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Utilizing Functional Genomics Screening to Identify Potentially Novel Drug Targets in Cancer Cell Spheroid Cultures
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Ras superfamily GEFs and GAPs: validated and tractable targets for cancer therapy?

Dominico Vigil1, Jacqueline Cherfils, Kent L Rossman

  • 1University of North Carolina at Chapel Hill, Lineberger Comprehensive Cancer Center, Department of Pharmacology, Chapel Hill, North Carolina 27599, USA.

Nature Reviews. Cancer
|November 25, 2010
PubMed

Insights

Aberrant Ras GTPase activity drives cancer. Regulatory proteins, guanine nucleotide exchange factors (GEFs) and GTPase-activating proteins (GAPs), are key to GTPase function and represent potential cancer drug targets.

Area of Science:

  • Molecular biology
  • Oncology
  • Biochemistry

Background:

  • Ras superfamily small GTPases are crucial regulators of cellular processes.
  • Aberrant GTPase activity is increasingly linked to human cancer development.

Purpose of the Study:

  • To review the role of guanine nucleotide exchange factors (GEFs) and GTPase-activating proteins (GAPs) in cancer.
  • To assess the potential of GEFs and GAPs as therapeutic targets in oncology.

Main Methods:

  • Literature review of studies on Ras GTPases, GEFs, and GAPs in cancer.
  • Analysis of the association between GEF/GAP deregulation and cancer pathogenesis.
  • Evaluation of the druggability of GEFs and GAPs for cancer treatment.

Main Results:

  • GEFs and GAPs are critical regulators of GTPase activity, controlling the GDP-GTP switch.
  • Deregulation of GEF and GAP expression or activity is a common mechanism in cancer.
  • Many GEFs and GAPs show promise as targets for novel cancer therapeutics.

Conclusions:

  • Targeting GEFs and GAPs offers a promising strategy for developing new cancer treatments.
  • Further research into the specific roles and druggability of these regulatory proteins is warranted.

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