Related Content
Search Google Scholar for:
|
|
Science 25 June 1993: Vol. 260. no. 5116, pp. 1937 - 1942 DOI: 10.1126/science.8316834
|
|
Articles
Science, Vol 260, Issue 5116, 1937-1942
Copyright © 1993 by American Association for the Advancement of Science
Benzodiazepine peptidomimetics: potent inhibitors of Ras farnesylation in animal cells
GL James,
JL Goldstein,
MS Brown,
TE Rawson,
TC Somers,
RS McDowell,
CW Crowley,
BK Lucas,
AD Levinson,
and
JC Marsters Jr
Department of Molecular Genetics, University of Texas Southwestern Medical Center, Dallas 75235.
Oncogenic Ras proteins transform animal cells to a malignant phenotype only when modified by farnesyl residues attached to cysteines near their carboxyl termini. The farnesyltransferase that catalyzes this reaction recognizes tetrapeptides of the sequence CAAX, where C is cysteine, A is an aliphatic amino acid, and X is a carboxyl-terminal methionine or serine. Replacement of the two aliphatic residues with a benzodiazepine-based mimic of a peptide turn generated potent inhibitors of farnesyltransferase [50 percent inhibitory concentration (IC50) < 1 nM]. Unlike tetrapeptides, the benzodiazepine peptidomimetics enter cells and block attachment of farnesyl to Ras, nuclear lamins, and several other proteins. At micromolar concentrations, these inhibitors restored a normal growth pattern to Ras-transformed cells. The benzodiazepine peptidomimetics may be useful in the design of treatments for tumors in which oncogenic Ras proteins contribute to abnormal growth, such as that of the colon, lung, and pancreas.
THIS ARTICLE HAS BEEN CITED BY OTHER ARTICLES:
- A Systems Perspective of Ras Signaling in Cancer.
- E. C. Stites and K. S. Ravichandran (2009)
Clin. Cancer Res.
15, 1510-1513
| Abstract »
| Full Text »
| PDF »
- Network Analysis of Oncogenic Ras Activation in Cancer.
- E. C. Stites, P. C. Trampont, Z. Ma, and K. S. Ravichandran (2007)
Science
318, 463-467
| Abstract »
| Full Text »
| PDF »
- Cellular palmitoylation and trafficking of lipidated peptides.
- J. M. Draper, Z. Xia, and C. D. Smith (2007)
J. Lipid Res.
48, 1873-1884
| Abstract »
| Full Text »
| PDF »
- The use of targeted mouse models for preclinical testing of novel cancer therapeutics..
- K. P. Olive and D. A. Tuveson (2006)
Clin. Cancer Res.
12, 5277-5287
| Abstract »
| Full Text »
| PDF »
- AAL881, a Novel Small Molecule Inhibitor of RAF and Vascular Endothelial Growth Factor Receptor Activities, Blocks the Growth of Malignant Glioma..
- S. Sathornsumetee, A. B. Hjelmeland, S. T. Keir, R. E. McLendon, D. Batt, T. Ramsey, N. Yusuff, B.K. A. Rasheed, M. W. Kieran, A. Laforme, et al. (2006)
Cancer Res.
66, 8722-8730
| Abstract »
| Full Text »
| PDF »
- Discovery and characterization of inhibitors of human palmitoyl acyltransferases..
- C. E. Ducker, L. K. Griffel, R. A. Smith, S. N. Keller, Y. Zhuang, Z. Xia, J. D. Diller, and C. D. Smith (2006)
Mol. Cancer Ther.
5, 1647-1659
| Abstract »
| Full Text »
| PDF »
- Thematic review series: Lipid Posttranslational Modifications. Structural biology of protein farnesyltransferase and geranylgeranyltransferase type I.
- K. T. Lane and L. S. Beese (2006)
J. Lipid Res.
47, 681-699
| Abstract »
| Full Text »
| PDF »
- Thematic review series: Lipid Posttranslational Modifications. Farnesyl transferase inhibitors.
- A. D. Basso, P. Kirschmeier, and W. R. Bishop (2006)
J. Lipid Res.
47, 15-31
| Abstract »
| Full Text »
| PDF »
- Thematic Review Series: Lipid Posttranslational Modifications. Prelamin A, Zmpste24, misshapen cell nuclei, and progeria--new evidence suggesting that protein farnesylation could be important for disease pathogenesis.
