Design, synthesis, and biological characterization of a potent STAT3 degrader for the treatment of gastric cancer

Article Biotechnology & Applied Microbiology

Characterization of a bioactive meroterpenoid isolated from the marine-derived fungus Talaromyces sp.

Xuan Hong et al.

Summary: A new meroterpenoid, taladrimanin A (1), was isolated from a marine-derived fungus, and its structure and activity were studied. Compound 1 showed inhibitory activity against gastric cancer cells and certain bacteria.

APPLIED MICROBIOLOGY AND BIOTECHNOLOGY (2022)

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Article Biochemistry & Molecular Biology

Targeting E2 ubiquitin-conjugating enzyme UbcH5c by small molecule inhibitor suppresses pancreatic cancer growth and metastasis

Simin Qi et al.

Summary: Inhibiting UbcH5c has been identified as a novel and effective strategy for treating pancreatic cancer, and DHPO represents a new class of UbcH5c inhibitor with potential as an anti-pancreatic cancer therapeutic agent.

MOLECULAR CANCER (2022)

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Article Pharmacology & Pharmacy

Inhibition of STAT3 Signaling Pathway by Terphenyllin Suppresses Growth and Metastasis of Gastric Cancer

Dehua Yu et al.

Summary: In this study, the marine-derived natural product terphenyllin was identified to directly interact with STAT3 and exhibit potent anticancer efficacy against gastric cancer through inhibiting the STAT3 signaling pathway.

FRONTIERS IN PHARMACOLOGY (2022)

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Article Biochemistry & Molecular Biology

STAT3 promotes melanoma metastasis by CEBP-induced repression of the MITF pathway

Alexander Swoboda et al.

Summary: The study found that STAT3 can promote the metastatic process of melanoma and antagonize MITF through direct induction of CEBP family member transcription, thereby playing different roles in melanoma progression.

ONCOGENE (2021)

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Article Oncology

Global cancer statistics 2020: GLOBOCAN estimates of incidence and mortality worldwide for 36 cancers in 185 countries

Hyuna Sung et al.

Summary: The global cancer burden in 2020 saw an estimated 19.3 million new cancer cases and almost 10.0 million cancer deaths. Female breast cancer surpassed lung cancer as the most commonly diagnosed cancer, while lung cancer remained the leading cause of cancer death. These trends are expected to rise in 2040, with transitioning countries experiencing a larger increase compared to transitioned countries due to demographic changes and risk factors associated with globalization and a growing economy. Efforts to improve cancer prevention measures and provision of cancer care in transitioning countries will be crucial for global cancer control.

CA-A CANCER JOURNAL FOR CLINICIANS (2021)

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Article Chemistry, Medicinal

Discovery of a Napabucasin PROTAC as an Effective Degrader of the E3 Ligase ZFP91

Maha Hanafi et al.

Summary: XD2-149, a PROTAC based on napabucasin, has a multi-targeted mechanism of action, inhibiting the STAT3 signaling pathway and degrading the ZFP91 protein. ZFP91 plays a critical role in tumorigenesis and is involved in oncogenic pathways such as NF-κB and HIF-1α.

JOURNAL OF MEDICINAL CHEMISTRY (2021)

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Review Oncology

Protein degradation technology: a strategic paradigm shift in drug discovery

Haobin Li et al.

Summary: Targeting pathogenic proteins with small-molecule inhibitors is a widely used strategy for treating malignant tumors, but the lack of active sites in most intracellular proteins poses a challenge for drug design. Protein degradation technologies, including proteolysis-targeting chimeric technology, provide additional approaches for targeting undruggable proteins with advantages like rapid target consumption and stronger pharmacological effects, making them a hot topic in current research.

JOURNAL OF HEMATOLOGY & ONCOLOGY (2021)

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Article Chemistry, Medicinal

Recent Update on Development of Small-Molecule STAT3 Inhibitors for Cancer Therapy: From Phosphorylation Inhibition to Protein Degradation

Jinyun Dong et al.

Summary: STAT3 is a transcription factor regulating various biological processes, frequently abnormally activated in cancer and associated with poor prognosis and tumor progression. Targeting the STAT3 protein may be an effective strategy for treating tumors.

JOURNAL OF MEDICINAL CHEMISTRY (2021)

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Article Biotechnology & Applied Microbiology

Chronos: a cell population dynamics model of CRISPR experiments that improves inference of gene fitness effects

Joshua M. Dempster et al.

Summary: Chronos is an algorithm for inferring gene knockout fitness effects based on cell proliferation dynamics after CRISPR gene knockout, outperforming competitors in control separation and strength of biomarker associations, especially when longitudinal data is available. Additionally, Chronos exhibits low copy number and screen quality bias compared to other evaluated methods.

GENOME BIOLOGY (2021)

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Article Integrative & Complementary Medicine

Safety assessment of Aconitum-Derived bulleyaconitine A: A 91-day oral toxicity study and a tissue accumulation study in rats

Shi-Liang Yin et al.

Summary: The study showed that 0.14 mg/kg BLA had potent analgesic effects, with an LD50 value of 3.4434 mg/kg. The no observed adverse effect level was 0.25 mg/kg in the subchronic toxicity study.

WORLD JOURNAL OF TRADITIONAL CHINESE MEDICINE (2021)

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Article Plant Sciences