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Updated: Sep 13, 2025

Gene Regulation and Targeted Therapy in Gastric Cancer Peritoneal Metastasis: Radiological Findings from Dual Energy CT and PET/CT
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Mechanism of SC targeting RhoA regulation and its potential value in gastric cancer therapy

Haixiu Ma1, Ping Jiang2, Ronghua Ma1

  • 1Research Center for High Altitude Medicine, Key Laboratory for High Altitude Medicine, Ministry of Education, Qinghai University, 16# Kunlun Road, Xining, 810016, Qinghai, China.

Biochemistry and Biophysics Reports
|August 1, 2025
PubMed

Insights

A novel compound, SC, effectively inhibits RhoA, a key driver of gastric cancer progression. This dual-action inhibitor shows promise in preclinical models by disrupting cancer cell migration and reducing tumor growth.

Area of Science:

  • Oncology
  • Molecular Biology
  • Biochemistry

Background:

  • RhoA signaling is crucial for gastric cancer progression, mediating cytoskeletal changes and epithelial-mesenchymal transition (EMT).
  • Targeting RhoA offers a potential therapeutic strategy for gastric cancer treatment.

Purpose of the Study:

  • To identify and characterize a novel small-molecule inhibitor of RhoA.
  • To evaluate the efficacy of the inhibitor, SC, in preclinical gastric cancer models.

Main Methods:

  • Molecular docking and surface plasmon resonance (SPR) were used to identify and validate SC as a RhoA inhibitor.
  • In vitro assays assessed the effects of SC on RhoA expression, EMT markers (E-cadherin, N-cadherin, Vimentin), and cell migration.
  • Scanning electron microscopy evaluated cytoskeletal changes.
  • A xenograft mouse model was used to assess in vivo anti-tumor efficacy.

Main Results:

  • SC demonstrated high-affinity binding to RhoA, with a dissociation constant (KD) of 1.588 μM.
  • In vitro, SC significantly suppressed RhoA, upregulated E-cadherin, downregulated N-cadherin and Vimentin, and inhibited cell migration (p < 0.001).
  • SC treatment led to cytoskeletal collapse and pseudopodia retraction, and significantly attenuated tumor growth in vivo.

Conclusions:

  • SC is a novel dual-action RhoA inhibitor that disrupts both GTPase activity and protein stability.
  • SC presents a promising therapeutic candidate for gastric cancer treatment by targeting key pathways of malignant progression.
Keywords:
Drug discoveryDual actionEMTNatural productRhoA inhibitor

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