- S. G. Young, L. G. Fong, and S. Michaelis (2005)
J. Lipid Res.
46, 2531-2558
| Abstract »
| Full Text »
| PDF »
- Prenylation-Defective Human Connexin32 Mutants Are Normally Localized and Function Equivalently to Wild-Type Connexin32 in Myelinating Schwann Cells.
- Y. Huang, E. E. Sirkowski, J. T. Stickney, and S. S. Scherer (2005)
J. Neurosci.
25, 7111-7120
| Abstract »
| Full Text »
| PDF »
- Phase I Pharmacokinetic and Pharmacodynamic Study of Weekly 1-Hour and 24-Hour Infusion BMS-214662, a Farnesyltransferase Inhibitor, in Patients With Advanced Solid Tumors.
- J. Tabernero, F. Rojo, I. Marimon, M. Voi, J. Albanell, M. Guix, F. Vazquez, J. Carulla, M. Cooper, J. Andreu, et al. (2005)
J. Clin. Oncol.
23, 2521-2533
| Abstract »
| Full Text »
| PDF »
- Overcoming Endocrine Therapy Resistance by Signal Transduction Inhibition.
- M. Ellis (2004)
Oncologist
9, 20-26
| Abstract »
| Full Text »
| PDF »
- Apoptotic and Cytostatic Farnesyltransferase Inhibitors Have Distinct Pharmacology and Efficacy Profiles in Tumor Models.
- V. Manne, F. Y. F. Lee, D. K. Bol, J. Gullo-Brown, C. R. Fairchild, L. J. Lombardo, R. A. Smykla, G. D. Vite, M.-L. D. Wen, C. Yu, et al. (2004)
Cancer Res.
64, 3974-3980
| Abstract »
| Full Text »
| PDF »
- Farnesyltransferase inhibitors in hematologic malignancies: new horizons in therapy.
- J. E. Lancet and J. E. Karp (2003)
Blood
102, 3880-3889
| Abstract »
| Full Text »
| PDF »
- Anti-Leukemia Effect of Perillyl Alcohol in Bcr/Abl-Transformed Cells Indirectly Inhibits Signaling through Mek in a Ras- and Raf-Independent Fashion.
- S. S. Clark, L. Zhong, D. Filiault, S. Perman, Z. Ren, M. Gould, and X. Yang (2003)
Clin. Cancer Res.
9, 4494-4504
| Abstract »
| Full Text »
| PDF »
- Farnesyltransferase Inhibitors: An Overview of the Results of Preclinical and Clinical Investigations.
- T. B. Brunner, S. M. Hahn, A. K. Gupta, R. J. Muschel, W. G. McKenna, and E. J. Bernhard (2003)
Cancer Res.
63, 5656-5668
| Abstract »
| Full Text »
| PDF »
- Modulation of Cellular Signaling Pathways: Prospects for Targeted Therapy in Hematological Malignancies.
- F. Ravandi, M. Talpaz, and Z. Estrov (2003)
Clin. Cancer Res.
9, 535-550
| Abstract »
| Full Text »
| PDF »
- Inhibition of Glucose- and Calcium-Induced Insulin Secretion from beta TC3 Cells by Novel Inhibitors of Protein Isoprenylation.
- R. Amin, H.-Q. Chen, M. Tannous, R. Gibbs, and A. Kowluru (2002)
J. Pharmacol. Exp. Ther.
303, 82-88
| Abstract »
| Full Text »
| PDF »
- Rig is a novel Ras-related protein and potential neural tumor suppressor.
- C. A. Ellis, M. D. Vos, H. Howell, T. Vallecorsa, D. W. Fults, and G. J. Clark (2002)
PNAS
99, 9876-9881
| Abstract »
| Full Text »
| PDF »
- Reversion of RhoC GTPase-induced Inflammatory Breast Cancer Phenotype by Treatment with a Farnesyl Transferase Inhibitor.
- K. L. van Golen, L. Bao, M. M. DiVito, Z. Wu, G. C. Prendergast, and S. D. Merajver (2002)
Mol. Cancer Ther.
