Skip to main content

Thank you for visiting nature.com. You are using a browser version with limited support for CSS. To obtain the best experience, we recommend you use a more up to date browser (or turn off compatibility mode in Internet Explorer). In the meantime, to ensure continued support, we are displaying the site without styles and JavaScript.

  • In Brief
  • Published:

Therapeutic resistance

Blocking the gatekeeper

Nature Reviews Cancer volume 14, page 766 (2014)Cite this article

Subjects

Access through your institution
Buy or subscribe

Tan et al. have identified covalent inhibitors of the fibroblast growth factor receptor (FGFR) that can block the proliferation of cells expressing FGFR1 or FGFR2 gatekeeper mutants, which are resistant to the first generation FGFR inhibitors that are being tested clinically for a variety of cancers. They used structure-based drug design to develop inhibitors that covalently target cysteine residues in the ATP binding pocket.

This is a preview of subscription content, access via your institution

Access options

Access through your institution

Buy this article

  • Purchase on SpringerLink
  • Instant access to full article PDF
Buy now

Prices may be subject to local taxes which are calculated during checkout

References

  1. Tan, L. et al. Development of covalent inhibitors that can overcome resistance to first-generation FGFR kinase inhibitors. Proc. Natl Acad. Sci. USA http://dx.doi.org/10.1073/pnas.1403438111 (2014)

Download references

Authors
  1. Sarah Seton-Rogers
    View author publications

    Search author on:PubMed Google Scholar

Rights and permissions

Reprints and permissions

About this article

Check for updates. Verify currency and authenticity via CrossMark

Cite this article

Seton-Rogers, S. Blocking the gatekeeper. Nat Rev Cancer 14, 766 (2014). https://doi.org/10.1038/nrc3871

Download citation

  • Published:

  • Issue date:

  • DOI: https://doi.org/10.1038/nrc3871

Search

Advanced search

Quick links

Nature Briefing

Sign up for the Nature Briefing newsletter — what matters in science, free to your inbox daily.

Get the most important science stories of the day, free in your inbox. Sign up for Nature Briefing