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The typical pharmacophore for GPR agonists contains four par
2021-12-20

The typical pharmacophore for GPR40 agonists contains four parts: head (acid moiety), central (phenyl ring), linker and tail (aromatic carbocyclic or heterocyclic ring) [20]. On the other hand, the chemical features that are required for the PPARγ agonists include hydrogen bond donors and acceptors
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On the contrary the benzhydrol series
2021-12-20

On the contrary, the benzhydrol series showed modest activity with EC of two digit micromole. The bulkiness of the SID 26681509 tail may be the reason for the low activity. Interestingly, introduction of H-bonding groups, such as OMe in and CF in , slightly improved the activity compared to the un
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br Promotion of GLS expression Glutamine metabolism is anoth
2021-12-20

Promotion of GLS2 expression Glutamine metabolism is another target for alteration in ferroptosis. Glutamine is required for the induction of ferroptosis during serum-induced injury after amino CP 31398 dihydrochloride australia starvation [72]. The first step of glutamine catabolism is its conve
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In this study we evaluated and
2021-12-20

In this study we evaluated and compared the kinetics and duration of the oral and systemic HPV-16 and HPV-18 specific antibody response to three doses of the qHPV vaccine in mid-adult aged HIV+ men from the AIDS Malignancy Cohort (AMC) 052 trial and mid-adult aged HIV− men from the Mid-Adult Male [M
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br Hippo pathway signalling The Hippo pathway is an
2021-12-20

Hippo pathway signalling The Hippo pathway is an evolutionarily conserved signal transduction pathway regulated by cell-cell contact, cell polarity, mechanical cues, ligands of G-protein coupled receptors, and cellular biotin-LC-LC-tyramide sale status [10]. This pathway is linked to development
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Recent studies have indicated that HDAC and
2021-12-18

Recent studies have indicated that HDAC and BRD4 are associated with similar biological phenotypes related to cancer and combination of the HDAC inhibitor LBH589 and BET inhibitor I-BET151 synergistically induces apoptosis of melanoma cells [20], [21]. Moreover, combination of Panobinostat and (+)-J
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GSTs have been originally named ligandins
2021-12-18

GSTs have been originally named ‘ligandins’ because of their capacity to bind large ligand molecules (of molecular weight >400 Da) (Oakley et al., 1999). At least three separate mol calculator have been reported for xenobiotics within the H-site; only one is for CDNB (Ralat and Colman, 2004). Usual
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br Endogenous and synthetic ligands
2021-12-18

Endogenous and synthetic ligands of GPR55 There are currently limited commercially available synthetic agonists and antagonists that are specific for GPR55. A large number of studies have investigated the pharmacology of GPR55 4, 23, 25, 30, 31, 32, 33, 34, 35, with contradictory findings reporte
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In summary our findings support
2021-12-18

In summary, our findings support the hypothesis that activation of GPR55 protects against deficits in neurogenesis induced by inflammatory insult both in vitro and in vivo through direct targeting of NSCs. Better understanding of the mechanisms by which GPR55 provides neuroprotection is critically n
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One previously unreported discovery is that Ptgds is alterna
2021-12-18

One previously unreported discovery is that Ptgds is alternatively spliced, such that partial removal of exon 3 correlates with higher levels of regeneration. The absence of exon 3 likely affects the functionality of the final product. The structure of Ptgds is that of the typical lipocalin β-barrel
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Cichlasoma dimerus as most teleost fish species present
2021-12-18

Cichlasoma dimerus, as most teleost fish species, present neurons expressing GnRH3 (Pandolfi et al., 2005). As in most Doxorubicin species, the neurons expressing GnRH3 are mainly located in the NOR, although few neurons were detected in the olfactory bulb, ventral telencephalon and the POA (Gonzál
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Morin is a flavonoid that has shown
2021-12-18

Morin is a flavonoid that has shown to have effective anti-inflammatory and anti-tumor function [118]. Morin was able to block the activation of NF-κB pathway by ROS and inflammatory cytokines, preventing a signaling cascade resulting in cell death [121]. Morin exerted its control over the signaling
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diacerein synthesis br Methods br Results br Discussion
2021-12-18

Methods Results Discussion In this series of studies we hypothesized that FHH-GHSRm1/Mcwi rats would, relative to their WT counterparts, exhibit a metabolic and behavioral phenotype reminiscent of GHSR−/− mice. Through the use of the GHSR−/− mouse, a great deal about the role of ghrelin sig
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Optimization of the tetrahydroindazole series led to the dis
2021-12-17

Optimization of the tetrahydroindazole series led to the discovery of two moderately potent γ-secretase modulators, 2-cyclobutane and 2-hydroxy-2-methylpropane which were subsequently evaluated in a kinetic aqueous solubility assay. Unfortunately, neither analog demonstrated improved solubility ()
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4SC-202 mg It has been shown that mice
2021-12-17

It has been shown that mice lacking SMAD2 in T cells do not develop spontaneous lymphoproliferative autoimmunity (Malhotra et al., 2010). Further, FOXO1 is known to activate proinflammatory MCP-1 and IL-6 (Ito et al., 2009). To this end, we also validated the downstream target FOXO1 and SMAD2 after
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