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2-Aminothiazole-4-carboxamides Enhance Readthrough of Premature Termination Codons by Aminoglycosides

Safwat M Rabea1, Alireza Baradaran-Heravi2, Aruna D Balgi2

  • 1Faculty of Pharmaceutical Sciences, University of British Columbia, 2405 Wesbrook Mall, Vancouver, British Columbia V6T 1Z3, Canada.

ACS Medicinal Chemistry Letters
|May 18, 2019
PubMed

Insights

Researchers identified novel compounds that enhance the readthrough of premature termination codons (PTCs). These compounds, when combined with G418, show potential for treating genetic diseases and cancers caused by PTCs.

Area of Science:

  • Biochemistry
  • Genetics
  • Pharmacology

Background:

  • Nonsense mutations lead to premature termination codons (PTCs), causing rare genetic diseases and cancers.
  • Aminoglycosides can promote readthrough of PTCs but are limited by inefficiency and toxicity.

Purpose of the Study:

  • To discover novel compounds that enhance premature termination codon readthrough (PTCR) in combination with existing drugs.
  • To identify chemical structures that potentiate the therapeutic effects of G418 for PTC-related disorders.

Main Methods:

  • Screening of novel 2-aminothiazole-4-carboxamide derivatives in a TP53 gene assay.
  • Assessing the potentiation of G418-induced PTCR in human HDQ-P1 cells.
  • Identifying lead compounds with specific structural motifs.

Main Results:

  • Six novel 2-aminothiazole-4-carboxamide derivatives were identified that potentiate G418-induced PTCR.
  • The two most effective compounds feature a 4-indazole motif and a hydrophobic aryl substituent.
  • These compounds significantly enhance readthrough efficiency at PTCs.

Conclusions:

  • Novel compounds can enhance the efficacy of G418 for premature termination codon readthrough.
  • The identified compounds are promising tools for further research into PTC-related disease therapies.
  • Further investigation into aminoglycoside-induced PTCR holds therapeutic potential.

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