Protein Prenylation Reprints
Fletcher, S., Keaney, E. P., Cummings, C. G., Blaskovich, M. A., Hast, M. A., Glenn, M. P., Chang, S.-Y., Bucher, C. J., Floyd, R. J., Katt, W. P., Gelb, M. H., Van Voorhis, W. C., Beese, L. S., Sebti, S. M., Hamilton, A. D. (2010) Structure-based design and synthesis of potent, ethylenediamine-based, mammalian farnesyltransferase inhibitors as anticancer agents, Med. Chem., 53:6867-6888. PMID: 20822181, PMCID: PMC3045627. reprint
Hast, M. A., Fletcher, S., Cummings, C.G., Pusateri, E.E., Blaskovich, M.A., Rivas, K., Gelb, M.H., Van Voorhis, W.C., Sebti, S.M., Hamilton, A.D., and Beese, L.S. (2009) Structural basis for binding and selectivity of antimalarial and anticancer ethylenediamine inhibitors to protein farnesyltransferase, Chemistry & Biology, 16:181-192. PMID: 19246009, PMCID: PMC2671474. reprint
Fletcher, S., Cummings, C.G., Rivas, K., Katt, W.P., Horney, C., Buckner, F.S., Chakrabarti, D., Sebti, S.M., Gelb, M.H., Van Voorhis, W.C., Hamilton, A.D. (2008) Potent, Plasmodium-selective farnesyltransferase inhibitors that arrest the growth of malaria parasites: Structure-activity relationships of ethylenediamine-analogue scaffolds and homology model validation, J. Med. Chem, 51(17):5176-5197. PMID: 18686940, PMCID: PMC3049929. reprint supp.
Bulbule, V. J., Rivas, K, Verlinde, C. L., Van Voorhis, W. C., Gelb, M. H., (2008) 2-oxotetrahydroquinoline-based antimalarials with high potency and metabolic stability, J. Med. Chem., 51:384-387. PMID: 18198825. reprint.pdf supp.
Olepu, S, Suryadevara, P. K., Rivas, K., Yokoyama, K., Verlinde, C. L., Chakrabarti, D., Van Voorhis, W. C., Gelb, M. H., (2008) 2-Oxo-tetrahydro-1,8-naphthyridines as selective inhibitors of malarial protein farnesyltransferase and as anti-malarials, Bioorg Med Chem Lett., 18:494-497. PMID: 18077162, PMCID: PMC2275803. reprint.pdf supp.
Yokoyama, K., Gillespie, J. R., Van Voorhis, W. C., Buckner, F. S., Gelb, M. H., (2008) Protein geranylgeranyltransferase-I of Trypanosoma cruzi, Mol Biochem Parasitol, 157:32-43. PMID: 17996962, PMCID: PMC2246023. reprint.pdf
Gillespie, J. R., Yokoyama, K, Lu, K, Eastman, R. T., Bollinger, J. G., Van Voorhis, W. C., Gelb, M. H., Buckner, F. S. (2007) C-terminal proteolysis of prenylated proteins in trypanosomatids and RNA interference of enzymes required for the post-translational processing pathway of farnesylated proteins, Mol. Biochem. Parasitol., 153:115-124. PMID: 17397944. reprint.pdf
Gelb, MH (2007) Drug discovery for malaria: a very challenging and timely endeavor, Current Opinion in Chemical Biology, 11:440-445. PMID: 17761335, PMCID: PMC1993815. reprint.pdf
Van Voorhis, W. C., Rivas, K. L., Bendale, P., Nallan, L., Horney, C., Barrett, L. K., Bauer, K. D., Smart, B. P., Ankala, S., Hucke, O., Verlinde, C. L., Chakrabarti, D., Strickland, C., Yokoyama, K., Buckner, F. S., Hamilton, A. D., Williams, D. K., Lombardo, L. J., Floyd, D., Gelb, M. H. (2007) Efficacy, pharmacokinetics, and metabolism of tetrahydroquinoline inhibitors of plasmodium falciparum protein farnesyltransferase, Antimicrob. Agents Chemother., 10:3659-3671. PMID: 17606674, PMCID: PMC2043286. reprint.pdf supp.
Bendale, P., Olepu, S., Suryadevara, P. K., Bulbule, V., Rivas, K., Nallan, L., Smart, B., Yokoyama, K., Ankala, S., Pendyala, P. R., Floyd, D., Lombardo, L. J., Williams, D. K., Buckner, F. S., Chakrabarti, D., Verlinde, C. L., Van Voorhis, W. C., Gelb, M. H. (2007) Second generation tetrahydroquinoline-based protein farnesyltransferase inhibitors as antimalarials, J. Med. Chem., 50:4585-4605. PMID: 17722901, PMCID: PMC2894570. reprint.pdf supp.
