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To date more than different mutations
2023-04-26
To date, more than 50 different mutations in the gene have been described (Human Gene Mutation Database at the Institute of Medical Genetics in Cardiff: SRD5A2 Gene: http://www.hgmd.cf.ac.uk). Most of them are missense mutations but premature stop codons and deletions leading to non-functional or su
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Since the localization of LO depends on phosphorylation we a
2023-04-26
Since the localization of 5-LO depends on phosphorylation, we also analyzed the phosphorylation profile of 5-LO-WT and all isoforms by Western blot using specific (+)-Usniacin against the phosphorylation sites S271 and S523. Whereas phosphorylation at S271 activates the 5-LO, inhibits nuclear expor
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In young animals the HT A receptor antagonist ketanserin at
2023-04-26
In young animals, the 5-HT2A LB42708 antagonist ketanserin, at relatively low concentrations, shifted 5-HT concentration-response curves rightward, suggesting a role for 5-HT2A receptors in mediating 5-HT-induced contractions of the ureter. The slopes of the ketanserin Schild plots for the antagoni
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Finasteride has been shown to
2023-04-26
Finasteride has been shown to be a mechanism-based inhibitor of 5AR-2 [9]. Finasteride acts as an alternate substrate for 5AR-2 and is initially bound in an extremely stable enzyme-bound NADP-dihydrofinasteride adduct which is ultimately processed to dihydrofinasteride. The NADP-dihydrofinasteride a
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br Autophagy at the Synapse The synapse
2023-04-26
Autophagy at the Synapse The synapse is a highly specialized neuronal compartment that forms the basic unit of communication between neurons. Communication relies on electrical signals that are propagated down the axon of the presynaptic neuron, where they trigger the quantal release of neurotran
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In this review we will present
2023-04-25
In this review, we will present the traditional and actual strategies to study orphan receptors and identify their ligands. An extensive description of the orphan GPCR field has been published in 2013 by Davenport et al. [22]. Therefore, we will focus on the deorphanizations that were reported since
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Receptor Subtypes and Their Function
2023-04-25
Receptor Subtypes and Their Function – Critical Appraisal Largely unselective ligands of the benzodiazepine binding site, such as diazepam, are known to elicit a wide range of in vivo effects including hypnosis, sedation, anxiolysis, and muscle relaxation. Genetically modified mice were introduced
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The mechanism governing how mechanotransduction signals
2023-04-25
The mechanism governing how mechanotransduction signals regulate a number of genes involved in cartilage hemostasis remains unclarified. Mitogen-activated protein kinase (MAPK) pathways are activated by static and dynamic compression of cartilage (31 32). c-Fos/AP-1 is downstream of the MAPK pathway
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br Results and discussion The soil fungus PSU
2023-04-25
Results and discussion The soil fungus PSU-RSPG37 (BCC56870) was isolated from soil samples collected from Rajjaprabha Dam, Suratthani Province, Thailand. The fungus was deposited at BIOTEC Culture Collection, National Center for Genetic Engineering and Biotechnology (BIOTEC), Thailand Science Pa
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Mirtazapine Introduction Inflammasomes are large cytosolic p
2023-04-25
Introduction Inflammasomes are large cytosolic protein complexes with multiple components that trigger a rapid immune response against pathogen-associated molecular pattern Mirtazapine (PAMPs) during pathogen infections or damage-associated molecular pattern molecules (DAMPs) during tissue damage
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Based on the observation that
2023-04-25
Based on the observation that antipsychotic drugs increase 5-HT1A–D2 heteromerization level (Łukasiewicz et al., 2016), we set out to compare the effect of paroxetine to that of risperidone. Paroxetine, a potent SSRI, is very effective in the treatment of depression and anxiety disorders, e.g., gene
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Earlier studies revealed an interaction between HSP and ACK
2023-04-25
Earlier studies revealed an interaction between HSP90β and ACK1 [15]. In the proteomic approach, we show that ACK1 associates with HSP90α and HSP90β. Additionally, we confirm the existence of a HSP90-ACK1 complex with co-IP experiments. We further analysed whether an inhibition of HSP90 affected the
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The results show that a tonic action
2023-04-25
The results show that a tonic action of ACh on respiration is lacking. However, it is clear that muscarinic cholinergic mechanisms can modulate both eupneic breathing and the cough reflex. When these mechanisms are brought into action is obscure and only tentative proposals can be advanced. ACh in t
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Direct inhibition of LO activity by BRP is clearly evident
2023-04-25
Direct inhibition of 5-LO activity by BRP-187 is clearly evident in cell-free assays using PMNL homogenates and isolated human recombinant 5-LO as enzyme source. In such assays, pure FLAP inhibitors like MK886 are inactive [9], [10], [29], [44]. Wash-out experiments and studies using the nonionic de
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Several dehidropregnenolone derivatives functionalized at C
2023-04-25
Several 16-dehidropregnenolone derivatives functionalized at C3, C4, C5 and C6 (Fig. 7) were prepared and evaluated as 5α-reductase inhibitors bearing in mind that after the formation of an enzyme-steroid complex a nucleophilic portion of the enzyme attacks the double bond of the steroid through Mic
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