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New fungal metabolite geranylgeranyltransferase inhibitors with antifungal activity.

Publication ,  Journal Article
Singh, SB; Kelly, R; Guan, Z; Polishook, JD; Domrowski, AW; Collado, J; Gonzalez, A; Pelaez, F; Register, E; Kelly, TM; Bonfiglio, C; Williamson, JM
Published in: Nat Prod Res
December 2005

Geranylgeranyltransferase I (GGTase I) catalyzes the post-translational transfer of lyophilic diterpenoid geranylgeranyl to the cysteine residue of proteins terminating with a CaaX motif such as Rho1p and Cdc42p. It has been shown that GGTase I activity is essential for viability of Saccharomyces cerevisiae and hence its inhibition is a potential antifungal target. From natural product screening, a number of azaphilones including one novel analog were isolated as broad-spectrum inhibitors of GGTase I. Isolation, structure elucidation, GGTase I inhibitory activities and antifungal activities of these compounds are described.

Duke Scholars

Published In

Nat Prod Res

DOI

ISSN

1478-6419

Publication Date

December 2005

Volume

19

Issue

8

Start / End Page

739 / 747

Location

England

Related Subject Headings

  • Saccharomyces cerevisiae Proteins
  • Saccharomyces cerevisiae
  • Pigments, Biological
  • Medicinal & Biomolecular Chemistry
  • Enzyme Inhibitors
  • Benzopyrans
  • Antifungal Agents
  • Alkyl and Aryl Transferases
 

Citation

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MLA
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Singh, S. B., Kelly, R., Guan, Z., Polishook, J. D., Domrowski, A. W., Collado, J., … Williamson, J. M. (2005). New fungal metabolite geranylgeranyltransferase inhibitors with antifungal activity. Nat Prod Res, 19(8), 739–747. https://doi.org/10.1080/1478641042000334715
Singh, Sheo B., Rosemarie Kelly, Ziqiang Guan, Jon D. Polishook, Anne W. Domrowski, Javier Collado, Antonio Gonzalez, et al. “New fungal metabolite geranylgeranyltransferase inhibitors with antifungal activity.Nat Prod Res 19, no. 8 (December 2005): 739–47. https://doi.org/10.1080/1478641042000334715.
Singh SB, Kelly R, Guan Z, Polishook JD, Domrowski AW, Collado J, et al. New fungal metabolite geranylgeranyltransferase inhibitors with antifungal activity. Nat Prod Res. 2005 Dec;19(8):739–47.
Singh, Sheo B., et al. “New fungal metabolite geranylgeranyltransferase inhibitors with antifungal activity.Nat Prod Res, vol. 19, no. 8, Dec. 2005, pp. 739–47. Pubmed, doi:10.1080/1478641042000334715.
Singh SB, Kelly R, Guan Z, Polishook JD, Domrowski AW, Collado J, Gonzalez A, Pelaez F, Register E, Kelly TM, Bonfiglio C, Williamson JM. New fungal metabolite geranylgeranyltransferase inhibitors with antifungal activity. Nat Prod Res. 2005 Dec;19(8):739–747.
Journal cover image

Published In

Nat Prod Res

DOI

ISSN

1478-6419

Publication Date

December 2005

Volume

19

Issue

8

Start / End Page

739 / 747

Location

England

Related Subject Headings

  • Saccharomyces cerevisiae Proteins
  • Saccharomyces cerevisiae
  • Pigments, Biological
  • Medicinal & Biomolecular Chemistry
  • Enzyme Inhibitors
  • Benzopyrans
  • Antifungal Agents
  • Alkyl and Aryl Transferases