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A Rapid Screening Workflow to Identify Potential Combination Therapy for GBM using Patient-Derived Glioma Stem Cells
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Multi-Targeting Approach in Glioblastoma Using Computer-Assisted Drug Discovery Tools to Overcome the Blood-Brain

Catarina Franco1,2, Samina Kausar1,2, Margarida F B Silva2,3

  • 1LASIGE, Department of Informatics, Faculty of Sciences, Universidade de Lisboa, Campo Grande, 1749-016 Lisboa, Portugal.

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Researchers identified novel drug candidates targeting both epidermal growth factor receptor (EGFR) and PI3Kp110β pathways to overcome glioblastoma resistance and blood-brain barrier challenges. These dual inhibitors show promising efficacy and safety for treating brain tumors.

Keywords:
blood–brain barrierdual-targetingepidermal growth factor receptorglioblastomaphosphatidylinositol-3-kinasequantitative structure–activity relationship modelsvirtual screening

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Area of Science:

  • Oncology
  • Pharmacology
  • Neuroscience

Background:

  • Glioblastoma exhibits upregulated epidermal growth factor receptor (EGFR), a key therapeutic target.
  • Compensatory signaling pathways and the blood-brain barrier (BBB) contribute to therapeutic resistance and limit drug efficacy.
  • Targeting both EGFR and PI3Kp110β simultaneously offers a potential strategy to overcome resistance.

Purpose of the Study:

  • To discover novel inhibitors of the EGFR/PI3Kp110β pathway with favorable ADMET properties and BBB permeability.
  • To develop multi-targeting agents for glioblastoma treatment, addressing resistance mechanisms.
  • To validate potential drug candidates using in vitro models of the BBB and glioblastoma.

Main Methods:

  • Quantitative structure-activity relationship (QSAR) modeling and structure-based virtual screening were employed.
  • ADMET properties and BBB permeability were assessed computationally.
  • In vitro validation involved human BBB models, BBB-glioma co-cultures, and glioblastoma cell lines (U87MG).

Main Results:

  • 27 potential inhibitors were identified (18 EGFR, 6 PI3Kp110β, 3 dual inhibitors).
  • Six molecules demonstrated significant glioblastoma cell viability reduction (40-99%), with dual inhibitors showing the greatest effect.
  • Three molecules (one EGFR, two PI3Kp110β) showed safety for BBB endothelial cells and successfully crossed the BBB in vitro.

Conclusions:

  • Novel drug candidates targeting EGFR and PI3Kp110β pathways were discovered.
  • Dual inhibitors exhibit potent anti-glioma activity and potential for BBB penetration.
  • These findings present promising therapeutic options for glioblastoma treatment, overcoming resistance and BBB limitations.