1, 575-583
| Abstract »
| Full Text »
| PDF »
- A Phase I Trial of the Farnesyltransferase Inhibitor L-778,123 and Radiotherapy for Locally Advanced Lung and Head and Neck Cancer.
- S. M. Hahn, E. J. Bernhard, W. Regine, M. Mohiuddin, D. G. Haller, J. P. Stevenson, D. Smith, B. Pramanik, J. Tepper, T. F. DeLaney, et al. (2002)
Clin. Cancer Res.
8, 1065-1072
| Abstract »
| Full Text »
| PDF »
- The Ras Inhibitor S-trans,trans-Farnesylthiosalicylic Acid Chemosensitizes Human Tumor Cells Without Causing Resistance.
- M. Gana-Weisz, J. Halaschek-Wiener, B. Jansen, G. Elad, R. Haklai, and Y. Kloog (2002)
Clin. Cancer Res.
8, 555-565
| Abstract »
| Full Text »
| PDF »
- Preclinical Antitumor Activity of BMS-214662, a Highly Apoptotic and Novel Farnesyltransferase Inhibitor.
- W. C. Rose, F. Y. F. Lee, C. R. Fairchild, M. Lynch, T. Monticello, R. A. Kramer, and V. Manne (2001)
Cancer Res.
61, 7507-7517
| Abstract »
| Full Text »
| PDF »
- Isotype-specific Ras{middle dot}GTP-Levels Predict the Efficacy of Farnesyl Transferase Inhibitors against Human Astrocytomas Regardless of Ras Mutational Status.
- M. M. Feldkamp, N. Lau, L. Roncari, and A. Guha (2001)
Cancer Res.
61, 4425-4431
| Abstract »
| Full Text »
| PDF »
- Characterization of the Antitumor Effects of the Selective Farnesyl Protein Transferase Inhibitor R115777 in Vivo and in Vitro.
- D. W. End, G. Smets, A. V. Todd, T. L. Applegate, C. J. Fuery, P. Angibaud, M. Venet, G. Sanz, H. Poignet, S. Skrzat, et al. (2001)
Cancer Res.
61, 131-137
| Abstract »
| Full Text »
- Targeting the Ras signaling pathway: a rational, mechanism-based treatment for hematologic malignancies?.
- C. W. M. Reuter, M. A. Morgan, and L. Bergmann (2000)
Blood
96, 1655-1669
| Abstract »
| Full Text »
| PDF »
- Functional Requirement of Plant Farnesyltransferase during Development in Arabidopsis.
- S. Yalovsky, A. Kulukian, M. Rodríguez-Concepción, C. A. Young, and W. Gruissem (2000)
PLANT CELL
12, 1267-1278
| Abstract »
| Full Text »
- Inhibition of cell growth in human glioblastoma cell lines by farnesyltransferase inhibitor SCH66336.
- T. L. Glass, T.-J. Liu, and W.K. A. Yung (2000)
Neuro-oncol
2, 151-158
| Abstract »
| PDF »
- The Role of Polypeptide Growth Factors in Human Carcinomas: New Targets for a Novel Pharmacological Approach.
- R. E. Favoni and A. De Cupis (2000)
Pharmacol. Rev.
52, 179-206
| Abstract »
| Full Text »
| PDF »
- Comparison of Potential Markers of Farnesyltransferase Inhibition.
- A. A. Adjei, J. N. Davis, C. Erlichman, P. A. Svingen, and S. H. Kaufmann (2000)
Clin. Cancer Res.
6, 2318-2325
| Abstract »
| Full Text »
- Mouse Mammary Tumor Virus-Ki-rasB Transgenic Mice Develop Mammary Carcinomas That Can Be Growth-inhibited by a Farnesyl:Protein Transferase Inhibitor.
- C. A. Omer, Z. Chen, R. E. Diehl, M. W. Conner, H. Y. Chen, M. E. Trumbauer, S. Gopal-Truter, G. Seeburger, H. Bhimnathwala, M. T. Abrams, et al. (2000)
Cancer Res.
60, 2680-2688
| Abstract »
| Full Text »
- A Phase I Trial of the Farnesyl Transferase Inhibitor SCH66336: Evidence for Biological and Clinical Activity.
- A. A. Adjei, C. Erlichman, J. N. Davis, D. L. Cutler, J. A. Sloan, R. S. Marks, L. J. Hanson, P. A. Svingen, P. Atherton, W. R. Bishop, et al. (2000)
Cancer Res.
