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Here we report discovery of highly
2024-05-29

Here we report discovery of highly selective pan-Aurora kinase inhibitors through phenotypic screening. The co-crystal structure of MPI-0479605 bound in the ATP binding site of Aurora A is described, and provides insight into the possible structural basis for the selectivity of the interaction. To
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br Conflict of interest statement br Acknowledgments br
2024-05-29

Conflict of interest statement Acknowledgments Introduction Cellular responses to genotoxic stress in eukaryotic cells are coordinated by members of the phosphoinositide kinase related protein kinase (PIKK) family. Two members of this family, Ataxia–Telangiectasia mutated (ATM) and ATM and
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For the TSH receptor signaling at the
2024-05-29

For the TSH receptor, signaling at the Golgi/trans-Golgi network appears required for both rapid effects of TSH − such as Pracinostat receptor depolymerization, which is implicated in thyroglobulin reuptake and, thus, thyroid hormone release − and late ones, such as those on gene transcription. Con
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These recommendations may be useful for the future to
2024-05-29

These recommendations may be useful for the future to avoid misleading reports and pairings. However, the existing literature can also hold back current research on some given orphans. Before entering into drug development or further physiological conceptual framework, these pairings should be thoro
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br Acknowledgment Supported in part by NIH R
2024-05-29

Acknowledgment Supported in part by NIH1R21EB012707 (Biegon, Anat PI). Introduction Estrogens exert pleiotropic effects on a variety of morphological, physiological and behavioral responses in all vertebrate classes ranging from fishes to mammals. Effects of estrogens in the Azimilide sale c
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CVT 10216 br Experimental br Acknowledgment This paper was f
2024-05-29

Experimental Acknowledgment This paper was financially supported by the Project Funded by China Postdoctoral Science Foundation (2017T100186), Natural Science Foundation of Liaoning Province (20170540858), General Scientific Research Projects of Department of Education of Liaoning Province (20
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br Results br Discussion Cardiac
2024-05-28

Results Discussion Cardiac dysfunction, common complication of severe sepsis, is one cause of death in intensive care units. Accumulated evidence revealed the regulatory effect of autophagy on sepsis-induced cardiac dysfunction [15], [22], although the mechanisms in young and aging are not elu
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Introduction Induction of long term potentiation LTP the cel
2024-05-28

Introduction Induction of long-term potentiation (LTP), the cellular correlate of learning and memory, triggers profound changes in the structure and function of excitatory synapses by increasing dendritic spine size and synaptic strength. Significant progress has been made in understanding the int
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Based on their different sources the APN inhibitors
2024-05-28

Based on their different sources, the APN inhibitors (APNIs) can be divided into the natural products and synthetic compounds. Bestatin (1, Fig. 1), isolated from the Streptomyces oliuoreticuli by Umezawa et al., is the first reported and only marketed natural dipeptidomimetic inhibitor of APN. Afte
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Adiponectin is an adipokine whose circulating
2024-05-28

Adiponectin is an adipokine whose circulating level is depleted in a number of metabolic diseases including insulin resistance, diabetes and cancer (Khan et al., 2015, Singh et al., 2014a, Singh et al., 2014b, Yamauchi et al., 2014). Despite its importance in health and pathophysiology, adiponectin
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The relatively high concentration of HT used in
2024-05-28

The relatively high concentration of 5-HT used in this study (100 µM) is consistent with the concentrations used in other published ex vivo studies (Ropert and Guy, 1991, Passani et al., 1994, Shen and Andrade, 1998). In our paradigm 5-HT was focally applied at the surface of the slice via a fast pe
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br Conflict of interest br Acknowledgements The authors woul
2024-05-28

Conflict of interest Acknowledgements The authors would like to thank Mrs. Amparo Pacheco from CMPL, PUC, for her technical and secretarial assistance. This work was supported by the Fondo Nacional de Desarrollo Científico y Tecnológico (FONDECYT 1150344, 1050377, 11150083), and the Direccioń
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In order to investigate their effects in vitro therefore we
2024-05-28

In order to investigate their effects in vitro, therefore, we first used TE671 cells, which have provided a useful source of human AChR for in vitro and radioimmunoassay studies. We found no marked effect of either MuSK-MG or SNMG sera on AChR numbers or on AChR subunit expression. This appears to c
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An alternative to the agonist or antagonist
2024-05-28

An alternative to the agonist or antagonist potential in drug discovery is the positive allosteric modulator (PAM) approach, which can augment the normal processes of neurotransmission as opposed to directly replacing or antagonizing them. PAMs are thought to bind to sites that are distinct from the
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For some fishstocks landed by FMA ACE
2024-05-28

For some fishstocks landed by FMA3 ACE fishers, the designated Quota Management Area (QMA) extends beyond the geographic demarcations of FMA3.Fig. 1 shows the ten FMAs, highlighting the study area FMA3. Gurnard 3 QMA is included as an example of a QMA that Epibrassinolide extends across more than on
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