Skip to main content

Cell-Based Methods for the Identification of MYC-Inhibitory Small Molecules

  • Protocol
  • First Online:
The Myc Gene

Part of the book series: Methods in Molecular Biology ((MIMB,volume 1012))

  • 2520 Accesses

Abstract

Oncoproteins encoded by dominant oncogenes have long been considered as targets for chemotherapeutic intervention. However, oncogenic transcription factors have often been dismissed as “undruggable.” Members of Myc family of transcription factors have been identified as promising targets for cancer chemotherapy in multiple publications reporting the requirement of Myc proteins for maintenance of almost every type of tumor. Here, we describe cell-based approaches to identify c-Myc small molecule inhibitors by screening complex libraries of diverse small molecules based on Myc functionality and specificity.

This is a preview of subscription content, log in via an institution to check access.

Access this chapter

Protocol
USD 49.95
Price excludes VAT (USA)
  • Available as PDF
  • Read on any device
  • Instant download
  • Own it forever
eBook
USD 84.99
Price excludes VAT (USA)
  • Available as EPUB and PDF
  • Read on any device
  • Instant download
  • Own it forever
Softcover Book
USD 119.00
Price excludes VAT (USA)
  • Compact, lightweight edition
  • Dispatched in 3 to 5 business days
  • Free shipping worldwide - see info
Hardcover Book
USD 109.99
Price excludes VAT (USA)
  • Durable hardcover edition
  • Dispatched in 3 to 5 business days
  • Free shipping worldwide - see info

Tax calculation will be finalised at checkout

Purchases are for personal use only

Institutional subscriptions

References

  1. Dang CV, O’Donnell KA, Zeller KI, Nguyen T, Osthus RC, Li F (2006) The c-Myc target gene network. Semin Cancer Biol 16:253–264

    Article  PubMed  CAS  Google Scholar 

  2. Dang CV (2012) MYC on the path to cancer. Cell 149:22–35

    Article  PubMed  CAS  Google Scholar 

  3. Malynn BA, de Alboran IM, O’Hagan RC, Bronson R, Davidson L, DePinho RA, Alt FW (2000) N-myc can functionally replace c-myc in murine development, cellular growth, and differentiation. Genes Dev 14:1390–1399

    PubMed  CAS  Google Scholar 

  4. Hermeking H (2003) The MYC oncogene as a cancer drug target. Curr Cancer Drug Targets 3:163–175

    Article  PubMed  CAS  Google Scholar 

  5. Arvanitis C, Felsher DW (2006) Conditional transgenic models define how MYC initiates and maintains tumorigenesis. Semin Cancer Biol 16:313–317

    Article  PubMed  CAS  Google Scholar 

  6. Schulte JH, Lindner S, Bohrer A, Maurer J, De Preter K, Lefever S, Heukamp L, Schulte S, Molenaar J, Versteeg R, Thor T, Künkele A, Vandesompele J, Speleman F, Schorle H, Eggert A, Schramm A (2013) MYCN and ALKF1174L are sufficient to drive neuroblastoma development from neural crest progenitor cells. Oncogene 32(8):1059–65

    Article  PubMed  CAS  Google Scholar 

  7. Soucek L, Whitfield J, Martins CP, Finch AJ, Murphy DJ, Sodir NM, Karnezis AN, Swigart LB, Nasi S, Evan GI (2008) Modelling Myc inhibition as a cancer therapy. Nature 455:679–683

    Article  PubMed  CAS  Google Scholar 

  8. Vita M, Henriksson M (2006) The Myc oncoprotein as a therapeutic target for human cancer. Semin Cancer Biol 16:318–330

    Article  PubMed  CAS  Google Scholar 

  9. Mateyak MK, Obaya AJ, Adachi S, Sedivy JM (1999) Phenotypes of c-Myc-deficient rat fibroblasts isolated by targeted homologous recombination. Cell Growth Differ 8:1039–1048

    Google Scholar 

  10. Wang H, Mannava S, Grachtchouk V, Zhuang D, Soengas MS, Gudkov AV, Prochownik EV, Nikiforov MA (2008) c-Myc depletion inhibits proliferation of human tumor cells at various stages of the cell cycle. Oncogene 27:1905–1915

    Article  PubMed  CAS  Google Scholar 

Download references

Acknowledgments

This work was supported by NIH R01 CA120244 and ACS RSG-10-121-01 grants to M.A.N., and by CINSW and NHMRC grants to M.H. and M.D.N.

Author information

Authors and Affiliations

Authors

Editor information

Editors and Affiliations

Rights and permissions

Reprints and permissions

Copyright information

© 2013 Springer Science+Business Media, LLC

About this protocol

Cite this protocol

Burkhart, C.A., Haber, M., Norris, M.D., Gudkov, A.V., Nikiforov, M.A. (2013). Cell-Based Methods for the Identification of MYC-Inhibitory Small Molecules. In: Soucek, L., Sodir, N. (eds) The Myc Gene. Methods in Molecular Biology, vol 1012. Humana Press, Totowa, NJ. https://doi.org/10.1007/978-1-62703-429-6_18

Download citation

  • DOI: https://doi.org/10.1007/978-1-62703-429-6_18

  • Published:

  • Publisher Name: Humana Press, Totowa, NJ

  • Print ISBN: 978-1-62703-428-9

  • Online ISBN: 978-1-62703-429-6

  • eBook Packages: Springer Protocols

Publish with us

Policies and ethics