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  2. Research Domains
  3. Biomedical And Clinical Sciences
  4. Oncology And Carcinogenesis
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  6. A Computational And In Vitro Appraisal Of Ostarine To Target Androgen Receptor In Glioma C6 Cells.
  1. Home
  2. Research Domains
  3. Biomedical And Clinical Sciences
  4. Oncology And Carcinogenesis
  5. Molecular Targets
  6. A Computational And In Vitro Appraisal Of Ostarine To Target Androgen Receptor In Glioma C6 Cells.

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A Computational and In Vitro Appraisal of Ostarine to Target Androgen Receptor in Glioma C6 Cells.

Satvika Sharma1, Sandeep Saini1,2, Vijayta Dani Chadha3

  • 1Department of Biophysics, Panjab University, Chandigarh, India.

Cell Biochemistry and Biophysics
|June 13, 2025

View abstract on PubMed

Summary
This summary is machine-generated.

Selective androgen receptor modulators (SARMs) show promise for glioma treatment. Ostarine (MK-2866) effectively inhibits glioma C6 cells by targeting the androgen receptor (AR), offering a potential new therapy.

Keywords:
Androgen receptorGliomaOstarineSARM

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Area of Science:

  • Neuro-oncology
  • Molecular Endocrinology
  • Cancer Therapeutics

Background:

  • Gliomas are primary brain tumors originating from glial cells, representing the majority of central nervous system (CNS) malignancies.
  • Androgen receptor (AR) signaling is implicated in tumor growth and altered in various cancers, including glioma.
  • Targeting AR for glioma treatment is of interest, but traditional antagonists are limited by glioma's heterogeneity.

Purpose of the Study:

  • To investigate the potential of selective androgen receptor modulators (SARMs) as a therapeutic strategy for glioma.
  • To evaluate the binding affinity and efficacy of SARMs against glioma cells.
  • To identify a SARM with promising anti-glioma activity.

Main Methods:

  • Computational screening of 20 SARMs using AutoDock vina for binding affinity analysis.
  • Molecular dynamics (MD) simulations and MM-PBSA analysis to assess binding stability.
  • In vitro assays including IC50 determination, cell viability, migration, and invasion assays using C6 glioma cells.
  • Main Results:

    • Ostarine (MK-2866) demonstrated high binding affinity (-9.4 Kcal/mol) to the AR N-terminal domain (NTD).
    • MD simulations and MM-PBSA confirmed strong and stable binding of Ostarine to AR.
    • Ostarine showed a twofold increase in C6 cell inhibition compared to Bicalutamide and reduced cell viability, migration, and invasion.

    Conclusions:

    • Ostarine acts as a potent AR antagonist with significant chemotherapeutic potential against glioma.
    • SARMs, exemplified by Ostarine, represent a promising therapeutic avenue for managing glioma propagation.
    • Further studies are warranted to explore Ostarine's efficacy in more aggressive glioma models.