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The gene SRD A encodes the reductase
2024-11-19

The gene SRD5A2 encodes the 5-α-reductase enzyme, which converts testosterone into dihydrotestosterone. Although dihydrotestosterone levels are considerably lower than testosterone, dihydrotestosterone has a five-fold stronger binding capacity to the androgen receptor and, thereby, a considerably mo
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Thirty six of the analogs synthesized showed ATX
2024-11-19

Thirty-six of the analogs synthesized showed ATX inhibition greater than 50% at 10μM with FS-3, twelve of which had improved potency over the lead (Fig. 5). Of these, 22 was sub-micromolar (IC50 670nM). The 3,5-dichlorophenoxy ring of 22 is reminiscent of the 3,5-dichlorophenylthiourea ring in Hoegl
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It has recently been reported that
2024-11-19

It has recently been reported that plasma and synovial fluid levels of autotaxin correlate with severity of knee OA. Synovial fibroblasts isolated from OA patients express significant amounts of autotaxin mRNA, and this increase in autotaxin etomoxir could lead to increased production of LPA, sugge
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The inhibition of ACLY induces an anticancer effect that
2024-11-19

The inhibition of ACLY induces an anticancer effect that has been reported to be involved in mitochondrial reactive oxygen species (ROS) generation [14], [16], dual blockade of mitogen-activated protein kinase and phosphatidylinositol-3-kinase/AKT pathways [11], and the glycolytic phenotype of tumor
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br Materials and methods br Results br Discussion Many
2024-11-19

Materials and methods Results Discussion Many studies investigate the role of 12/15-LOX in cancer cell,23, 24, 25 however we here first found that host 12/15-LOX also plays an important role in metastasis progression. We have demonstrated that 12(S)-HETE increased melanoma cell adhesion to
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Although TP status has been
2024-11-19

Although TP53 status has been shown to play a role in ATR inhibition and platinum resistance [7], [27], [38], in inhibition of ATM and sensitivity to IR [39], and in the activation of Chk1 and Chk2 [3], [4], ATM and ATR signaling can occur through the p38MAPK/MK2 pathway in p53-deficient N-acetyl D-
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In order to further explore whether the cytoprotective
2024-11-19

In order to further explore whether the cytoprotective effect of isogarcinol against oxidative stress in H2O2-induced HepG2 Disuflo Cy5 azide 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 la
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Our surprising results show that AAD treated
2024-11-19

Our surprising results show that AAD-treated tumors adjacent to adipose tissues and in steatotic liver continue to grow in the presence of a minimal number of microvessels. In non-adipose tumor models, the similar degree of vascular suppression is translated into marked suppression of tumor growth.
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Introduction Alzheimer s disease AD is
2024-11-18

Introduction Alzheimer's disease (AD) is a complex neurological disorder characterized by a progressive dementia resulting from synapse failure (Selkoe, 2002, Tanzi, 2005). The amyloid hypothesis maintains that the pivotal event in AD is the production of amyloid-β (Aβ) peptides following the prote
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Furthermore to address the concern that the observed
2024-11-18

Furthermore, to address the concern that the observed positive in vitro activity results might be stymied by the propensity of such assays to display false positives due to the inherent noxiousness of the tested compounds, all analogs were evaluated against Vero cells in an MTT assay. Some of the mo
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Recently two distinct small molecule
2024-11-18

Recently, two distinct small-molecule inhibitors of PHGDH were identified using high-throughput screens, both of which inhibit de novo serine biosynthesis and show selective toxicity to cancer Brilliant Blue G mg with high SSP flux [50,51]. The inhibitor NCT-503, which has an IC50 of 2.5μM, reduces
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As we previously observed in the NSFT Fukumoto et
2024-11-18

As we previously observed in the NSFT (Fukumoto et al., 2014), the effect of LY341495 in the FST was also inhibited by a 5-HT1A receptor antagonist, indicating the role of the 5-HT1A receptor in the actions of LY341495. Among the 5-HT1A receptors, which exist both presynaptically and postsynapticall
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br Experimental procedure br Funding The
2024-11-18

Experimental procedure Funding The present study was supported by the Grant Russian Foundation for basic research (project no. 16-04-01517). Introduction 5-HT, a monoaminergic neurotransmitter, is synthesised from l-tryptophan catalysed by the enzymes tryptophan hydroxylase (Tph) and aroma
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Nutritional factors affecting ASD have also recently
2024-11-18

Nutritional factors affecting ASD have also recently received attention. An increase in postsynaptic zinc (Zn) level induced by clioquinol (a Zn chelator and ionophore), and the subsequent activation of NMDA receptors through the tyrosine kinase Src, rescued social interaction in Shank2−/− mice (Lee
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We also investigated the transmittance of actin polymerized
2024-11-18

We also investigated the transmittance of actin polymerized with and without ABP. The presence of actin in the solution results in an increment in turbidity as other proteins provided egfr pathway features [21], [32]. While G-actin showed a transmittance peak positioned at 241 nm, F-actin exhibited
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