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GANT 58 receptor We have expressed the ECDs of
2024-04-17

We have expressed the ECDs of the human α1, β1, γ and ɛ AChR subunits in the past using the methylotropic yeast Pichia pastoris as soluble glycosylated proteins [15], [16]. Further work with the γ subunit ECD revealed a marked improvement of the solubility and yield following the mutation of hydrop
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Inhibitors of mPGES are considered as safe alternative to NS
2024-04-16

Inhibitors of mPGES-1 are considered as safe alternative to NSAIDs in the treatment of chronic inflammatory diseases that are characterized by excessive PGE2 production (Bahia et al., 2014; Khurana and Jachak, 2016; Koeberle et al., 2016; Korotkova and Jakobsson, 2014; Norberg et al., 2013; Psarra e
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An AXL decoy receptor with enhanced
2024-04-16

An AXL decoy receptor with enhanced GAS6-binding properties, MYD1, was engineered as a therapeutic tool to disrupt GAS6/AXL signaling in vivo (Kariolis et al., 2014). MYD1 was shown to block metastasis of human ovarian cancer nicotinic acetylcholine receptor and a murine breast cancer cell line in g
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Materials and methods br Results br Discussion ATX plays a
2024-04-16

Materials and methods Results Discussion ATX plays a significant role in initiating and sustaining tumor metastasis [43]. LPA stimulates cell proliferation, migration and survival by acting on its cognate G-protein-coupled receptors. Aberrant LPA production, receptor capivasertib and signali
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Over the past decade extensive
2024-04-16

Over the past decade, extensive research has been directed toward the discovery of Aurora-selective small-molecule inhibitors. As a result, a handful of Aurora inhibitors has been identified. Among them, 1 (VX-680) and 2 (SNS-314) have entered human clinical trials as pan-Aurora kinase inhibitors (F
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ATM dependent initiation of radiation induced G
2024-04-16

ATM-dependent initiation of radiation-induced G2/M checkpoint arrest is well established [11], [34], [35]. However, the ATR pathway may also be involved [36], [37]. Brown and Baltimore generated Cre/lox-conditional cell lines or taurolidine with a kinase inactive allele of ATR (ATRkd) to evaluate t
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br Materials and method br Results br Discussion Although se
2024-04-16

Materials and method Results Discussion Although several studies have showed the crude extracts of K. senegalensis possessed the anti-inflammatory and hypertensive activities (Olayinka et al., 1992). However, the anti-inflammatory effect and underlying molecular mechanisms of its bioactive
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The subnuclear localizations of redox regulators is also
2024-04-16

The subnuclear localizations of redox regulators is also largely unknown. The potential role of thiol reductases as transcription regulators or DNA repair molecules may suggest an association to DNA. In this way, the presence of a zinc finger domain potentially involved in protein/DNA interactions o
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br Future directions outlook Peptide based macrocycles are a
2024-04-16

Future directions-outlook Peptide-based macrocycles are among the privileged scaffolds in antibiotic drug discovery. Many compounds were discovered by natural product screening and developed unchanged, or as semi-synthetic derivatizations. Since the golden age of antibiotic discovery (1940s-mid 1
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The electrokinetic remediation technique is carried out with
2024-04-16

The electrokinetic remediation technique is carried out with a low-level direct current, and the pollutants in soil can be transported and removed by the electric field [19]. This works well even in soil with low permeability via electro-osmotic flow and electro-migration [20]. The electrokinetic pr
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Fish aminopeptidases from Alaska Pollack roe
2024-04-16

Fish aminopeptidases from Alaska Pollack roe and tuna pyloric caeca have been reported on [12,13]. More recently, we described the purification of a leucine aminopeptidase from the skeletal muscle of the common carp [14], red sea bream [15] and a lysine aminopeptidases from Japanese flounder [16]. T
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Regarding the HT B receptors they act
2024-04-15

Regarding the 5-HT1B receptors, they act as terminal receptors and are involved in the presynaptic regulation of the release of 5-HT. But at spinal level these receptors are principally situated post-synaptically (Sari, 2004). The ability of autoreceptors to regulate extracellular levels of 5-HT dur
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HT receptors are distributed throughout the brain
2024-04-15

5-HT3 receptors are distributed throughout the brain, within the brainstem (e.g., nucleus tractus solitarius, area postrema and spinal trigeminal nucleus) and AMG-208 australia (e.g., hippocampus, amygdala, nucleus accumbens, putamen and caudate) (Abi-Dargham et al., 1993, Barnes et al., 1989, Buft
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The same applies also to intermediate formally obtained by e
2024-04-15

The same applies also to intermediate , formally obtained by elimination of the R substituent from compound . If compared to the thienopyrimidine derivatives (series , C), the thieno[3,2-]pyridazin-5(4H)-ones – explored herein seem to maintain similar size and shape and also analogue structural char
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A more versatile cellular delivery
2024-04-15

A more versatile cellular delivery system for adenosine was generated by engineering mouse embryonic stem cells to lack both muscarinic receptors of Adk (Fedele et al., 2004). Using a step-wise differentiation protocol (Okabe et al., 1996) Adk−/− ES cells were differentiated into transplantable ade
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