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CP-225,917 and CP-263,114, novel Ras farnesylation inhibitors from an unidentified fungus. I. Taxonomy, fermentation, isolation, and biochemical properties.

Publication ,  Journal Article
Dabrah, TT; Harwood, HJ; Huang, LH; Jankovich, ND; Kaneko, T; Li, JC; Lindsey, S; Moshier, PM; Subashi, TA; Therrien, M; Watts, PC
Published in: The Journal of antibiotics
January 1997

During the course of our screening for squalene synthase inhibitors and Ras farnesylation inhibitors, a novel fungal culture was discovered to produce two structurally unique compounds, CP-225,917 and CP-263,114, as well as zaragozic acid A (squalestatin I). The two compounds are characterized by a bicyclo[4.3.1]dec-1,6-diene core plus two extended alkyl chains. CP-225,917 and CP-263,114 inhibit Ras farnesyl transferase from rat brain with IC50 values of 6 microM and 20 microM, respectively. CP-225,917 inhibits squalene synthase with an IC50 value of 43 microM and CP-263,114 with an IC50 of 160 microM. The producing organism, though not fully classified, exhibits the characteristics of a sterile Phoma species.

Duke Scholars

Published In

The Journal of antibiotics

ISSN

0021-8820

Publication Date

January 1997

Volume

50

Issue

1

Start / End Page

1 / 7

Location

japan

Related Subject Headings

  • Microbiology
  • Medicinal & Biomolecular Chemistry
  • 3214 Pharmacology and pharmaceutical sciences
  • 3107 Microbiology
  • 1115 Pharmacology and Pharmaceutical Sciences
  • 0605 Microbiology
 

Citation

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Dabrah, T. T., Harwood, H. J., Huang, L. H., Jankovich, N. D., Kaneko, T., Li, J. C., … Watts, P. C. (1997). CP-225,917 and CP-263,114, novel Ras farnesylation inhibitors from an unidentified fungus. I. Taxonomy, fermentation, isolation, and biochemical properties. The Journal of Antibiotics, 50(1), 1–7.
Dabrah, T. T., H. J. Harwood, L. H. Huang, N. D. Jankovich, T. Kaneko, J. C. Li, S. Lindsey, et al. “CP-225,917 and CP-263,114, novel Ras farnesylation inhibitors from an unidentified fungus. I. Taxonomy, fermentation, isolation, and biochemical properties.The Journal of Antibiotics 50, no. 1 (January 1997): 1–7.
Dabrah TT, Harwood HJ, Huang LH, Jankovich ND, Kaneko T, Li JC, et al. CP-225,917 and CP-263,114, novel Ras farnesylation inhibitors from an unidentified fungus. I. Taxonomy, fermentation, isolation, and biochemical properties. The Journal of antibiotics. 1997 Jan;50(1):1–7.
Dabrah TT, Harwood HJ, Huang LH, Jankovich ND, Kaneko T, Li JC, Lindsey S, Moshier PM, Subashi TA, Therrien M, Watts PC. CP-225,917 and CP-263,114, novel Ras farnesylation inhibitors from an unidentified fungus. I. Taxonomy, fermentation, isolation, and biochemical properties. The Journal of antibiotics. 1997 Jan;50(1):1–7.

Published In

The Journal of antibiotics

ISSN

0021-8820

Publication Date

January 1997

Volume

50

Issue

1

Start / End Page

1 / 7

Location

japan

Related Subject Headings

  • Microbiology
  • Medicinal & Biomolecular Chemistry
  • 3214 Pharmacology and pharmaceutical sciences
  • 3107 Microbiology
  • 1115 Pharmacology and Pharmaceutical Sciences
  • 0605 Microbiology