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

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Date Issued:
1996
Title: A cembranolide diterpene farnesyl protein transferase inhibitor from the marine soft coral Lobophytum cristagalli.
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Name(s): Coval, S. J., creator
Patton, R. W., creator
Petrin, J. M., creator
James, L., creator
Rothofsky, M. L., creator
Lin, S. L., creator
Patel, Mahesh, creator
Reed, John K., creator
McPhail, A. T., creator
Bishop, W. R., creator
Type of Resource: text
Genre: Article
Issuance: single unit
Date Issued: 1996
Publisher: Elsevier B.V.
Extent: 5 p.
Physical Description: pdf
Language(s): English
Identifier: 3331913 (digitool), FADT3331913 (IID), fau:6151 (fedora), 10.1016/0960-894X(96)00142-4 (doi)
Note(s): 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.
This manuscript is an author version with the final publication available at http://www.sciencedirect.com/science/journal/0960894X and may be cited as: Coval, S. J., Patton, R. W., Petrin, J. M., James, L., Rothofsky, M. L., Lin, S. L., Patel, M., Reed, J. K., McPhail, A. T., & Bishop, W. R. (1996). A cembranolide diterpene farnesyl protein transferase inhibitor from the marine soft coral Lobophytum cristagalli. Bioorganic & Medicinal Chemistry Letters, 6(7), 909-912. doi:10.1016/0960-894X(96)00142-4
Florida Atlantic University. Harbor Branch Oceanographic Institute contribution #1131.
Subject(s): Corals
Alcyoniidae
Ras proteins
Diterpenes
Antineoplastic agents
Persistent Link to This Record: http://purl.flvc.org/FCLA/DT/3331913
Links: http://dx.doi.org/10.1016/0960-894X(96)00142-4
Restrictions on Access: ©1996 Elsevier B.V.
Host Institution: FAU