60, 1871-1877
| Abstract »
| Full Text »
- Phase I and Pharmacokinetic Study of Farnesyl Protein Transferase Inhibitor R115777 in Advanced Cancer.
- J. Zujewski, I. D. Horak, C. J. Bol, R. Woestenborghs, C. Bowden, D. W. End, V. K. Piotrovsky, J. Chiao, R. T. Belly, A. Todd, et al. (2000)
J. Clin. Oncol.
18, 927
| Abstract »
| Full Text »
| PDF »
- A Ras-Dependent Chloride Current Activated by Adrenocorticotropin in Rat Adrenal Zona Glomerulosa Cells.
- A. Chorvatova, L. Gendron, L. Bilodeau, N. Gallo-Payet, and M. D. Payet (2000)
Endocrinology
141, 684-692
| Abstract »
| Full Text »
| PDF »
- Inhibition of juvenile myelomonocytic leukemia cell growth in vitro by farnesyltransferase inhibitors.
- P. D. Emanuel, R. C. Snyder, T. Wiley, B. Gopurala, and R. P. Castleberry (2000)
Blood
95, 639-645
| Abstract »
| Full Text »
| PDF »
- Novel Ras antagonist blocks human melanoma growth.
- B. Jansen, H. Schlagbauer-Wadl, H. Kahr, E. Heere-Ress, B. X. Mayer, H.-G. Eichler, H. Pehamberger, M. Gana-Weisz, E. Ben-David, Y. Kloog, et al. (1999)
PNAS
96, 14019-14024
| Abstract »
| Full Text »
| PDF »
- Ras Protein Farnesyltransferase: A Strategic Target for Anticancer Therapeutic Development.
- E. K. Rowinsky, J. J. Windle, and D. D. Von Hoff (1999)
J. Clin. Oncol.
17, 3631-3652
| Abstract »
| Full Text »
| PDF »
- Geranylgeranylated RhoB Mediates Suppression of Human Tumor Cell Growth by Farnesyltransferase Inhibitors.
- W. Du and G. C. Prendergast (1999)
Cancer Res.
59, 5492-5496
| Abstract »
| Full Text »
| PDF »
- Critical role of p42/44MAPK activation in anisomycin and hepatocyte growth factor-induced LDL receptor expression: activation of Raf-1/MEK-1/p42/44MAPK cascade alone is sufficient to induce LDL receptor expression.
- P. Dhawan, A. Bell, A. Kumar, C. Golden, and K. D. Mehta (1999)
J. Lipid Res.
40, 1911-1919
| Abstract »
| Full Text »
- Ligands for kappa -Opioid and ORL1 Receptors Identified from a Conformationally Constrained Peptide Combinatorial Library.
- J. A. J. Becker, A. Wallace, A. Garzon, P. Ingallinella, E. Bianchi, R. Cortese, F. Simonin, B. L. Kieffer, and A. Pessi (1999)
J. Biol. Chem.
274, 27513-27522
| Abstract »
| Full Text »
| PDF »
- A Mutant Form of Human Protein Farnesyltransferase Exhibits Increased Resistance to Farnesyltransferase Inhibitors.
- K. Del Villar, J. Urano, L. Guo, and F. Tamanoi (1999)
J. Biol. Chem.
274, 27010-27017
| Abstract »
| Full Text »
| PDF »
- Activation of the PI3'K-AKT Pathway Masks the Proapoptotic Effects of Farnesyltransferase Inhibitors.
- W. Du, A. Liu, and G. C. Prendergast (1999)
Cancer Res.
59, 4208-4212
| Abstract »
| Full Text »
| PDF »
- Elevation of {{alpha}}2(I) Collagen, a Suppressor of Ras Transformation, Is Required for Stable Phenotypic Reversion by Farnesyltransferase Inhibitors.
- W. Du, P. F. Lebowitz, and G. C. Prendergast (1999)
Cancer Res.
59, 2059-2063
| Abstract »
| Full Text »
| PDF »
- High-level expression, purification, kinetic characterization and crystallization of protein farnesyltransferase ß-subunit C-terminal mutants.
