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The most potent compounds within
2024-06-21

The most potent compounds within the current series of compounds were therefore , , , , and , with SCH527123 possessing the best selectivity towards the lyase reaction in comparison to the hydroxylase reaction, indeed, this compound was found to possess an IC value of 1210nM against the 17α-OHase
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br Disclosure br Acknowledgement br Introduction CYP A is a
2024-06-21

Disclosure Acknowledgement Introduction CYP17A1 is a multifunctional enzyme with both 17α-hydroxylase and 17,20-lyase activities and is essential for the biosynthesis of steroidal nor-NOHA acetate in male testes and adrenal glands. The 17α-hydroxylase activity of CYP17A1 is involved in the
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Our results showed suppressed autophagy in GECs under HAGG s
2024-06-21

Our results showed suppressed autophagy in GECs under HAGG stimulation. Recently, people have paid more attentions on the roles of autophagy in lupus and tried to use autophagy regulators for therapy. Rapamycin could prevent the development of nephritis [49] and attenuate the established nephritis [
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The following are the supplementary data
2024-06-21

The following are the supplementary data related to this article. Competing interest Ethics approval and consent to participate Authors' contributions Acknowledgements The authors thank Dr. D. R. Kaplan for kind advice and materials derived from NB primary cell lines, Dr. F. D. Miller f
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TPEN The results of our in vivo
2024-06-21

The results of our in vivo experiments provide promising evidence that the apelin/APLNR axis is implicated in CCA growth and that targeting this axis with a receptor specific antagonist may help develop effective, tumor directed therapies. Not only do we show decreased proliferation and angiogenesis
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br Acknowledgements The authors would
2024-06-20

Acknowledgements The authors would like to thank Dr. Bradford B. Lowell for providing us with β-less and WT breeding pairs. Funding sources: This work was supported by NIH Grant DK028082 (to E.M.F) and by an Institutional Research Training Grant NRSA 5T32DK751627 (to N.D.). Introduction The e
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br Experimental section br Results and discussion br
2024-06-20

Experimental section Results and discussion Conclusions We present a simple, sensitive and selective assay of ADA activity and its inhibitor using the enzyme catalyzed reaction and the different interaction intensity of dye-labeled AD aptamer, aptamer/AD complex with GO. The as-proposed met
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Finasteride has been shown to be
2024-06-20

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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Ryoichi et al modified potent clinical candidate
2024-06-20

Ryoichi et al. modified potent clinical candidate VX-680 (6) with 3-cyano-6-(5-methyl-3-pyrazolamino)pyridine as Aurora kinase inhibitor. Substituted cyano pyridine derivative (7) inhibited proliferation of HCT-116 cells with an IC50 value of 115 nM. It showed tumor inhibition in mice model at a dos
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Cerebral ischemia occurs following the occlusion of
2024-06-20

Cerebral ischemia occurs following the occlusion of a cerebral artery by a thrombus and causes cell swelling due to cytotoxic edema and BBB disruption with vasogenic edema (Loreto and Reggio, 2010, Nakaji et al., 2006, Shibata et al., 2004). Vasogenic edema is directly linked to alteration of the BB
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133 2 mg The structural analysis of the ASK activation segme
2024-06-20

The structural analysis of the ASK1 activation segment, which was not phosphorylated in the crystal structure, showed interactions mimicking those found in activated kinases. In addition, the isolated unphosphorylated ASK1-CD is active and able to autophosphorylate itself at three sites, Thr813, Thr
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br Materials and methods br Results br Discussion In
2024-06-19

Materials and methods Results Discussion In this study, the orphan receptor GPR25 was cloned from several representative vertebrate species including zebrafish. Although the overall amino Evans Blue tetrasodium salt sequence identity among these species is not high (38–52%), our synteny an
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Besides above mentioned UV visible and fluorescence spectros
2024-06-19

Besides above-mentioned UV–visible and fluorescence spectroscopy methods, electron paramagnetic resonance (EPR) spectroscopy, the only analytical method that detect compounds having unpaired electrons known as free radicals, was rarely used in antioxidant capacity measurement (Amarowicz et al., 2004
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Thiazole heterocycles constitute an interesting class of mol
2024-06-19

Thiazole heterocycles constitute an interesting class of molecules, which exhibit a broad spectrum of biological activity, including antifungal properties [[16], [17], [18], [19]]. Encouraged by our previous study that describes the activity of hydrazine-thiazole derivatives against C. gattii and C.
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Prolonged duration of antimicrobial agents
2024-06-19

Prolonged duration of antimicrobial agents is also associated with increased risk of CDI by extending the time disruption of normal enteric flora. This emphasizes the importance for clinicians to adhere to shorter durations of therapy. Although longer durations of therapy are associated with a great
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