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Related Concept Videos

The JAK-STAT Signaling Pathway01:20

The JAK-STAT Signaling Pathway

Several cytokine receptors have tightly bound Janus kinase or JAK proteins attached at their cytosolic tail. Small signaling molecules such as cytokines, growth hormones, or prolactins bind to the cytokine receptors and initiate their dimerization. The dimerization brings the cytosolic JAKs together that trans-phosphorylate and activates each other. The activated JAKs now phosphorylate cytosolic tails of the cytokine receptors, which serve as binding sites for adaptor proteins such as  SH2...
Hedgehog Signaling Pathway02:33

Hedgehog Signaling Pathway

The Hedgehog gene (Hh) was first discovered due to its control of the growth of disorganized, hair-like bristles phenotype in Drosophila, much like hedgehog spines. Hh plays a crucial role in the development of organs and the maintenance of homeostasis in both invertebrates and vertebrates. However, while Drosophila has only one Hh protein, mammals have multiple functional Hedgehog proteins - Sonic (Shh), Desert (Dhh), and Indian Hedgehog (Ihh). All of these homologous proteins have adapted to...
PI3K/mTOR/AKT Signaling Pathway01:22

PI3K/mTOR/AKT Signaling Pathway

The mammalian target of rapamycin  (mTOR) is a serine/threonine kinase that regulates growth, proliferation, and cell survival in response to hormones, growth factors, or nutrient availability. This kinase exists in two structurally and functionally distinct forms: mTOR complex 1  (mTORC1) and mTOR complex 2  (mTORC2). The first form (mTORC1) is composed of a rapamycin-sensitive Raptor and proline-rich Akt substrate, PRAS40. In contrast,  mTORC2 consists of a rapamycin-insensitive companion...
IP3/DAG Signaling Pathway01:11

IP3/DAG Signaling Pathway

Membrane lipids such as phosphatidylinositol (PI) are precursors for several membrane-bound and soluble second messengers. Specific kinases phosphorylate PI and produce phosphorylated inositol phospholipids. One such inositol phospholipids are the  phosphatidylinositol-4,5 bisphosphate [PI(4,5)P2], present in the inner half of the lipid bilayer. Upon ligand binding, GPCR stimulates Gq proteins to turn on phospholipase Cꞵ. Activated phospholipase Cꞵ cleaves PI(4,5)P2 and produces two-second...

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Related Experiment Video

Updated: May 19, 2026

The Efficacy and Underlying Pathway Mechanisms of ShiDuGao Treatment for Anus Eczema Based on GEO Datasets and Network Pharmacology
12:34

The Efficacy and Underlying Pathway Mechanisms of ShiDuGao Treatment for Anus Eczema Based on GEO Datasets and Network Pharmacology

Published on: January 12, 2024

Small-molecule STAT3 signaling pathway modulators from Polygonum cuspidatum.

Jiawei Liu1, Qing Zhang, Kaotang Chen

  • 1Ministry of Education Key Laboratory of Chinese Medicinal Plants Resource from Lingnan, Research Center of Medicinal Plants Resource Science and Engineering, Guangzhou University of Chinese Medicine, Guangzhou, People's Republic of China. jiawei.liu@ymail.com

Planta Medica
|August 3, 2012
PubMed
Summary

Researchers identified novel STAT3 inhibitors from Polygonum cuspidatum roots. Compound 1 potently inhibited STAT3 activation and breast cancer cell proliferation, highlighting its therapeutic potential.

Related Experiment Videos

Last Updated: May 19, 2026

The Efficacy and Underlying Pathway Mechanisms of ShiDuGao Treatment for Anus Eczema Based on GEO Datasets and Network Pharmacology
12:34

The Efficacy and Underlying Pathway Mechanisms of ShiDuGao Treatment for Anus Eczema Based on GEO Datasets and Network Pharmacology

Published on: January 12, 2024

Area of Science:

  • Pharmacology
  • Molecular Biology
  • Natural Products Chemistry

Background:

  • Constitutively activated STAT3 is crucial for cancer development and metastasis.
  • STAT3 is a validated therapeutic target for anticancer drug development.
  • Identifying small molecules to modulate STAT3 activity is of significant therapeutic interest.

Purpose of the Study:

  • To isolate novel STAT3 signaling pathway modulators from Polygonum cuspidatum roots.
  • To evaluate the anticancer potential of isolated compounds.
  • To understand the structure-activity relationships of quinone analogues.

Main Methods:

  • Bioassay-guided fractionation using a STAT3 reporter gene assay.
  • Isolation and structural elucidation of active compounds from Polygonum cuspidatum.
  • In vitro evaluation of STAT3 inhibitory activity and antiproliferative effects on human breast cancer cells.

Main Results:

  • 2-Methoxystypandrone (1) and three anthraquinones (2-4) were identified as major active components.
  • Compound 1 exhibited potent inhibition of STAT3 activation.
  • Compound 1 significantly inhibited proliferation of human breast cancer cells, particularly those with activated STAT3 (IC50 = 2.7-3.1 µM).
  • Structure-activity relationship analysis indicated phenolic and carbonyl groups are key for STAT3 inhibitory activity.

Conclusions:

  • Polygonum cuspidatum is a source of novel STAT3 inhibitors.
  • 2-Methoxystypandrone is a promising lead compound for developing STAT3-targeted anticancer therapies.
  • The identified structural features provide insights for designing more potent STAT3 modulators.