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br Aberrantly enhanced adenosine signaling in retina
2025-01-24
Aberrantly enhanced adenosine signaling in retina of oxygen-induced retinopathy Current therapeutic development of ROP focuses on directly targeting VEGF and HIF-1α signaling pathway (Cavallaro et al., 2014, Penn et al., 2008, Mintz-Hittner et al., 2011, Hartnett and Penn, 2012). However, cellula
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On the basis of the above information we designed
2025-01-24
On the basis of the above information, we designed a new series of benzothiazole–piperazine derivatives (–) that have the aforementioned structural requirements (). Benzothiazole is an important ring system in the drug discovery studies of AD. There are several benzothiazole compounds that show pot
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Our previous studies found that
2025-01-24
Our previous studies found that some steroid mimetic structures such as stilbene, biphenyl, naphthalene and benzothiophene rings were suitable for lipophilic moieties of 17,20-lyase inhibitors, and several inhibitors obtained using a steroid A, C-ring mimetic approach have already been published. D
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For both the hydroxylation and lyase reactions the
2025-01-24
For both, the 17α-hydroxylation and 17, 20-lyase reactions, the heme iron center of P450 17A1 receives electron reducing equivalents from CPR. Both reactions require one pair of electrons and molecular oxygen for the conversion of the substrate into product in each catalytic cycle. However, the 17,2
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Jesus et al discovered a new series of azaindole as
2025-01-23
Jesus et al. discovered a new series of azaindole as Aurora inhibitors through various modification of GSK1070916 (47). They synthesized series from modification of the GSK1070916 and evaluated for in-vitro Aurora-B/INCENP and Aurora-A/TPX2 inhibition assays. Modified lpa receptor 48 and 49 showed
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br Author contributions br Conflicts of interest The authors
2025-01-23
Author contributions Conflicts of interest The authors declare no competing financial interests. Acknowledgement This work was supported by grants from the Deutsche Forschungsgemeinschaft (Sonderforschungsbereich/Transregio 166–Project C1 and grant CA 1014/1-1 to D.C.) and the IZKF Würzbur
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Fourth non canonical sites may be
2025-01-23
Fourth, non-canonical sites may be targeted. Classical benzodiazepines require the presence of a γ subunit for high-affinity binding, which limits their activity to a specific large pool of receptor isoforms, leaving other isoforms unaffected. In particular, δ subunit-containing receptors, as well a
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rock inhibitor Additionally we used the predicted Cyp a b am
2025-01-23
Additionally, we used the predicted Cyp19a1b amino rock inhibitor sequence from a number of bony fish species to infer their genetic relatedness and found that R. quelen occupies an ancient position within the Siluriformes group. A phylogenetic tree was constructed and it included both full-length
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br Antioxidant polymers conjugates Natural antioxidants are
2025-01-23
Antioxidant-polymers conjugates Natural antioxidants are usually used as a substitute for synthetics but some degradation phenomena could influence their applications. For example, ascorbic Cancer therapy as a natural antioxidant undergoes yellowish coloration as a result of oxidation [29]. Sing
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br Natriuretic peptides and neprilysin Left ventricular syst
2025-01-23
Natriuretic peptides and neprilysin Left ventricular systolic function, most commonly due to myocardial damage as a consequence of coronary artery disease, hypertension or both, and leading to sustained, pathological activation of the renin angiotensin LDN193189 Hydrochloride system (RAAS) and s
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In conclusion our study has identified a spl
2025-01-23
In conclusion, our study has identified a splice site GC-rich DNA targeting (c.1769-1G > C) in the AR gene from two patients with complete androgen insensitivity syndrome. The c.1769-1G > C mutation may provide us new insights into the molecular mechanism involved in splicing defects underlying CAIS
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There are several reports providing evidences
2025-01-23
There are several reports providing evidences that functional and mechanistic connection between Sirt1 and LKB1/AMPK in metabolic regulation [26], [32], [33]. It has been reported that the deacetylation of LKB1 by Sirt1 is one of the determining factors of the subcellular localization of LKB1. In ag
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p m x Hepatic inflammation and fibrosis are hallmarks
2025-01-23
Hepatic p m x and fibrosis are hallmarks of the NASH phenotype and are thought to occur in a subset of patients with NAFLD. While it is hypothesized that therapeutic lowering of hepatic lipids will be sufficient to improve hepatic fibrosis and inflammation secondarily, this remains controversial an
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The application of diuretics induce an increased rate
2025-01-23
The application of diuretics induce an increased rate of water exiting brain cells encouraging the formation of increased intracellular polyphosphoric acid. In the absence of the diuretic water is retained in cells converting polyphosphoric ATP Synthesis to monophosphoric acid. The latter change de
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The G R mutation is located at the solvent front
2025-01-23
The G1202R mutation is located at the solvent front of the ALK kinase domain adjacent to the inhibitor's binding pocket. Although barely reported in the setting of crizotinib resistance, it has emerged as the most refractory mutation to both the first- and second-generation ALK inhibitors. The large
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