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Finasteride has been shown to be a mechanism based inhibitor
2025-02-27
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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guanosine derivative The relatively high concentration of HT
2025-02-27
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 H N mutation in
2025-02-27
The H373N mutation in exon 6 has not previously been reported [3], [4], [5], [6]; thus, this mutation appears to be a novel mutation. The functional expression study demonstrated that the H373N mutation results in almost complete loss of enzymatic activity. Thus, it is highly likely that the H373N m
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In our previous report we synthesized derivatives with some
2025-02-27
In our previous report, we synthesized derivatives with some straight chain residues on the 2-position of the 3-cyanopyridine ring of compound 1. In this time we tried to introduce aromatic ring on the chain of the 2-position. Namely, we replaced the hydroxyl-alkylamino group in the position 2 of t
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Aurora kinases are a conserved family of serine
2025-02-27
Aurora kinases are a conserved family of serine/threonine kinases that are important for the transition through mitosis and amplification and overexpression of Aurora kinases have been implicated in Alarelin Acetate and transformation. Aurora B is located at the centromere and controls aspects of k
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The identification of novel kinase
2025-02-27
The identification of novel kinase inhibitor scaffolds is highly desirable in order to develop selective kinase inhibitors. Small-molecule inhibitors of Interleukin-2-inducible T-cell kinase (Itk) that are based on the 3-aminopyridin-2-one fragment 1 have been reported. Despite derivatisation of 1 y
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Our results clearly demonstrate that
2025-02-27
Our results clearly demonstrate that inhibition of ATM pathway activation results in resistance to Vγ2Vδ2 T cell-mediated cell death. Therefore, enhancing ATM activation along with Vγ2Vδ2 T cell treatment would promote the cytotoxicity of resistant ovarian cancer cells. To our knowledge, this is the
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br Aromatase the key enzyme for
2025-02-27
Aromatase: the key enzyme for estrogen formation in adipose tissue Estrogens are synthesized from androgens by aromatase, a member of the cytochrome P450 superfamily, which is the rate-limiting enzyme in estrogen biosynthesis (Santen et al, 2009, Simpson et al, 1994). At the cellular level, aroma
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br Experimental section br Acknowledgements
2025-02-27
Experimental section Acknowledgements The authors thank Prof. Yongbing Cao from School of Pharmacy, the Second Military Medical University, for providing the fluconazole-resistant strains of Candida albicans(strain 100 and strain 103). This work was supported by Program for Innovative Research
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We provide here direct evidences
2025-02-27
We provide here direct evidences that AT1 receptors are active in ADSCs since Ang II induces intracellular Ca mobilization in these cells. Data obtained during the observation of Ca influxes led us to the search for the ADSCs subpopulation constantly expressing AT1 receptor. ADSCs are necessary for
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On the contrary Birrel and colleagues observed divergent pro
2025-02-27
On the contrary, Birrel and colleagues observed divergent proliferative responses to androgens in different BC cell lines: DHT and mibolerone were found to inhibit the T47-D and ZR-75-1 Group III mGluR agonist growth, while the proliferation of MCF-7 cells was increased by both the androgens [53]. I
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br Materials and methods br Results br Discussion We
2025-02-26
Materials and methods Results Discussion We have in this study used semi-nested degenerative PCR to identify the lipoxygenases expressed in the lung tissue from M. fascicularis and report on the identification of 5- and 12/15-LO transcripts from this tissue. Although we did not find transcr
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In human epidermoid carcinoma A cells lipoxygenase was signi
2025-02-26
In human epidermoid carcinoma A431 cells, 12-lipoxygenase was significantly increased in glutathione-depleted cells. The relative abundance of phospholipid hydroperoxide versus glutathione peroxidase seems to play an important role in controlling the lipoxygenase reaction [57]. It has been proposed
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br Acknowledgments This work was supported by
2025-02-26
Acknowledgments This work was supported by Grant-in-aid for Scientific Research (S) (20229008) (to T.K.), Targeted Proteins Research Program (to T.K.), the Global COE Research Program (to T.K.) and Translational Systems Biology and Medicine Initiative (to T.K.) from the Ministry of Education, Cu
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G actin has a molecular weight of
2025-02-26
G-actin has a molecular weight of 42 kD and dimensions about 55 × 55 × 35 Å3. It consists of 375 amino acids arranged into two individual domains (Alberts et al., 2014). A central cleft bisects the protein into two aforementioned domains which surround a deep cleft containing ATP or ADP and a tightl