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Anticancer activities of a benzimidazole compound through sirtuin inhibition in colorectal cancer

Yi Jer Tan1, Yeuan Ting Lee1, Keng Yoon Yeong1,2

  • 1Institute for Research in Molecular Medicine (INFORMM), Universiti Sains Malaysia, Penang, 11800, Malaysia.

Future Medicinal Chemistry
|August 2, 2018
PubMed
Abstract

Insights

A novel sirtuin inhibitor, BZD9L1, effectively reduced colorectal cancer (CRC) cell viability and migration by inducing apoptosis. This compound shows promise as a colorectal cancer therapeutic strategy.

Area of Science:

  • Oncology
  • Molecular Biology
  • Pharmacology

Background:

  • Colorectal cancer (CRC) remains a significant global health challenge.
  • Targeted therapies are crucial for improving CRC treatment outcomes.
  • Sirtuin inhibitors represent a potential new class of anticancer agents.

Purpose of the Study:

  • To elucidate the mechanism of action of a novel sirtuin inhibitor, BZD9L1.
  • To investigate the molecular pathways affected by BZD9L1 in colorectal cancer (CRC) cells.
  • To evaluate the therapeutic potential of BZD9L1 in CRC.

Main Methods:

  • Cytotoxicity assays were performed on metastatic CRC cell lines (HCT 116, HT-29).
  • Cell cycle progression, apoptosis, and senescence were analyzed.
  • Expression of apoptosis-related genes and proteins was assessed.
  • Impact on major cancer signaling pathways was evaluated.

Main Results:

  • BZD9L1 significantly reduced viability, migration, and colony formation in CRC cells.
  • Apoptosis was identified as the primary mechanism of BZD9L1-induced cell death.
  • BZD9L1 modulated cancer signaling pathways differently based on CRC mutation profiles.
  • The inhibitor demonstrated cytotoxic effects against metastatic CRC cell lines.

Conclusions:

  • BZD9L1 exhibits potent anticancer activities in colorectal cancer.
  • BZD9L1 induces apoptosis and inhibits key cancer hallmarks in CRC cells.
  • BZD9L1 represents a promising therapeutic strategy for colorectal cancer treatment.
Keywords:
BZD9L1colorectal cancersirtuintargeted therapy

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