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Fencilli et al reported derivatives of
2023-09-14
Fencilli et al. reported derivatives of PHA-680626 (15) which demonstrated strong anti-proliferative activity against large group of leukaemia cell lines including IM-resistant BAF3 cells expressing mutants like T315I, M351T and E255K. Decrease in Histone H3 phosphorylation led to induction of endo-
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There are profound differences between acute
2023-09-14
There are profound differences between acute and chronic pain when dramatic changes occur in peripheral nociceptors and central nociceptive pathways and the pain system is sensitised thereby leading to exaggerated responses to noxious stimuli (hyperalgesia) and responses to non-noxious stimuli (allo
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br Experimental and simulation section br Acknowledgments Fi
2023-09-14
Experimental and simulation section Acknowledgments Financial support for this work was provided by the National Natural Science Foundation of China (No. 81101688). We would like to thank NC State University High Performance Computing Center for providing us computing resources, and Dr. Lihui
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The mitochondrial protein AIF was the first caspase
2023-09-14
The mitochondrial protein AIF was the first caspase-independent death effector. AIF can induce caspase-independent chromatin condensation and large-scale DNA fragmentation to approximately 50 KB. AIF that is released to cytoplasm can mediate apoptosis when special extracellular signals trigger the o
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br Small molecule homoisoflavonoid in combination
2023-09-14
Small molecule homoisoflavonoid in combination with anti-VEGF therapy Basavarajappa et al. [11] reported a new synthetic homoisoflavonoid compound, SH-11037 by modifying the structure of naturally occurring homoisoflavonoid cremastranone. SH-11037 exhibited promising inhibition of human retinal m
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We have recently begun to
2023-09-14
We have recently begun to demonstrate this concept by reporting a novel class of β-hairpin peptidomimetics, built on a piperidine-pyrrolidine semi-rigid β-turn inducer [12] and bearing two recognition pentapeptide sequences, designed on oligomeric and fibril structures of Aβ1-42 (compound 1, Fig. 1)
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br Author contributions br Financial disclosures br
2023-09-13
Author contributions Financial disclosures Acknowledgements We thank Ms. Eva So for the editorial assistance. This work was supported by grants from the National Natural Science Foundation of China (No. 81622015, 81571042 and 81501143) and the National Basic Research Program of China (No. 2
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br Introduction The structural similarities between puromyci
2023-09-13
Introduction The structural similarities between puromycin (1, Fig. 1) and the aminoacyl adenyl terminal of aminoacyl–tRNA allow it to terminate the protein synthesis process by causing premature release of a polypeptide from the ribosome [1], [2]. Tremendous progress in the study of puromycin an
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AKT activity is also self
2023-09-13
AKT activity is also self-limiting through its substrate GSK3β; the kinase activity of which is negatively regulated by AKT phosphorylation (Fig. 3; Li, Liu, & Gao, 2009). GSK3β activation results in phosphorylation and subsequent ubiquitin mediated degradation of PHLPP (Li et al., 2009). AKT activa
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A-1155463 br Introduction Several studies have found
2023-09-13
Introduction Several studies have found that hypothalamic Akt-mediated signaling pathways play critical roles in the regulation of food intake and A-1155463 metabolism in mammals [[1], [2], [3], [4], [5], [6]]. Central injections of the inhibitor of phosphoinositide 3- kinases (PI3 K, an upstrea
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Pregnane X receptor PXR is a
2023-09-13
Pregnane X receptor (PXR) is a nuclear receptor that plays an important role in regulation of metabolism and disposition of structurally diverse xenobiotics as well as endogenous steroids and bile acids (Bertilsson et al., 1998, Kliewer et al., 1998, Lehmann et al., 1998). PXR regulates the metaboli
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Among all the compounds the novel L derivative d showed
2023-09-13
Among all the compounds, the novel L-748,337 derivative (23d) showed the potent human β3-AR antagonist activity and high lipolysis inhibitory activity in vitro. The Methylpiperidino pyrazole 23d displayed 23-fold more potent β3-AR antagonist activity (EC50 = 0.5117 nM) than that of L-748,337 (EC50 =
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Derivatives of M that possess either an alkyne or an
2023-09-13
Derivatives of (+)-M100907 that possess either an alkyne or an azide have been synthesized. The most active enantiomer was obtained by resolution of a relatively early intermediate in the synthesis. The ability of these Bleomycin A5 hydrochloride australia to maintain 5-HTR antagonist properties as
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In model plant Arabidopsis there are myosin XI isoforms
2023-09-13
In model plant Arabidopsis, there are 13 myosin XI isoforms (XI-1, XI-2, XI-A, XI-B, XI-C, XI-D, XI-E, XI-F, XI-G, XI-H, XI-I, XI-J, and XI-K) and 4 myosin VIII isoforms (ATM1, ATM2, VIII-A, VIII-B) [9,13]. Arabidopsis myosin XIs have the common domain composition: a motor domain that interacts with
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For these reasons the role played
2023-09-13
For these reasons, the role played by autophagy in environmental neurotoxicity is not always easily determinable. Indeed, although the neuroprotective role of autophagy has been shown by several studies, sometimes induction of autophagy was associate with deleterious effects (Glick et al., 2010, Sri
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