Recent advances in the development of mammalian geranylgeranyl diphosphate synthase inhibitors

Staci L. Haney, Veronica S. Wills, David F. Wiemer, Sarah A. Holstein

Research output: Contribution to journalReview articlepeer-review

24 Scopus citations


The enzyme geranylgeranyl diphosphate synthase (GGDPS) catalyzes the synthesis of the 20-carbon isoprenoid geranylgeranyl diphosphate (GGPP). GGPP is the isoprenoid donor for protein geranylgeranylation reactions catalyzed by the enzymes geranylgeranyl transferase (GGTase) I and II. Inhibitors of GGDPS result in diminution of protein geranylgeranylation through depletion of cellular GGPP levels, and there has been interest in GGDPS inhibitors as potential anti-cancer agents. Here we discuss recent advances in the development of GGDPS inhibitors, including insights gained by structure-function relationships, and review the preclinical data that support the continued development of this novel class of drugs.

Original languageEnglish (US)
Article number886
Issue number6
StatePublished - Jun 2017


  • Geranylgeranyl diphosphate synthase
  • Geranylgeranylation
  • Inhibitors
  • Isoprenoid

ASJC Scopus subject areas

  • Analytical Chemistry
  • Chemistry (miscellaneous)
  • Molecular Medicine
  • Pharmaceutical Science
  • Drug Discovery
  • Physical and Theoretical Chemistry
  • Organic Chemistry


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