- Z. Wu, M. Demma, C. L. Strickland, R. Syto, H. V. Le, W. T. Windsor, and P. C. Weber (1999)
Protein Eng. Des. Sel.
12, 341-348
| Abstract »
| Full Text »
| PDF »
- RAS and Leukemia: From Basic Mechanisms to Gene-Directed Therapy.
- D. M. Beaupre and R. Kurzrock (1999)
J. Clin. Oncol.
17, 1071
| Abstract »
| Full Text »
| PDF »
- Cell Growth Inhibition by Farnesyltransferase Inhibitors Is Mediated by Gain of Geranylgeranylated RhoB.
- W. Du, P. F. Lebowitz, and G. C. Prendergast (1999)
Mol. Cell. Biol.
19, 1831-1840
| Abstract »
| Full Text »
| PDF »
- HMG-CoA reductase regulation: use of structurally diverse first half-reaction squalene synthetase inhibitors to characterize the site of mevalonate-derived nonsterol regulator production in cultured IM-9 cells.
- S. F. Petras, S. Lindsey, and H. J. Harwood , Jr. (1999)
J. Lipid Res.
40, 24-38
| Abstract »
| Full Text »
- Treatment with Farnesyl-Protein Transferase Inhibitor Induces Regression of Mammary Tumors in Transforming Growth Factor (TGF) {{alpha}} and TGF{{alpha}}/neu Transgenic Mice by Inhibition of Mitogenic Activity and Induction of Apoptosis.
- P. Norgaard, B. Law, H. Joseph, D. L. Page, Y. Shyr, D. Mays, J. A. Pietenpol, N. E. Kohl, A. Oliff, R. J. Coffey Jr., et al. (1999)
Clin. Cancer Res.
5, 35-42
| Abstract »
| Full Text »
| PDF »
- MEK and ERK Activation in Ras-Disabled RBL-2H3 Mast Cells and Novel Roles for Geranylgeranylated and Farnesylated Proteins in Fc{epsilon}RI-Mediated Signaling.
- T. E. Graham, J. R. Pfeiffer, R. J. Lee, D. F. Kusewitt, A. M. Martinez, T. Foutz, B. S. Wilson, and J. M. Oliver (1998)
J. Immunol.
161, 6733-6744
| Abstract »
| Full Text »
| PDF »
- Use of a Prenylation Inhibitor as a Novel Antiviral Agent.
- J. S. Glenn, J. C. Marsters Jr., and H. B. Greenberg (1998)
J. Virol.
72, 9303-9306
| Abstract »
| Full Text »
| PDF »
- Protein Farnesyltransferase from Trypanosoma brucei. A HETERODIMER OF 61- AND 65-kDa SUBUNITS AS A NEW TARGET FOR ANTIPARASITE THERAPEUTICS.
- K. Yokoyama, P. Trobridge, F. S. Buckner, W. C. Van Voorhis, K. D. Stuart, and M. H. Gelb (1998)
J. Biol. Chem.
273, 26497-26505
| Abstract »
| Full Text »
| PDF »
- Farnesyltransferase inhibitors induce dramatic morphological changes of KNRK cells that are blocked by microtubule interfering agents.
- N. Suzuki, K. Del Villar, and F. Tamanoi (1998)
PNAS
95, 10499-10504
| Abstract »
| Full Text »
| PDF »
- J-104,871, a Novel Farnesyltransferase Inhibitor, Blocks Ras Farnesylation In Vivo in a Farnesyl Pyrophosphate-Competitive Manner.
- M. Yonemoto, T. Satoh, H. Arakawa, I. Suzuki-Takahashi, Y. Monden, T. Kodera, K. Tanaka, T. Aoyama, Y. Iwasawa, T. Kamei, et al. (1998)
Mol. Pharmacol.
54, 1-7
| Abstract »
| Full Text »
- Inhibiting geranylgeranylation blocks growth and promotes apoptosis in pulmonary vascular smooth muscle cells.
- W. W. Stark Jr., M. A. Blaskovich, B. A. Johnson, Y. Qian, A. Vasudevan, B. Pitt, A. D. Hamilton, S. M. Sebti, and P. Davies (1998)
Am J Physiol Lung Cell Mol Physiol
275, L55-L63
| Abstract »
| Full Text »
| PDF »
- Impact of oncogenes in tumor angiogenesis: Mutant K-ras up-regulation of vascular endothelial growth factor/vascular permeability factor is necessary, but not sufficient for tumorigenicity of human colorectal carcinoma cells.