Gelb, M. H., Brunsveld, L., Hrycyna, C. A., Michaelis, S., Tamanoi, F., Van Voorhis, W. C. and Waldmann, H. (2006) Therapeutic intervention based on protein prenylation and associated modifications, Nature Chem. Biol. 10: 518-528 reprint.pdf
Eastman, R. T., Buckner, F. S., Yokoyana, K., Gelb, M. H. and Van Voorhis, W .C. (2006) Thematic review series: lipid posttranslational modifications. Fighting parasitic disease by blocking protein farnesylation, J. Lipid Res. 47: 233-40 reprint.pdf
Buckner, F. S., Eastman, R. T., Yokoyama, K.., Gelb, M. H., Van Voorhis, W. C. (2005) ” Protein farnesyl transferase inhibitors for the treatment of malaria and African trypanosomiasis,” Curr Opin Investig Drugs 6:791-7 reprint.pdf
Yang, S. H., Bergo, M. O., Toth, J. I., Qiao, X., Hu, Y., Sandoval, S., Meta, M., Bendale, P., Gelb, M. H., Young, S. G., Fong, L. G. (2005) “Blocking protein farnesyltransferase improves nuclear blebbing in mouse fibroblasts with a targeted Hutchinson-Bilford progeria syndrome mutation,” Prof. Natl. Acad. Sci 102:10291-6 reprint.pdf
Mallampalli, M .P., Huyer, G., Bendale, P., Gelb, M. H. and Michaelis, S. (2005) “Inhibiting farnesylation reverses the nuclear morphology defect in a HeLa cell model for Hutchinson-Gilford progeria syndrome,” Proc. Natl. Acad. Sci.102:14416-21 reprint.pdf
Toth, J. I., Yang, S. H., Qiao, X., Beigneux, A. P., Gelb, M. H., Moulson, C. L., Miner, J. H., Young, S. G. and Fong, L. G. (2005) “Blocking protein farnesyltransferase improves nuclear shape in fibroblasts from humans with progeroid syndromes,” Proc. Natl. Acad. Sci. 102:12873-8 reprint.pdf
Hucke, O., Gelb, M. H.., Verlinde, C. L. M. J. et al. (2005) “The protein farnesyltransferase inhibitor tipifarnib as a new lead for the development of drugs against Chagas disease,” J. Med. Chem., 48: 5415-5418. reprint.pdf
Glenn, M. R., Chang, S. Y., Hucke, O., et al. (2005) “Structurally simple farnesyltransferase inhibitors arrest the growth of malaria parasites,” Angew. Chem. Int. Ed. 41: 4903-4906. reprint.pdf
Toth, J. I., Yang, S. H., Qiao, X., et al. (2005) “Blocking protein farnesyltransferase improves nuclear shape in fibroblasts from humans with progeroid syndromes,” Proc. Natl. Acad. Sci. 102:12873-12878. reprint.pdf
Eastman, R. T., White, J., Hucke, O., et al. (2005) “Resistance to a protein farnesyltransferase inhibitor in Plasmodium falciparum,” J. Biol. Chem. 280:13554-13559. reprint.pdf
Yang, S. H., Bergo, M. O., Toth, J. L., Qiao, X., Hu, Y., Sandoval, S., Meta, M., Bendale, P., Gelb, M. H., Young, S. G. and Fong, L. G. (2005) “Blocking protein farnesyltransferase improves nuclear blebbing in mouse fibroblasts with a targeted Hutchinson-Gilford progeria syndrome mutation,” Proc. Natl. Acad. Sci. 109:10291-10296. reprint.pdf
Nallan, L., Bauer, K. D., Bendale, P., Rivas, K., Yokoyama, K., Horney, C. P., Pendyala, P. R., Floyd, D., Lombardo, L. J., Williams, D. K., Hamilton, A., Sebti, S., Windsor, W. T., Weber, P. C., Buckner, F. S., Chakrabarti, D., Gelb, M. H. and Van Voorhis, W. C. (2005) “Protein farnesyltransferase inhibitors exhibit potent antimalarial activity,” J. Med. Chem., 48:3704-3713. reprint.pdf data supplement.pdf
Carrico, D., Ohkanda, J., Kendrick, H., Yokoyama, K., Blaskovich, M. A., Bucher, C. J., Buckner, F. S., Van Voorhis, W. C., Chakrabarti, D., Croft, S. L., Gelb, M. H., Sebti, S. M. and Hamilton, A. D. (2004) “In vitro and in vivo antimalarial activity of peptidomimetic protein farnesyltransferase inhibitors with improved membrane permeability,” Bioorg Med Chem., 12:6517-26. reprint.pdf
