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Ryoichi et al modified potent clinical candidate VX with cya
2023-09-25
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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The therapeutic potential of ML
2023-09-25
The therapeutic potential of ML327-induced MET against Meropenem of mesenchymal origin has not been explored. In the present study, we hypothesized that induction of MET using ML327 would block the growth of ES cells and sensitize to TRAIL-mediated apoptosis. Herein, we report that ML327 induces ap
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br Materials and Methods br Results br Discussion XHP is
2023-09-25
Materials and Methods Results Discussion XHP is a traditional Chinese anti-cancer medicine that is widely used for the treatment and adjuvant treatment of breast cancer. XHP has been shown to induce apoptosis in various breast cancer mth1 pathway in vitro, including Hs578T, MCF-7, and MDA-
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It has been reported that trehalose
2023-09-25
It has been reported that trehalose shows beneficial effects in a mouse model of several neurodegenerative diseases [21], [22], [23]. There are also reports showing that trehalose can improve the impaired cognitive and learning ability and reduced Aβ deposit in hippocampus of APP/PS1 transgenic mice
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Cy7.5 NHS ester (non-sulfonated) sale Synaptic scaling up is
2023-09-25
Synaptic scaling up is induced within primary visual Cy7.5 NHS ester (non-sulfonated) sale (V1) by brief sensory deprivation (Desai et al., 2002; Lambo and Turrigiano, 2013). Several studies have examined the transcriptional changes within extracts of V1 following visual deprivation protocols (Lach
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All desired compounds with a carboxylic acid
2023-09-25
All desired compounds with a carboxylic TP-0903 substituent at N1 position of the quinoxalinone scaffold and a variety of aromatic substituents at C3 position were obtained by the syntheses starting from methoxy-substituted 3-chloro-quinoxalin-2(1)-ones () prepared as previously. As shown in , comp
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AhR is also known to cross talk
2023-09-25
AhR is also known to “cross-talk” with a variety of other cell signaling pathways, which has been the focus of a number of recent reviews [40], [41], [42]. It has long been known that TCDD is anti-estrogenic. For example, activation of AhR by TCDD and related HAHs inhibits estrogen dependent uterus
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AdK as an important upstream regulator of adenosine based ho
2023-09-25
AdK as an important upstream regulator of adenosine-based homeostasis represents a promising drug target since it leads to an increase in adenosine concentrations. Taking into account that the adenosine formation is only increased in affected tissues under stress with high adenosine levels, AdK inhi
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br Experimental Procedures br Acknowledgments br
2023-09-23
Experimental Procedures Acknowledgments Introduction Synapses are fundamental units for efficient communication between neurons and their target cells. Despite significant progress in understanding the structure of matured synapses, less is known about the mechanisms by which neurotransmitt
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Molecular docking simulations were carried
2023-09-23
Molecular docking simulations were carried out for ligands – in the ACE crystal structure (1O86) and DPP4 crystal structure (2G5P). Comparison of the binding mode of – () with enalaprilat (a) in ACE shows that the phenethyl group (–, enalaprilat) occupies the S1 pocket and the adjacent carboxylic La
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br Dihydrotestosterone in adult fish and frogs
2023-09-23
Dihydrotestosterone in adult fish and frogs New perspectives and next directions Similar to other androgens, DHT can modulate reproductive endpoints in both fish and amphibians. However, predicting the effects of DHT can be challenging, as reproductive homeostasis is dependent upon the balance
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br Expression of autotaxin in
2023-09-23
Expression of autotaxin in cancer Autotaxin (ATX) is a member of the family of NPPs (Nucleotides pyrophosphatases phosphodiesterases (NPP) family with a unique lysophospholipase D (lysoPLD) activity, allowing the synthesis of LPA from lysophospholipid precursors such as the lysophosphatidylcholin
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NOXA a member of the
2023-09-23
NOXA, a member of the pro-apoptotic B-cell lymphoma 2 (BCL-2) family, plays a vital role in regulating mitochondrial or inherent apoptotic pathways [7,8]. NOXA binds to MCL-1 with high affinity and interacts with A1 (known as BCL2A1), resulting in BIM release to trigger subsequent apoptosis [9]. In
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It was previously demonstrated that dissociation of the V AT
2023-09-23
It was previously demonstrated that dissociation of the V-ATPase in response to glucose depletion in yeast requires an intact microtubular network [28] and a catalytically active enzyme [29]. Interestingly, mutations in the non-homologous region of the catalytic subunit A are able to block dissociat
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As shown in B the recombinant human LOX nM
2023-09-23
As shown in B, the recombinant human 15-LOX-1 (30nM) showed a time-dependent increase in fluorescent signal, and signal development was almost completed within 20min in the presence of 50μM arachidonic Z-WEHD-FMK and 5μM DHR. For both purified enzyme and cell lysates, the enzyme activities disappea
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