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Blood smear stain Finasteride was the first steroidal reduct
2025-02-18
Finasteride (13) was the first steroidal 5α-reductase inhibitor approved by the US Food and Drug Administration (FDA) in 1992 for treatment of BPH. In fact, long term clinical studies with this drug demonstrated a sustained reduction of the prostatic specific antigen and an overall improvement in BH
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Cimetidine A variety of quinazoline or fused pyrimidine subs
2025-02-18
A variety of quinazoline or fused pyrimidine-substituted diaminotriazoles showed sub-100nM inhibition of Axl (). Diaminotriazoles similarly substituted with quinolines, isoquinolines and benzothiazoles also showed potent Axl activity (data not shown), but generally exhibited potent cytotoxicity and
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Previously several genes such as cytokine Lyu and Park cell
2025-02-18
Previously, several genes such as cytokine (Lyu and Park, 2007), cell motility-associated genes (Schotterl et al., 2017), transforming growth factor-β (TGF-β), TGF-β receptor II which is a cell surface receptor with serine/threonine kinase activity (Jiang et al., 2014, Schotterl et al., 2017), cell
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For these reasons the role played by autophagy
2025-02-18
For these reasons, the role played by autophagy in environmental neurotoxicity is not always easily determinable. Indeed, although the neuroprotective role of autophagy has been shown by several studies, sometimes induction of autophagy was associate with deleterious effects (Glick et al., 2010, Sr
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IC values were obtained for an expanded
2025-02-18
IC50 values were obtained for an expanded version of the fragment library using the previously described mobility shift assay. Subsequently, Ki values were estimated from IC50 values to allow better comparison of the activity against targets which were measured at different substrate concentrations
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In this paper we described synthesis biological
2025-02-18
In this paper, we described synthesis, biological evaluation and docking study of 3-aroyl-1-(4-sulfamoylphenyl)thiourea derivatives 4a–o as 15-lipoxygenase inhibitors. Results and discussion Conclusion We designed and synthesized a novel of thiourea derivatives containing phenylsulfonamide mo
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As shown in B the recombinant
2025-02-18
As shown in B, the recombinant human 15-LOX-1 (30nM) showed a time-dependent increase in fluorescent signal, and signal development was almost completed within 20min in the presence of 50μM arachidonic tyrosine kinase receptor and 5μM DHR. For both purified enzyme and cell lysates, the enzyme activ
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Regulators of the DDR have therefore become
2025-02-18
Regulators of the DDR have therefore become attractive targets for cancer therapy primarily through two potential approaches. First, to be used as chemo- or radiosensitisers to increase the effectiveness of standard genotoxic treatments and to help prevent or overcome the development of resistance.
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From an historical perspective ligands
2025-02-18
From an historical perspective, ligands for GPCRs (adrenaline, serotonin, SGC-CBP30 or morphine, to name a few) have been identified before their receptor counterparts, at a time when the concept of receptor itself was controversial [15]. Although many cognate receptors for endogenous ligands were
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Apamin br Conclusions br Author declaration br Acknowledgeme
2025-02-18
Conclusions Author declaration Acknowledgements Introduction ASK1 scaffolding proteins ASK1 adaptor proteins Conclusions Scaffolding and adaptor proteins can coordinate the specific activation of a MAP3K-MAP2K-MAPK pathway in response to various stimuli. For example, both Apamin
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TLX may promote survival and prevent apoptosis
2025-02-18
TLX may promote survival and prevent apoptosis in NB glycine transporter [12]. Here, we ask whether the survival-promoting effects of TLX are mediated by Apoptosis Signal-regulating Kinase-1 (ASK1, MAP3K5). ASK1 is a member of the Mitogen-Activated Protein (MAP) kinase family and it preferentially
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There are several AP binding
2025-02-18
There are several AP-1 EP4 signaling inhibitor in the sequence of TIMP-1 promoter [18,19]. EBV could up-regulate TIMP-1 expression by binding to the AP-1 site in the TIMP-1 promoter [18]. IL-32, a newly multi-function cytokine, could activate AP-1, NF-κβ, p38MAPK signal pathways, and induce cytokin
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Schizophrenia treatment Since the beginning of s more than p
2025-02-18
Since the beginning of 1990s, more than 17,000 papers about physiological relevance of antioxidants have been published according to data from web of science. Based on the available literature, it seems that assessing the antioxidant potential of food by means of in vitro assays or solely epidemiolo
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br Introduction Increasing number of
2025-02-18
Introduction Increasing number of mycosis infections has been reported during the past several years because of the rise in the number of immuno-compromised individuals in subtropical and tropical countries with high mortality and morbidity [1], [2]. Trichophyton mentagrophytes, Trichophyton rubr
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Androgen receptor translocates from the cytoplasm to the nuc
2025-02-18
Androgen receptor translocates from the cytoplasm to the nucleus after binding to its ligands (Quigley et al., 1995). In the current study, although propofol did not significantly affect total androgen receptor protein levels, it significantly decreased nuclear androgen receptor levels. These findin
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