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 article

7 Citations (Scopus)

Abstract

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
JournalMolecules
Volume22
Issue number6
DOIs
StatePublished - Jun 1 2017

Fingerprint

Farnesyltranstransferase
diphosphates
inhibitors
Protein Prenylation
Terpenes
Enzymes
Transferases
enzymes
Proteins
Carbon
proteins
Pharmaceutical Preparations
depletion
drugs
geranylgeranyl pyrophosphate
cancer
Neoplasms
carbon
synthesis

Keywords

  • Geranylgeranyl diphosphate synthase
  • Geranylgeranylation
  • Inhibitors
  • Isoprenoid

ASJC Scopus subject areas

  • Medicine(all)
  • Organic Chemistry

Cite this

Recent advances in the development of mammalian geranylgeranyl diphosphate synthase inhibitors. / Haney, Staci L.; Wills, Veronica S.; Wiemer, David F.; Holstein, Sarah A.

In: Molecules, Vol. 22, No. 6, 886, 01.06.2017.

Research output: Contribution to journalReview article

Haney, Staci L. ; Wills, Veronica S. ; Wiemer, David F. ; Holstein, Sarah A. / Recent advances in the development of mammalian geranylgeranyl diphosphate synthase inhibitors. In: Molecules. 2017 ; Vol. 22, No. 6.
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