ACS Publications. Most Trusted. Most Cited. Most Read
My Activity

A New Class of Highly Potent Farnesyl Diphosphate-Competitive Inhibitors of Farnesyltransferase

View Author Information
Drug Discovery Research Laboratories and Biomedical Research Laboratories, Tsukuba Research Institute, Banyu Pharmaceutical Co. Ltd., Okubo 3 Tsukuba 300-26, Japan
Cite this: J. Med. Chem. 1998, 41, 2, 143–147
Publication Date (Web):January 15, 1998
Copyright © 1998 American Chemical Society

    Article Views





    Other access options
    Supporting Info (1)»

    Note: In lieu of an abstract, this is the article's first page.

    Free first page

    Read this article

    To access this article, please review the available access options below.

    Get instant access

    Purchase Access

    Read this article for 48 hours. Check out below using your ACS ID or as a guest.


    Access through Your Institution

    You may have access to this article through your institution.

    Your institution does not have access to this content. You can change your affiliated institution below.


    In papers with more than one author, the asterisk indicates the name of the author to whom inquiries about the paper should be addressed.

    Supporting Information Available

    Jump To

    Experimental data for 2 and 18 (1 page). Ordering information is given on any current masthead page.

    Terms & Conditions

    Most electronic Supporting Information files are available without a subscription to ACS Web Editions. Such files may be downloaded by article for research use (if there is a public use license linked to the relevant article, that license may permit other uses). Permission may be obtained from ACS for other uses through requests via the RightsLink permission system:

    Cited By

    This article is cited by 23 publications.

