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As with most G protein coupled receptors GPCRs sustained
2024-05-06
As with most G protein-coupled receptors (GPCRs), sustained activation of APJ can cause desensitization and this has been reported to occur for APJ-mediated effects on cytoplasmic Ca2+ concentration, as well as for effects on activity of adenylyl cyclase, ERK and Akt (Ishida et al., 2004, Masri et a
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br Future view and implications The selection
2024-05-06
Future view and implications The selection and spread of multi(drug)-resistant microorganisms over the last decades has become a major and global public health concern [35]. Two growing threats originating from the fungal kingdom, i.e. Aspergillus fumigatus and Candida auris[36], [37], re-emphasi
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Tumor tissues often experience hypoxia owing to accelerated
2024-05-06
Tumor tissues often experience hypoxia owing to accelerated growth rates of malignant cells, accumulation of metabolic products, disorganization of tumor blood vessels, and high interstitial fluid pressures (Makino et al., 2001). In response to AAD treatment, tumor vascular density often decreases t
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The loss of synaptic proteins
2024-05-06
The loss of synaptic proteins such as synaptophysin from the Epiandrosterone mg is indicative of synapse degeneration and provided a good correlate of the degree of dementia in AD [12], [13], [14]. Consequently, the loss of synaptic proteins from cultured primary neurons incubated with Aβ provides
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Aldose reductase ALR EC the first enzyme
2024-05-06
Aldose reductase (ALR2, EC1.1.1.21), the first enzyme in the polyol pathway, is a monomeric oxidoreductase that catalyses the NADPH-dependent reduction of a wide variety of carbonyl compounds, especially glucose. In this metabolism pathway, glucose is firstly reduced to sorbitol catalyzed by ALR2 wi
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The binding of TQ to hsALDH changes the characteristic
2024-05-06
The binding of TQ to hsALDH changes the characteristic Eplerenone spectrum of the enzyme. Therefore, TQ forms a complex with hsALDH and changes its absorption properties [39]. Ksv and Kb values indicate that the binding of TQ to hsALDH is very strong and of the order of static binding (complex form
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Princen Panier specifically address the issue of ACE
2024-05-03
Princen, 2012, Panier, 2013 specifically address the issue of ACE using the commercial database AMADEUS. However, both studies focus only on corporate leverage and the ACE in Belgium. Due to the lack of a counterfactual, these authors consider firms in other European countries, e.g., France, as a co
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br LOX in esophageal cancer Various studies suggest
2024-05-03
5-LOX in esophageal cancer Various studies suggest that abnormal levels of AA metabolites play an essential role in human esophageal adenocarcinogenesis (EAC). The key AA derivatives of 5-LOX signaling molecules namely include, 5-HETE, LTB4, and cysteinyl LTs, which are well-known to initiate inf
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The following are the supplementary data
2024-05-03
The following are the supplementary data related to this article. Funding Work in Dr. Rosell's laboratory is partially supported by a grant from La Caixa Foundation, and an Instituto de Salud Carlos III grant (RESPONSE, PIE16/00011). Work in Dr. Cao's laboratory is partially supported by the Maj
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In order to further explore whether the cytoprotective effec
2024-05-03
In order to further explore whether the cytoprotective effect of isogarcinol against oxidative stress in H2O2-induced HepG2 PJ34 receptor is a consequence of the breakdown of the endogenous antioxidant defence mechanism, we measured the LDH release, MDA levels, GSH levels and SOD activity. A large
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To further demonstrate the significance of Nrf activation in
2024-05-02
To further demonstrate the significance of Nrf2 activation in the prevention of EGF-induced CRC growth by AR inhibitor, we examined the effect of fidarestat on EGF-induced cell viability in Nrf2-ablated cells. Our results suggest that AR inhibitor prevented the EGF-induced cell viability in control
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In the late s Solvay Pharmaceuticals discontinued the Phase
2024-04-30
In the late ‘90s, Solvay Pharmaceuticals discontinued the Phase 2 development of a promising potent and highly selective A1AR antagonist based on the pyrrolopyrimidine scaffold, SLV320 [43] (2, Chart 1, also named derenofylline; Ki hA1AR = 1 nM), for the treatment of acute heart failure [24]. In the
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where is the breaking force
2024-04-30
where is the breaking force. In the following, the details of the simulation are presented and subsequently, the results are discussed. The initial atomic structure is extracted from the crystal structure of single AF (PDB identification 3G37) which consist 12 monomers. As aforementioned 4 monomer
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A high throughput small molecule ACK biochemical inhibition
2024-04-30
A high-throughput small molecule ACK1 biochemical inhibition screen was performed in-house and led to the identification of 1μM inhibitor furanopyrimidine (). Further binding studies found Asiatic acid australia to be both ATP-competitive and reversible. Early structure-activity relationship (SAR) w
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In these experiments recordings were performed continuously
2024-04-30
In these experiments, recordings were performed continuously in the homecage and during the first 5 days of training on a randomized forced alternation T-maze working memory task (Figures 1A, 1B, 3A, and 3B) (Kucewicz et al., 2011). Sleep and wake states were determined by simultaneous recording of
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