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Isolation of Human Endothelial Cells from Normal Colon and Colorectal Carcinoma - An Improved Protocol
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RKI-1447 suppresses colorectal carcinoma cell growth via disrupting cellular bioenergetics and mitochondrial dynamics

Liyi Li1,2, Qin Chen3, Yaojun Yu2

  • 1General Surgery Department, Shandong Provincial Hospital Affiliated to Shandong University, Ji'nan, Shandong, China.

Journal of Cellular Physiology
|June 26, 2019
PubMed

Insights

The Rho/Rho-kinase (ROCK) inhibitor RKI-1447 suppresses colorectal cancer (CRC) growth by disrupting cell energy production and promoting apoptosis. This ROCK inhibitor shows promise as an effective antitumor drug candidate for CRC treatment.

Area of Science:

  • Oncology
  • Molecular Biology
  • Biochemistry

Background:

  • The Rho/Rho-kinase (ROCK) signaling pathway is implicated in cancer progression.
  • The specific role of ROCK in colorectal carcinoma (CRC) remains unclear.
  • Understanding ROCK's function in CRC is crucial for developing targeted therapies.

Purpose of the Study:

  • To investigate the effect of ROCK signaling on colorectal cancer behavior.
  • To evaluate the efficacy of a novel ROCK inhibitor, RKI-1447, in CRC.
  • To elucidate the molecular mechanisms underlying RKI-1447's anti-cancer effects.

Main Methods:

  • Utilized human CRC cell lines (HCT-8, HCT-116) for in vitro studies.
  • Assessed cell viability, apoptosis, mitochondrial respiration, and glycolysis.
  • Investigated reactive oxygen species generation, ER-stress, and CHOP involvement.
  • Conducted in vivo studies using a mouse model of CRC.

Main Results:

  • RKI-1447 significantly inhibited CRC cell growth and induced apoptosis.
  • Inhibition of ROCK by RKI-1447 suppressed mitochondrial respiration and ATP production.
  • RKI-1447 reduced cellular glycolysis and induced reactive oxygen species generation and ER-stress.
  • CHOP was identified as essential for RKI-1447-mediated apoptosis.
  • RKI-1447 demonstrated significant in vivo inhibition of CRC growth.

Conclusions:

  • ROCK signaling inhibition by RKI-1447 effectively suppresses CRC.
  • RKI-1447 disrupts CRC cell bioenergetics through mitochondrial dysfunction.
  • RKI-1447 represents a potential therapeutic candidate for colorectal cancer treatment.
Keywords:
ER-stressRKI-1447cellular bioenergeticscolorectal carcinomamitochondrial dysfunction

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