- F. Okada, J. W. Rak, B. St. Croix, B. Lieubeau, M. Kaya, L. Roncari, S. Shirasawa, T. Sasazuki, and R. S. Kerbel (1998)
PNAS
95, 3609-3614
| Abstract »
| Full Text »
| PDF »
- Farnesyl transferase inhibitors cause enhanced mitotic sensitivity to taxol and epothilones.
- M. M. Moasser, L. Sepp-Lorenzino, N. E. Kohl, A. Oliff, A. Balog, D.-S. Su, S. J. Danishefsky, and N. Rosen (1998)
PNAS
95, 1369-1374
| Abstract »
| Full Text »
| PDF »
- Interactions of Benzodiazepine Derivatives with Annexins.
- A. Hofmann, A. Escherich, A. Lewit-Bentley, J. Benz, C. Raguenes-Nicol, F. Russo-Marie, V. Gerke, L. Moroder, and R. Huber (1998)
J. Biol. Chem.
273, 2885-2894
| Abstract »
| Full Text »
| PDF »
- A Farnesyltransferase Inhibitor Induces Tumor Regression in Transgenic Mice Harboring Multiple Oncogenic Mutations by Mediating Alterations in Both Cell Cycle Control and Apoptosis.
- R. E. Barrington, M. A. Subler, E. Rands, C. A. Omer, P. J. Miller, J. E. Hundley, S. K. Koester, D. A. Troyer, D. J. Bearss, M. W. Conner, et al. (1998)
Mol. Cell. Biol.
18, 85-92
| Abstract »
| Full Text »
- Substrate specificity determinants in the farnesyltransferase beta -subunit.
- C. E. Trueblood, V. L. Boyartchuk, and J. Rine (1997)
PNAS
94, 10774-10779
| Abstract »
| Full Text »
| PDF »
- Juvenile Myelomonocytic Leukemia.
- M. Arico, A. Biondi, and C.-H. Pui (1997)
Blood
90, 479-488
| Full Text »
| PDF »
- .
- M. Raiteri, L. Arnaboldi, P. Mcgeady, M. H. Gelb, D. Verri, C. Tagliabue, P. Quarato, P. Ferraboschi, E. Santaniello, R. Paoletti, et al. (1997)
J. Pharmacol. Exp. Ther.
281, 1144-1153
| Abstract »
| Full Text »
- Direct Demonstration of Geranylgeranylation and Farnesylation of Ki-Ras in Vivo.
- C. A. Rowell, J. J. Kowalczyk, M. D. Lewis, and A. M. Garcia (1997)
J. Biol. Chem.
272, 14093-14097
| Abstract »
| Full Text »
| PDF »
- Inhibition of Protein Geranylgeranylation Causes a Superinduction of Nitric-oxide Synthase-2 by Interleukin-1beta in Vascular Smooth Muscle Cells.
- J. D. Finder, J. L. Litz, M. A. Blaskovich, T. F. McGuire, Y. Qian, A. D. Hamilton, P. Davies, and S. M. Sebti (1997)
J. Biol. Chem.
272, 13484-13488
| Abstract »
| Full Text »
| PDF »
- Substrate Binding Is Required for Release of Product from Mammalian Protein Farnesyltransferase.
- W. R. Tschantz, E. S. Furfine, and P. J. Casey (1997)
J. Biol. Chem.
272, 9989-9993
| Abstract »
| Full Text »
| PDF »
- Characterization of Ha-Ras, N-Ras, Ki-Ras4A, and Ki-Ras4B as in Vitro Substrates for Farnesyl Protein Transferase and Geranylgeranyl Protein Transferase Type I.
- F. L. Zhang, P. Kirschmeier, D. Carr, L. James, R. W. Bond, L. Wang, R. Patton, W. T. Windsor, R. Syto, R. Zhang, et al. (1997)
J. Biol. Chem.
272, 10232-10239
| Abstract »
| Full Text »
| PDF »
- In Vitro Assay and Characterization of the Farnesylation-dependent Prelamin A Endoprotease.
