility are mediated by PLD-dependent caspofungin australia polymerization [20]. Reduction of PIP2 synthesis inhibited actin polymerization and motility, and increasing PIP2 synthesis enhanced these activities. Furthermore, sperm demonstrating low motility c
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br Funding This work was supported by Arena
2023-02-25

Funding This work was supported by Arena Pharmaceuticals, Inc, San Diego, CA, USA. Introduction 5-hydroxytryptamine 1B (5-HT1B) receptors are widely distributed in the central nervous system (CNS); they have various modulatory functions in drug reinforcement, appetitive behaviors, stress, moo
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Acknowledgments br P c is expressed in several steroidogenic
2023-02-25

Acknowledgments P450c17 is expressed in several steroidogenic tissues, including the adrenal cortex, the ovary, and the testes (). Thus, 17α-hydroxylase/17,20-lyase is a key enzyme required for the production of both cortisol and sex steroids. This enzyme defect blocks the synthesis of cortisol,
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Normally the activity of the lyase
2023-02-25

Normally, the activity of the 17,20-lyase increases with the onset of adrenarche [7], [8], [15]. Adrenarche has previously been perceived as a relatively sudden event, occurring physiologically between 6 and 8years of age. However, results from our laboratory clearly indicated that adrenarche is a c
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Cyclic di-GMP mg br Discussion br Acknowledgments Writing
2023-02-24

Discussion Acknowledgments Writing of this review and collection of data from our laboratories that are presented were supported by a grant from the Belgian Science Policy (BELSPO) SSTC Interuniversity Attraction Poles Plastoscine P7/17 to AVDL and JB, multiple grants from the Fund for Scienti
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ldk378 Previously we have detected the
2023-02-24

Previously, we have detected the expression of APJ receptor on stomach projecting ldk378 in DMV, in addition, icv administration of apelin-13 induced a remarkable c-Fos activation in those cells which were previously marked by a retrograde neuronal tracer fast blue (Birsen et al., 2016). Moreover,
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