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To guide our attempts at achieving AKT potency
2023-01-09
To guide our attempts at achieving AKT potency and selectivity against p70S6K and other kinases from (p70 S6K IC: 0.004 μM) and , we took advantage of exploiting the subtle sequence differences in the active sites of the AGC family kinases, we utilized the information around crystal structure of AK
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Protein blast analysis of the sequence of globin
2023-01-09
Protein blast analysis of the sequence of globin-B with those of other CX4945 suggests that the globin-B domain in the HemAC-Lm displays only 6% identity and 34% similarity with that of cytoglobin/neuroglobin (Fig. 2). Furthermore, SWISS-MODEL protein modeling also predicts that the His311 is the p
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br Actin cytoskeleton in protrusion Pushing
2023-01-05
Actin cytoskeleton in protrusion Pushing force driving membrane protrusion is generated by polymerizing Tamoxifen filaments organized either into branched networks or parallel bundles. Branched networks are assembled through Arp2/3 complex-dependent actin nucleation and drive protrusion of lamel
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br Methods br Results and discussion br Conclusions
2023-01-05
Methods Results and discussion Conclusions Acknowledgements The authors thank Dr. Francois Alhenc-Gelas (then INSERM U367, Paris, France), who kindly provided the plasmid for truncated soluble recombinant human ACE – WTΔ, Dr. Elena Arablinskaya (Institute of Phtiziopulmonology, Moscow, R
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Here we show that the co activation of RTKs and
2023-01-05
Here, we show that the co-activation of RTKs and non-RTKs is a common trait in treatment-naïve EGFR-mutation-positive NSCLC Cyclosporin A and patients, with AXL and CDCP1 being commonly over-expressed. The combination of gefitinib or osimertinib with the Src/FAK/Janus kinase 2 (JAK2) inhibitor TPX-
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Here we report discovery of highly
2023-01-05
Here we report discovery of highly selective pan-Aurora kinase inhibitors through phenotypic screening. The co-crystal structure of Probenecid mg 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.
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It has been reported that Daxx
2023-01-05
It has been reported that Daxx, an interacting partner of MCRS2/MSP58, promotes ASK1 activation following direct interaction with ASK1 [10], [11]. However, it has not been determined whether MCRS2 is involved in ASK1 signalling. In this study, we identified the direct interaction between MCRS2 and A
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l Arginine supplementation was reported to be efficient
2023-01-05
l-Arginine supplementation was reported to be efficient, inefficient or toxic in aged patients. The present study does not support our hypothesis that increased tissue arginase activity may account for the ineffectiveness and even the toxicity of l-arginine supplementation in ageing. Indeed, except
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Derquantel australia br Materials and methods br Results br
2023-01-05
Materials and methods Results Discussion I/R injury is characterized by myocardial damage triggered by the ischemic insult followed by reperfusion injury. While the primary insult depends mainly on the severity and duration of blood flow restriction and the breakdown of ATP-dependent Derqua
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The functions of HMGN protein are
2023-01-05
The functions of HMGN1 protein are modulated by various post-translational modifications, including phosphorylation , , , acetylation , and glycosylation . Phosphorylation in HMGN1 may influence its binding affinity to DNA or nucleosome-associated proteins and affect the sub-cellular localization an
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LDN193189 Hydrochloride In conclusion there are only a few e
2023-01-05
In conclusion, there are only a few experimental reports evaluating the influence of LDN193189 Hydrochloride on allergy. With the exception of studies using macrolides, most point to their harmful effect on the severity of this disease. Future studies will be crucial to define the impact of antibio
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Linagliptin is a recently approved dipeptidyl peptidase DPP
2023-01-05
Linagliptin is a recently approved dipeptidyl peptidase-4 (DPP-4) inhibitor and widely considered as first-line treatment for patients with type 2 diabetes. DPP-4 is responsible for the inactivation of incretin hormones, such as glucagon-like peptide 1 (GLP-1). GLP-1 is released by the intestine af
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The current study was designed to
2023-01-05
The current study was designed to investigate the effects of the 12/15-LOX inhibitor, LOXBlock-1 (LB1) in mice using a FeCl3-induced distal MCAO model, and to test its utility in conjunction with subsequent thrombolysis with tPA, which is to date the only FDA-approved drug for acute stroke treatment
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BITC significantly enhanced the gene expression of the Nrf
2023-01-05
BITC significantly enhanced the gene expression of the Nrf2-dependent genes, such as NQO1 and HO-1 (Fig. 4), as well as the ALDH genes (Fig. 2). Nrf2 is a key transcriptional factor which activates the expression of the genes that contain ARE in their promoter. Nrf2 translocates to the nucleus where
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AKT activity is also self limiting through its
2023-01-05
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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