- F. Kilic, M. B. Dalton, S. K. Burrell, J. P. Mayer, S. D. Patterson, and M. Sinensky (1997)
J. Biol. Chem.
272, 5298-5304
| Abstract »
| Full Text »
| PDF »
- Amino Acid Substitutions That Convert the Protein Substrate Specificity of Farnesyltransferase to That of Geranylgeranyltransferase Type I.
- K. Del Villar, H. Mitsuzawa, W. Yang, I. Sattler, and F. Tamanoi (1997)
J. Biol. Chem.
272, 680-687
| Abstract »
| Full Text »
| PDF »
- Selection of Potent Inhibitors of Farnesyl-protein Transferase from a Synthetic Tetrapeptide Combinatorial Library.
- A. Wallace, K. S. Koblan, K. Hamilton, D. J. Marquis-Omer, P. J. Miller, S. D. Mosser, C. A. Omer, M. D. Schaber, R. Cortese, A. Oliff, et al. (1996)
J. Biol. Chem.
271, 31306-31311
| Abstract »
| Full Text »
| PDF »
- Platelet-derived Growth Factor Receptor Tyrosine Phosphorylation Requires Protein Geranylgeranylation but not Farnesylation.
- T. F. McGuire, Y. Qian, A. Vogt, A. D. Hamilton, and S. M. Sebti (1996)
J. Biol. Chem.
271, 27402-27407
| Abstract »
| Full Text »
| PDF »
- Effect of Insulin on Farnesyltransferase Activity in 3T3-L1 Adipocytes.
- M. L. Goalstone and B. Draznin (1996)
J. Biol. Chem.
271, 27585-27589
| Abstract »
| Full Text »
| PDF »
- Interaction of Transforming Growth Factor-beta Receptor I with Farnesyl-protein Transferase-alpha in Yeast and Mammalian Cells.
- F. Ventura, F. Liu, J. Doody, and J. Massague (1996)
J. Biol. Chem.
271, 13931-13934
| Abstract »
| Full Text »
| PDF »
- Localization of Epidermal Growth Factor-stimulated Ras/Raf-1 Interaction to Caveolae Membrane.
- C. Mineo, G. L. James, E. J. Smart, and R. G. W. Anderson (1996)
J. Biol. Chem.
271, 11930-11935
| Abstract »
| Full Text »
| PDF »
- Protein Prenyltransferases.
- P. J. Casey and M. C. Seabra (1996)
J. Biol. Chem.
271, 5289-5292
| Full Text »
| PDF »
- The Hepatitis Delta Virus Large Antigen Is Farnesylated Both in Vitro and in Animal Cells.
- J. C. Otto and P. J. Casey (1996)
J. Biol. Chem.
271, 4569-4572
| Abstract »
| Full Text »
| PDF »
- Regulation of Cytokine-inducible Nitric Oxide Synthase in Cardiac Myocytes and Microvascular Endothelial Cells.
- K. Singh, J.-L. Balligand, T. A. Fischer, T. W. Smith, and R. A. Kelly (1996)
J. Biol. Chem.
271, 1111-1117
| Abstract »
| Full Text »
| PDF »
- Disruption of Oncogenic K-Ras4B Processing and Signaling by a Potent Geranylgeranyltransferase I Inhibitor.
- E. C. Lerner, Y. Qian, A. D. Hamilton, and S.ïd M. Sebti (1995)
J. Biol. Chem.
270, 26770-26773
| Abstract »
| Full Text »
| PDF »
- Mechanisms of Toxicity and Carcinogenesis.
- B. F. Trump (1995)
Toxicol Pathol
23, 775-827
| PDF »
- Selective Inhibition of Ras-dependent Cell Growth by Farnesylthiosalisylic Acid.
- M. Marom, R. Haklai, G. Ben-Baruch, D. Marciano, Y. Egozi, and Y. Kloog (1995)
J. Biol. Chem.
270, 22263-22270
| Abstract »
| Full Text »
| PDF »
- Photoreactive Analogues of Prenyl Diphosphates as Inhibitors and Probes of Human Protein Farnesyltransferase and Geranylgeranyltransferase Type I.
- Y. E. Bukhtiyarov, C. A. Omer, and C. M. Allen (1995)
J. Biol. Chem.
270, 19035-19040
| Abstract »
| Full Text »
| PDF »
- Differential Effects of Monoterpenes and Lovastatin on RAS Processing.
