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A cembranolide diterpene farnesyl protein transferase inhibitor from the marine soft coral Lobophytum cristagalli

Publication ,  Journal Article
Coval, SJ; Patton, RW; Petrin, JM; James, L; Rothofsky, ML; Lin, SL; Patel, M; Reed, JK; McPhail, AT; Bishop, WR
Published in: Bioorganic and Medicinal Chemistry Letters
April 9, 1996
Published version (DOI)

A previously described cembranolide diterpene from Lobophytum cristagalli was identified as a potent (IC50 0.15 μM) inhibitor of farnesyl protein transferase (FPT). The compound showed selectivity for FPT as compared to the closely related enzyme geranylgeranyl protein transferase-1 (IC50 5.3 μM). Kinetic evaluation suggests that this compound competes with the protein/peptide farnesyl acceptor substrate, and not with farnesyl pyrophosphate for inhibition of FPT.

Duke Scholars

Andrew T. McPhail
Author Andrew T. McPhail Chemistry

Published In

Bioorganic and Medicinal Chemistry Letters

DOI

10.1016/0960-894X(96)00142-4

ISSN

0960-894X

Publication Date

April 9, 1996

Volume

6

Issue

7

Start / End Page

909 / 912

Related Subject Headings

  • Medicinal & Biomolecular Chemistry
  • 3405 Organic chemistry
  • 3404 Medicinal and biomolecular chemistry
  • 1115 Pharmacology and Pharmaceutical Sciences
  • 0305 Organic Chemistry
  • 0304 Medicinal and Biomolecular Chemistry
 

Citation

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Coval, S. J., Patton, R. W., Petrin, J. M., James, L., Rothofsky, M. L., Lin, S. L., … Bishop, W. R. (1996). A cembranolide diterpene farnesyl protein transferase inhibitor from the marine soft coral Lobophytum cristagalli. Bioorganic and Medicinal Chemistry Letters, 6(7), 909–912. https://doi.org/10.1016/0960-894X(96)00142-4
Coval, S. J., R. W. Patton, J. M. Petrin, L. James, M. L. Rothofsky, S. L. Lin, M. Patel, J. K. Reed, A. T. McPhail, and W. R. Bishop. “A cembranolide diterpene farnesyl protein transferase inhibitor from the marine soft coral Lobophytum cristagalli.” Bioorganic and Medicinal Chemistry Letters 6, no. 7 (April 9, 1996): 909–12. https://doi.org/10.1016/0960-894X(96)00142-4.
Coval SJ, Patton RW, Petrin JM, James L, Rothofsky ML, Lin SL, et al. A cembranolide diterpene farnesyl protein transferase inhibitor from the marine soft coral Lobophytum cristagalli. Bioorganic and Medicinal Chemistry Letters. 1996 Apr 9;6(7):909–12.
Coval, S. J., et al. “A cembranolide diterpene farnesyl protein transferase inhibitor from the marine soft coral Lobophytum cristagalli.” Bioorganic and Medicinal Chemistry Letters, vol. 6, no. 7, Apr. 1996, pp. 909–12. Scopus, doi:10.1016/0960-894X(96)00142-4.
Coval SJ, Patton RW, Petrin JM, James L, Rothofsky ML, Lin SL, Patel M, Reed JK, McPhail AT, Bishop WR. A cembranolide diterpene farnesyl protein transferase inhibitor from the marine soft coral Lobophytum cristagalli. Bioorganic and Medicinal Chemistry Letters. 1996 Apr 9;6(7):909–912.
Journal cover image

Published In

Bioorganic and Medicinal Chemistry Letters

DOI

10.1016/0960-894X(96)00142-4

ISSN

0960-894X

Publication Date

April 9, 1996

Volume

6

Issue

7

Start / End Page

909 / 912

Related Subject Headings

  • Medicinal & Biomolecular Chemistry
  • 3405 Organic chemistry
  • 3404 Medicinal and biomolecular chemistry
  • 1115 Pharmacology and Pharmaceutical Sciences
  • 0305 Organic Chemistry
  • 0304 Medicinal and Biomolecular Chemistry