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br Experimental EPR spectra of probes a f were
2024-11-11

Experimental EPR spectra of probes 1a–f were recorded on a Bruker EMX-1572 operating at X-band (9.0–9.9 GHz), at 21 ± 1 °C. The EPR parameters were the same in all experiments: microwave power, 1 mW; modulation amplitude, 5 G; time constant, 10.24 ms; and conversion time, 40.96 ms. Reduced gluta
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br HIF Signaling in AA Therapy
2024-11-11

HIF-α Signaling in AA Therapy Resistance An important result emerging from Phase 3 clinical trials testing AA therapies is improvement of progression-free survival (PFS) that is not accompanied by enhanced overall survival (OS) [26]. This dichotomy has been attributed to mechanisms of acquired re
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br Conclusion We have identified three non
2024-11-11

Conclusion We have identified three non-competitive inhibitors of the human and porcine APN with Ki values in the μM range, by combining virtual screening and kinetic assays. Molecular docking simulations suggest these novel inhibitors block APN activity by an alternative mechanism to Zn coordina
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It is well known that
2024-11-11

It is well-known that TCDD is the most potent ligand of AhR and it regulates gene expression, such as CYP1A1, via activation of AhR (Mimura and Fujii-Kuriyama, 2003). Besides Tomblin et al. (2016) have recently shown that TCDD via AhR regulated L-type amino Lomustine transporter 1 expression in MCF
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Furthermore stress hormones can indirectly induce DNA
2024-11-09

Furthermore, stress hormones can indirectly induce DNA damage, for example by altering DNA repair and transcriptional regulation of the cell cycle. It has been found that stress hormones induce the up-regulation of checkpoint kinase 1 (Chk1) and checkpoint kinase 2 (Chk2) and proto-oncogene cell div
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HT modulates cortical and hippocampal pyramidal cell functio
2024-11-09

5-HT modulates cortical and hippocampal pyramidal cell function in a very complex manner, since most 5-HT receptor subtypes (excitatory as well as inhibitory) are expressed on pyramidal Apoptozole synthesis as well as GABAergic interneurons that exert inhibitory control over pyramidal cells (Leiser
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br Conclusion br Conflicts of interest br Introduction Enzym
2024-11-09

Conclusion Conflicts of interest Introduction Enzymes are widely applied as biocatalysts in fields such as synthetic chemistry [1], pharmaceuticals [2], environmental treatment [3], and food technology [4] because they can catalyze chemical transformations in a highly selective manner under
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The results show that a tonic
2024-11-09

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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br Methods br Transparency document br
2024-11-09

Methods Transparency document Introduction Epinephrine (EP) is a critical hormone and catecholamine neurotransmitter in nervous system of mammals.1, 2, 3 It has been known to accelerate and regulate heartbeat, blood pressure, bronchodilation, mydriasis, blood sugar and lipolysis, and can he
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A combination of factors might however
2024-11-09

A combination of factors might, however, account for the low rate of success of drug development for neuropsychiatric disorders. First, in most neuropsychiatric disorders, the symptomatology is heterogeneous and the neurobiology remains poorly understood, making therapeutic targets difficult to iden
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While the direct effects of ARI
2024-11-09

While the direct effects of 5-ARI lead to a dramatic WST-8 assay vs MTT assay comparison in serum DHT levels, other laboratory values are also affected by 5-ARI use. Serum testosterone elevations are known to occur with both finasteride and dutasteride use, but values will typically remain within t
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The relatively high concentration of HT used
2024-11-09

The relatively high concentration of 5-HT used in this study (100 µM) is consistent with the concentrations used in other published ex vivo studies (Ropert and Guy, 1991, Passani et al., 1994, Shen and Andrade, 1998). In our paradigm 5-HT was focally applied at the surface of the slice via a fast pe
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The consensus amino acid recognition sequence for
2024-11-09

The consensus amino bepridil recognition sequence for p38α substrates is (Ser/Thr)Pro (Cuadrado and Nebreda, 2010), typically assisted by upstream docking motifs (Remenyi et al, 2005, Sharrocks et al, 2000). P450c17 has 32 Ser and 25 Thr residues, of which only Thr 341 and Ser 427 are immediately fo
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br Acknowledgements We thank Dr Stefan Schulte Merker
2024-11-09

Acknowledgements We thank Dr. Stefan Schulte-Merker and his group members at the Hubrecht Institute (Utrecht, the Netherlands) for their invaluable support of the zebrafish studies. Our work is supported by grants from the Dutch Cancer Society (KWF) and the Netherlands Organisation for Scientific
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The present study indicates elevated
2024-11-09

The present study indicates elevated ATX activity as a highly sensitive and specific biomarker to differentiate ICP from other pregnancy-related liver disorders or pruritic dermatoses. In 1-NM-PP1 to the current gold standard for diagnosis, total fasting serum bile salt levels, ATX appeared as a ve
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