Results 261 to 270 of about 11,649,511 (362)

NMR screening of low molecular weight inhibitors targeting the papain‐like protease (PLPro) of SARS‐CoV‐2

open access: yesFEBS Open Bio, EarlyView.
Papain‐like protease from SARS‐CoV‐2 plays an important role in the cleavage of the viral polyproteins and in the suppression of the host's immune response. Here, we present the results of an NMR screening study. We identified 86 binding compounds, of which five candidates were chosen for in‐depth analysis.
Dennis J. Pyper   +5 more
wiley   +1 more source

Ro 31‐8220 suppresses bladder cancer progression via enhancing autophagy in vitro and in vivo

open access: yesFEBS Open Bio, EarlyView.
The pan‐protein kinase C inhibitor Ro‐31‐8220 demonstrates potent anti‐bladder cancer effects both in vitro and in vivo by suppressing migration/invasion, inducing apoptosis and crucially activating autophagy, where blocking autophagy with chloroquine reduces its cell‐killing efficacy, suggesting its promise as a novel therapeutic candidate requiring ...
Shengjun Fu   +12 more
wiley   +1 more source

Polydatin ameliorates ovalbumin‐induced asthma in a rat model through NCOA4‐mediated ferroautophagy and ferroptosis pathway

open access: yesFEBS Open Bio, EarlyView.
In this research, a rat model of asthma was created using OVA, and polydatin served as an intervention. By inhibiting ferroautophagy mediated by NCOA4 and averting ferroptosis, polydatin has been demonstrated to reduce asthma. This work presents new ideas for investigating the mechanism of polydatin's ability to alleviate asthma, in addition to ...
Wei Li   +5 more
wiley   +1 more source

Drug Exposure in Chronic Kidney Disease: It Is Not Just About the Glomerular Filtration Rate. [PDF]

open access: yesFundam Clin Pharmacol
Liabeuf S   +6 more
europepmc   +1 more source

Blocking the voltage‐gated sodium channel hNav1.5 as a novel pH‐dependent mechanism of action for tamoxifen

open access: yesFEBS Open Bio, EarlyView.
Patch‐clamp recordings revealed that tamoxifen inhibits voltage‐gated sodium channels, especially under acidic conditions, both common in metastatic cancer cells. These effects may explain certain antitumor properties of tamoxifen, highlighting a novel mechanism of action beyond its known endocrine effects.
Karl Josef Föhr   +5 more
wiley   +1 more source

Menthol‐like cooling compounds, including (R)‐(‐)‐carvone, inhibit the human bitter taste receptors for saccharin and acesulfame K

open access: yesFEBS Open Bio, EarlyView.
We report that some menthol‐like cooling compounds, including (R)‐(‐)‐carvone, act as inhibitors of TAS2R31 and TAS2R43, which are taste receptors responsible for the intrinsic bitter aftertastes of saccharin and acesulfame K. However, there was little correlation between the intensity of the cooling sensation and the potency of bitterness inhibition ...
Miyuu Saito, Takumi Misaka
wiley   +1 more source

Cis‐unsaturated sphingolipids support growth of sphingoid base‐deficient yeast but impair plasma membrane integrity

open access: yesFEBS Open Bio, EarlyView.
Sphingoid base structures, the sphingolipid backbones, vary among species. We established yeast cells in which the native sphingoid base was replaced with plant‐type bases containing cis or trans double bonds. This is, to our knowledge, the first eukaryotic model mostly composed of sphingolipids containing cis‐unsaturated sphingoid base, providing a ...
Takashi Higuchi   +5 more
wiley   +1 more source

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