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Updated: Feb 10, 2026

Molecular Analysis of Endothelial-mesenchymal Transition Induced by Transforming Growth Factor-β Signaling
07:49

Molecular Analysis of Endothelial-mesenchymal Transition Induced by Transforming Growth Factor-β Signaling

Published on: August 3, 2018

11.8K

A targeted transforming growth factor-beta (TGF-β) blocker, TTB, inhibits tumor growth and metastasis

Changhua Zhou1,2, Jing Li1,2, Limin Lin1,2

  • 1School of Pharmaceutical Sciences, Sun Yat-Sen University, Guangzhou, 510006, China.

Oncotarget
|May 26, 2018
PubMed

Insights

A novel tumor-targeting TGF-β receptor blocker (TTB) effectively inhibits cancer progression and metastasis. This targeted therapy shows potent anti-cancer activity in preclinical models, offering a promising approach for late-stage cancers.

Area of Science:

  • Oncology
  • Molecular Biology
  • Biotechnology

Background:

  • Transforming growth factor beta (TGF-β) is a key driver of cancer progression in advanced stages.
  • Targeting the TGF-β pathway is a therapeutic strategy to inhibit tumor growth and metastasis.

Purpose of the Study:

  • To investigate the efficacy of a novel tumor-targeting TGF-β receptor blocker (TTB) in inhibiting cancer progression.
  • To evaluate the therapeutic potential of TTB in preclinical cancer models.

Main Methods:

  • TTB was engineered by fusing the TGF-β receptor II extracellular domain, TGF-β receptor III endoglin domain, and human IgG1 Fc fragment.
  • An RGD peptide was incorporated for enhanced tumor microenvironment targeting.
  • In vitro assays assessed TGF-β neutralization, cell migration, invasion, and colony formation.
  • In vivo studies utilized xenograft models to evaluate tumor inhibition and metastasis suppression.

Main Results:

  • TTB demonstrated potent TGF-β neutralization activity in vitro.
  • TTB significantly inhibited cancer cell migration, invasion, and colony formation.
  • In vivo, TTB exhibited significant tumor inhibition and suppressed breast cancer metastasis.
  • TTB attenuated TGF-β1-induced Smad2 phosphorylation and epithelial-to-mesenchymal transition (EMT).

Conclusions:

  • The engineered TTB is an effective TGF-β pathway inhibitor.
  • TTB demonstrates strong anti-tumor and anti-metastatic potential in preclinical settings.
  • TTB represents a promising therapeutic candidate for blocking TGF-β-induced pathogenesis in vivo.
Keywords:
RGDTGF-βTGF-β inhibitorscancer metastasisreceptor

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