- R. J. Hohl and K. Lewis (1995)
J. Biol. Chem.
270, 17508-17512
| Abstract »
| Full Text »
| PDF »
- Regions Outside of the CAAX Motif Influence the Specificity of Prenylation of G Protein [IMAGE] Subunits.
- V. K. Kalman, R. A. Erdman, W. A. Maltese, and J. D. Robishaw (1995)
J. Biol. Chem.
270, 14835-14841
| Abstract »
| Full Text »
| PDF »
- Protein lipidation in cell signaling.
- P. Casey (1995)
Science
268, 221-225
| Abstract »
| PDF »
- CAAX Geranylgeranyl Transferase Transfers Farnesyl as Efficiently as Geranylgeranyl to RhoB.
- S. A. Armstrong, V. C. Hannah, J. L. Goldstein, and M. S. Brown (1995)
J. Biol. Chem.
270, 7864-7868
| Abstract »
| Full Text »
| PDF »
- Tyrosine kinase inhibition: an approach to drug development.
- A Levitzki and A Gazit (1995)
Science
267, 1782-1788
| Abstract »
| PDF »
- Polylysine and CVIM Sequences of K-RasB Dictate Specificity of Prenylation and Confer Resistance to Benzodiazepine Peptidomimetic in Vitro.
- G. L. James, J. L. Goldstein, and M. S. Brown (1995)
J. Biol. Chem.
270, 6221-6226
| Abstract »
| Full Text »
| PDF »
- A Non-peptide Mimetic of Ras-CAAX: Selective Inhibition of Farnesyltransferase and Ras Processing.
- A. Vogt, Y. Qian, M. A. Blaskovich, R. D. Fossum, A. D. Hamilton, and S. M. Sebti (1995)
J. Biol. Chem.
270, 660-664
| Abstract »
| Full Text »
| PDF »
- Oncology and Hematology.
- J. E. Karp and S. Broder (1994)
JAMA
271, 1693-1695
| Abstract »
| PDF »
- Expression of prelamin A but not mature lamin A confers sensitivity of DNA biosynthesis to lovastatin on F9 teratocarcinoma cells.
- M Sinensky, T McLain, and K Fantle (1994)
J. Cell Sci.
107, 2215-2218
| Abstract »
| PDF »
- Molecular Genetic Changes Found in Human Lung Cancer and Its Precursor Lesions.
- A.F. Gazdar, S. Bader, J. Hung, Y. Kishimoto, Y. Sekido, K. Sugio, A. Virmani, J. Fleming, D.P. Carbone, and J.D. Minna (1994)
Cold Spring Harb Symp Quant Biol
59, 565-572
| Abstract »
| PDF »
- The processing pathway of prelamin A.
- M Sinensky, K Fantle, M Trujillo, T McLain, A Kupfer, and M Dalton (1994)
J. Cell Sci.
107, 61-67
| Abstract »
| PDF »
- Novel anticancer agents move closer to reality.
- J Travis (1993)
Science
260, 1877-1878
| PDF »
- Prenylation-dependent Association of Protein-tyrosine Phosphatases PRL-1, -2, and -3 with the Plasma Membrane and the Early Endosome.
- Q. Zeng, X. Si, H. Horstmann, Y. Xu, W. Hong, and C. J. Pallen (2000)
J. Biol. Chem.
275, 21444-21452
| Abstract »
| Full Text »
| PDF »
- Farnesyl Transferase Inhibitors Block the Farnesylation of CENP-E and CENP-F and Alter the Association of CENP-E with the Microtubules.
- H. R. Ashar, L. James, K. Gray, D. Carr, S. Black, L. Armstrong, W. R. Bishop, and P. Kirschmeier (2000)
J. Biol. Chem.
275, 30451-30457
| Abstract »
| Full Text »
| PDF »
- Interaction of Farnesylated PRL-2, a Protein-tyrosine Phosphatase, with the beta -Subunit of Geranylgeranyltransferase II.
- X. Si, Q. Zeng, C. H. Ng, W. Hong, and C. J. Pallen (2001)
J. Biol. Chem.
276, 32875-32882
| Abstract »
| Full Text »
| PDF »
|
|