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Determination of the Apoptotic Effect and Molecular Docking of Benzamide Derivative XT5 in K562 Cells

Tulin Ozkan1, Yalda Hekmatshoar1, Tugba Ertan-Bolelli2

  • 1Department of Medical Biology, School of Medicine, Ankara University, Ankara, Turkey.

Anti-Cancer Agents in Medicinal Chemistry
|January 5, 2018
PubMed
Abstract

Insights

The novel compound XT5 shows significant anticancer effects and enhances imatinib efficacy in Chronic Myeloid Leukemia (CML) cells. This combination therapy offers a promising strategy to overcome imatinib resistance in CML patients.

Area of Science:

  • Oncology
  • Pharmacology
  • Molecular Biology

Background:

  • Imatinib is a first-line treatment for Chronic Myeloid Leukemia (CML).
  • Therapy failure and resistance to imatinib are significant clinical challenges.
  • Novel drug combinations are being explored to improve CML treatment outcomes.

Purpose of the Study:

  • To investigate the antileukemic and apoptotic effects of XT5 and XT2B, alone and in combination with imatinib.
  • To evaluate these effects in both imatinib-sensitive (K562S) and imatinib-resistant (K562R) CML cell lines.
  • To explore the potential of XT5 as a new anticancer agent and combination therapy for CML.

Main Methods:

  • In vitro cytotoxicity assessed using MTT assay.
  • Apoptotic effects evaluated via Annexin V flow cytometry, caspase activation assays, and RT-PCR.
  • Molecular docking studies performed using AutoDock Vina to analyze drug-target interactions.

Main Results:

  • XT5 demonstrated significant antiproliferative and pro-apoptotic effects on CML cell lines.
  • Combination of XT5 with imatinib enhanced cytotoxicity and apoptosis induction (Annexin V binding, caspase 3/7 activation).
  • XT5 treatment increased the expression of pro-apoptotic genes (BAX, BAD, BIM) and showed favorable molecular interactions with the BCR-ABL kinase receptor.

Conclusions:

  • XT5 is a potential candidate for a new anticancer drug.
  • Combining XT5 with imatinib represents a viable strategy to overcome imatinib resistance in CML.
  • Further research into XT5 and its combinations is warranted for CML treatment.
Keywords:
CMLK562apoptosisbenzamideimatinib resistance.

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