    1. Mitchell J. Polley,, David A. Winkler, and, Frank R. Burden. Broad-Based Quantitative Structure−Activity Relationship Modeling of Potency and Selectivity of Farnesyltransferase Inhibitors Using a Bayesian Regularized Neural Network. Journal of Medicinal Chemistry 2004, 47 (25) , 6230-6238.
    2. Tammy C. Turek,, Igor Gaon, and, Mark D. Distefano, , Corey L. Strickland. Synthesis of Farnesyl Diphosphate Analogues Containing Ether-Linked Photoactive Benzophenones and Their Application in Studies of Protein Prenyltransferases. The Journal of Organic Chemistry 2001, 66 (10) , 3253-3264.
    3. Todd J. Zahn,, Markus Eilers,, Zhengmao Guo,, Mohamad B. Ksebati,, Matthew Simon,, Jeffrey D. Scholten,, Steven O. Smith, and, Richard A. Gibbs. Evaluation of Isoprenoid Conformation in Solution and in the Active Site of Protein-Farnesyl Transferase Using Carbon-13 Labeling in Conjunction with Solution- and Solid-State NMR. Journal of the American Chemical Society 2000, 122 (30) , 7153-7164.
    4. Elie Giraud,, Claude Luttmann,, François Lavelle,, Jean-François Riou,, Patrick Mailliet, and, Abdelazize Laoui. Multivariate Data Analysis Using D-Optimal Designs, Partial Least Squares, and Response Surface Modeling:  A Directional Approach for the Analysis of Farnesyltransferase Inhibitors. Journal of Medicinal Chemistry 2000, 43 (9) , 1807-1816.
    5. Kareem A. H. Chehade,, Douglas A. Andres,, Hiromi Morimoto, and, H. Peter Spielmann. Design and Synthesis of a Transferable Farnesyl Pyrophosphate Analogue to Ras by Protein Farnesyltransferase. The Journal of Organic Chemistry 2000, 65 (10) , 3027-3033.
    6. Melanie J. Blanden, Sudhat Ashok, James L. Hougland. Mechanisms of CaaX Protein Processing: Protein Prenylation by FTase and GGTase-I. 2020, 497-527.
    7. James J. Fiordalisi, Adrienne D. Cox. Farnesyltransferase Inhibitors. 2010, 1819-1826.
    8. Kimberly T. Lane, Lorena S. Beese. Thematic review series: Lipid Posttranslational Modifications. Structural biology of protein farnesyltransferase and geranylgeranyltransferase type I. Journal of Lipid Research 2006, 47 (4) , 681-699.
    9. D. W. End, L. Mevellec, P. Angibaud. Farnesyl Protein Transferase Inhibitors: Medicinal Chemistry, Molecular Mechanisms, and Progress in the Clinic. 2006, 133-168.
    10. Y. L. Janin. Peptides with anticancer use or potential. Amino Acids 2003, 25 (1) , 1-40.
    11. James J. Fiordalisi, Adrienne D. Cox. Farnesyltransferase Inhibitors. 2003, 737-744.
    12. Kimberly L. Terry, Stephen B. Long, Lorena S. Beese. 2 Structure of protein farnesyltransferase. 2001, 19-46.
    13. Jackson B. Gibbs. 4 Farnesyltransferase inhibitors. 2001, 81-103.
    14. Nicholas J.S Harmat, Silvia Mangani, Enzo Perrotta, Danilo Giannotti, Rossano Nannicini, Maria Altamura. Enantioselective syntheses of orthogonally protected tricarballylic acid esters. Tetrahedron Letters 2000, 41 (8) , 1261-1264.
    15. Russell B. Lingham, Sheo B. Singh. Farnesyl-Protein Transferase: A New Paradigm for Cancer Chemotherapy, Advances in Discovery and Development of Natural Product Inhibitors. 2000, 403-472.
    16. NANCY E. KOHL. Farnesyltransferase Inhibitors: Preclinical Development. Annals of the New York Academy of Sciences 1999, 886 (1) , 91-102.
    17. Martin Schlitzer, Isabel Sattler. Aromatic carboxylic acids as farnesyl surrogates in farnesylpyrophosphate-based farnesyltransferase inhibitors. Bioorganic & Medicinal Chemistry 1999, 7 (11) , 2391-2395.
    18. Theresa M Williams. Inhibitors of protein prenylation 1999. Expert Opinion on Therapeutic Patents 1999, 9 (9) , 1263-1280.
    19. Wang Shen, Stephen Fakhoury, Greg Donner, Kenneth Henry, Jang Lee, Haichao Zhang, Jerry Cohen, Robert Warner, Badr Saeed, Sajeev Cherian, Stephen Tahir, Peter Kovar, Joy Bauch, Shi-Chung Ng, Kennan Marsh, Hing Sham, Saul Rosenberg. Potent inhibitors of protein farnesyltransferase: Heteroarenes as cysteine replacements. Bioorganic & Medicinal Chemistry Letters 1999, 9 (5) , 703-708.
    20. Amelia Moreno Barber, Ian R Hardcastle, Martin G Rowlands, Bernard P Nutley, Jonathan H Marriott, Michael Jarman. Solid-phase synthesis of novel inhibitors of Farnesyl Transferase. Bioorganic & Medicinal Chemistry Letters 1999, 9 (4) , 623-626.
    21. Jeffrey T Eummer, Barbara S Gibbs, Todd J Zahn, Judith S Sebolt-Leopold, Richard A Gibbs. Novel limonene phosphonate and farnesyl diphosphate analogues: design, synthesis, and evaluation as potential protein-farnesyl transferase inhibitors. Bioorganic & Medicinal Chemistry 1999, 7 (2) , 241-250.
    22. Mari Yonemoto, Toshihiko Satoh, Hiroharu Arakawa, Ikuko Suzuki-Takahashi, Yoshiaki Monden, Tsutomu Kodera, Kenji Tanaka, Tetsuya Aoyama, Yoshikazu Iwasawa, Toshio Kamei, Susumu Nishimura, Koji Tomimoto. J-104,871, a Novel Farnesyltransferase Inhibitor, Blocks Ras Farnesylation In Vivo in a Farnesyl Pyrophosphate-Competitive Manner. Molecular Pharmacology 1998, 54 (1) , 1-7.
    23. Martin Schlitzer. Hemmstoffe der Farnesyltransferase: Ein neuer Ansatz zur Entwicklung potentieller Krebstherapeutika. Pharmazie in unserer Zeit 1998, 27 (6) , 278-288.

    Pair your accounts.

    Export articles to Mendeley

    Get article recommendations from ACS based on references in your Mendeley library.

    Pair your accounts.

    Export articles to Mendeley

    Get article recommendations from ACS based on references in your Mendeley library.

    You’ve supercharged your research process with ACS and Mendeley!

    STEP 1:
    Click to create an ACS ID

    Please note: If you switch to a different device, you may be asked to login again with only your ACS ID.

    Please note: If you switch to a different device, you may be asked to login again with only your ACS ID.

    Please note: If you switch to a different device, you may be asked to login again with only your ACS ID.

    Your Mendeley pairing has expired. Please reconnect