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Identification, Synthesis, and Biological Evaluations of Potent Inhibitors Targeting Type I Protein Arginine Methyltransferases
Published 2022“…In this study, we first identified several hit compounds against CARM1 by structure-based virtual screening (IC<sub>50</sub> = 35.51 ± 6.68 to 68.70 ± 8.12 μM) and then carried out chemical structural optimizations, leading to six compounds with significantly improved activities targeting CARM1 (IC<sub>50</sub> = 18 ± 2 to 107 ± 6 nM). …”
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IDD388 Polyhalogenated Derivatives as Probes for an Improved Structure-Based Selectivity of AKR1B10 Inhibitors
Published 2016“…Next, by means of IC<sub>50</sub> measurements, X-ray crystallography, WaterMap analysis, and advanced binding free energy calculations with a quantum-mechanical (QM) approach, we have studied their structure–activity relationship (SAR) against both enzymes. …”
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1708
Gene clustering identifies up- and down-regulated groups that control development, pluripotency, and cell division.
Published 2019“…<p>Pluripotent H9 hESCs were differentiated for 50 days as previously described [<a href="http://www.plosone.org/article/info:doi/10.1371/journal.pone.0222946#pone.0222946.ref012" target="_blank">12</a>], beginning with high (7.5 μM or 10 μM) CHIR99021 concentrations. mRNA samples from the indicated time points were subjected to gene expression profiling. …”
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Data Sheet 1_Reduced hemolytic complement activity in the classical pathway (CH50) is a risk factor for poor clinical outcomes of patients with infections: a retrospective analysis...
Published 2025“…</p>Results<p>Of 2,726 patients who met the inclusion criteria, logistic regression models demonstrated that decreased CH50 is a significant predictor of 180-day mortality (OR: 0.98-0.99). …”
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Discovery of Betulinic Acid Derivatives as Potent Intestinal Farnesoid X Receptor Antagonists to Ameliorate Nonalcoholic Steatohepatitis
Published 2022“…Evidence showed that intestinal FXR antagonism exhibited remarkable metabolic improvements in mice. Herein, we developed a series of betulinic acid derivatives as potent intestinal FXR antagonists, and <b>F6</b> was identified as the most potent one with an IC<sub>50</sub> at 2.1 μM. …”
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Discovery of Betulinic Acid Derivatives as Potent Intestinal Farnesoid X Receptor Antagonists to Ameliorate Nonalcoholic Steatohepatitis
Published 2022“…Evidence showed that intestinal FXR antagonism exhibited remarkable metabolic improvements in mice. Herein, we developed a series of betulinic acid derivatives as potent intestinal FXR antagonists, and <b>F6</b> was identified as the most potent one with an IC<sub>50</sub> at 2.1 μM. …”
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Combination of DNA Damage, Autophagy, and ERK Inhibition: Novel Evodiamine-Inspired Multi-Action Pt(IV) Prodrugs with High-Efficiency and Low-Toxicity Antitumor Activity
Published 2023“…Among them, compound <b>10</b> exhibited a 118-fold enhancement in the IC<sub>50</sub> value compared to cisplatin and low toxicity to normal cells. …”
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Combination of DNA Damage, Autophagy, and ERK Inhibition: Novel Evodiamine-Inspired Multi-Action Pt(IV) Prodrugs with High-Efficiency and Low-Toxicity Antitumor Activity
Published 2023“…Among them, compound <b>10</b> exhibited a 118-fold enhancement in the IC<sub>50</sub> value compared to cisplatin and low toxicity to normal cells. …”
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Combination of DNA Damage, Autophagy, and ERK Inhibition: Novel Evodiamine-Inspired Multi-Action Pt(IV) Prodrugs with High-Efficiency and Low-Toxicity Antitumor Activity
Published 2023“…Among them, compound <b>10</b> exhibited a 118-fold enhancement in the IC<sub>50</sub> value compared to cisplatin and low toxicity to normal cells. …”
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Combination of DNA Damage, Autophagy, and ERK Inhibition: Novel Evodiamine-Inspired Multi-Action Pt(IV) Prodrugs with High-Efficiency and Low-Toxicity Antitumor Activity
Published 2023“…Among them, compound <b>10</b> exhibited a 118-fold enhancement in the IC<sub>50</sub> value compared to cisplatin and low toxicity to normal cells. …”
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Combination of DNA Damage, Autophagy, and ERK Inhibition: Novel Evodiamine-Inspired Multi-Action Pt(IV) Prodrugs with High-Efficiency and Low-Toxicity Antitumor Activity
Published 2023“…Among them, compound <b>10</b> exhibited a 118-fold enhancement in the IC<sub>50</sub> value compared to cisplatin and low toxicity to normal cells. …”
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