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Inhibitors of EYA3 Protein in Ewing Sarcoma

Fahad Hassan Shah1, Song Ja Kim1

  • 1Department of Biological Sciences, College of Natural Sciences, Kongju National University, Gongju 32588, Republic of Korea.

Asian Pacific Journal of Cancer Prevention : APJCP
|May 28, 2022
PubMed
Abstract

Insights

Researchers identified Sorbifolin and 1,7-Dihydroxy-3-methylanthracene-9.10-dione as potential inhibitors for Eyes absent homolog 3 (EYA3). These compounds show promise for treating Ewing sarcoma (EWS) by targeting the EWSR1/FLI1 fusion gene

Area of Science:

  • Oncology
  • Molecular Biology
  • Pharmacology

Background:

  • Ewing sarcoma (EWS) is a highly malignant bone tumor driven by the EWSR1/FLI1 gene fusion.
  • The EWSR1/FLI1 fusion protein activates Eyes absent homolog 3 (EYA3), promoting tumor growth and angiogenesis.
  • EYA3 is recognized as a critical therapeutic target for EWS treatment.

Purpose of the Study:

  • To identify potential EYA3 inhibitors using medicinal compounds.
  • To discover novel therapeutic strategies for Ewing sarcoma.

Main Methods:

  • In silico screening of over 2,000 medicinal compounds from the NuBBE database using PyRX software.
  • Evaluation of compound structural information and binding affinity to EYA3 active residues.

Main Results:

  • Sorbifolin and 1,7-Dihydroxy-3-methylanthracene-9.10-dione demonstrated significant binding affinity to EYA3.
  • These compounds exhibited adequate toxicity and induced cytotoxicity in EWS cells.
  • The identified compounds were capable of regulating gene expression influenced by EWSR1/FLI1.

Conclusions:

  • Sorbifolin and 1,7-Dihydroxy-3-methylanthracene-9.10-dione are promising drug candidates for EWS treatment.
  • Further in vitro testing is recommended to validate their therapeutic potential.
Keywords:
Ewing sarcomaEyes Absent Homolog-3In silico Gene expressionMedicinal CompoundsVirtual screening

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