ARC (NSC 188491) has identical activity to Sangivamycin (NSC 65346) including inhibition of both P-TEFb and PKC
2009

ARC and Sangivamycin: Similarities in Cancer Cell Activity

publication Evidence: moderate

Author Information

Author(s): Stockwin Luke H, Yu Sherry X, Stotler Howard, Hollingshead Melinda G, Newton Dianne L

Primary Institution: Developmental Therapeutics Program, SAIC-Frederick Inc., NCI- Frederick, Frederick, MD, USA

Hypothesis

Does ARC (NSC 188491) exhibit similar anti-cancer activity to Sangivamycin (NSC 65346)?

Conclusion

ARC shows similar in vitro biological activity to Sangivamycin but requires further studies before clinical development.

Supporting Evidence

  • ARC and Sangivamycin both inhibit protein kinase C and P-TEFb.
  • ARC shows similar cytotoxicity profiles to Sangivamycin in various cancer cell lines.
  • Both drugs induce apoptosis and block the cell cycle in a similar manner.

Takeaway

ARC is a new cancer drug that works like an older drug called Sangivamycin, but we need to do more tests before using it in people.

Methodology

The study used structure-based homology searches, viability assays, cell cycle and apoptosis assays, gene-expression analysis, and kinase inhibition assays.

Limitations

ARC was found to be inactive in several xenograft models, likely due to rapid serum clearance.

Digital Object Identifier (DOI)

10.1186/1471-2407-9-63

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