Ohkanda, J., Buckner, F. S, Lockman, J. W., Yokoyama, K., Carrico, D., Eastman, R., Luca-Fradley, K., Davies, W., Croft, S. L., Van Voorhis, W. C., Gelb, M. H., Sebti, S. M., and Hamilton, A. D. (2004) “Design and Sythesis of Peptidominetic Protein Farnesyltransferase Inhibitors as Anti-Typanosoma brucei Agents,”J. Med. Chem., 47:432-445. reprint.pdf
Buckner, F., Yokoyama, K., Lockman, J., Aikenhead, K., Ohkanda, J., Sadilek, M., Sebti, S., Van Voorhis, W., Hamilton, A., and Gelb, M. H. (2003) “A class of sterol 14-demethylase inhibitors as anti-Trypanosoma cruzi agents,” PNAS, 100:15149-15153. reprint.pdf
Ferri, N., Yokoyama, K., Sadilek, M., Paoletti, R., Apitz-Castro, R., Gelb, M. H., and Corsini, A. (2003) “Ajoene, a garlic compound, inhibits protein prenylation and arterial smooth muscle cell proliferation,” Br. J. Pharmacol., 138:811-818. reprint.pdf
Clerici, F., Gelmi, M.L., Yokoyama, K., Pocar, D., Van Voorhis, W. C., Buckner, F. S., and Gelb, M. H. (2002) “Isothiazole dioxides: synthesis and inhibition of Trypanosoma brucei protein farnesyltrasnferase,” Bioorg. Med. Chem. Lett., 12:2217-2220 reprint.pdf
Buckner, F. S., Eastman, R. T., Nepomuceno-Silva, J. L., Speelmon, E. C., Myler, P. J., Van Voorhis, W. C., and Yokoyama, K. (2002) “Cloning, heterologous expression, and substrate specificities of protein farnesyltransferases from Trypanosoma cruzi and Leishmania major,” Molec. & Biochem. Parasitol., 122:181-188. reprint.pdf
Ferri, N., Arnaboldi, A., Orlandi, A., Yokoyama, K., Gree, R., Granata, A., Hachem, A., Paoletti, R., Gelb, M. H., and Corsini, A. (2001) “Effect of S(-) perillic acid on protein prenylation and arterial smooth muscle cell proliferation,” Biochem. Pharm., 62:1637-1645. reprint.pdf
Nepomuceno-Silva, J. L., Yokoyama, K., de Mello, L. D. B., Mendonca, S. M., Paixao, J. C., Baron, R., Faye, J.-C., Buckner, F. S., Van Voorhis, W. C., Gelb, M. H., and Lopes, U. G. (2001) “TcRho1, a farnesylated Rho family homologue from Trypanosoma cruzi,” J. Biol. Chem., 276:29711-29718. reprint.pdf
Ohkanda, J., Lockman, J. W., Yokoyama, K., Gelb, M. H., Croft, S., Kendrick, H., Harrell, M. I., Feagin, J. E., Blaskovich, M. A., Sebti, S. M., and Hamilton, A. D. (2001) “Peptidomimetic inhibitors of protein farnesyltransferase show potent antimalarial activity,” Bioorg. Med. Chem. Lett., 11:761-764. reprint.pdf
Terry A. Cook, Ghomashchi, F., Gelb, M. H., Florio, S. K., and Beavo, J. A. (2000) The delta subunit of type 6 phosphodiesterase reduces light-induced cGMP hydrolysis in rod outer segments J. Biol. Chem., 276:5248-5255. reprint.pdf
Cook, T. A., Ghomashchi, F., Gelb, M. H., Florio, S., Beavo, J. A. (2001) “Binding of the delta subunit to rod phosphodiesterase catalytic subunits requires methylated, prenylated C-termini of their catalytic subunits,” Biochemistry 2000. reprint.pdf
Buckner, F. S., Yokoyama, K., Nguyen, L., Grewal, A., Erdjument-Bromage, H., Tempst, P., Strickland, C. L., Xiao, L, Van Voorhis, W. C., Gelb, M. H. (2000) “Cloning, heterologous expression, and distinct substrate specificity of protein farnesyltransferase from Trypanosoma brucei,” J Biol Chem. 2000 Jul 21;275(29):21870-6. reprint.pdf
Yokoyama, K., Trobridge, P., Buckner, F. S., Van Voorhis, W. C., Stuart. K. D., Gelb, M. H. (1998) “Protein farnesyltransferase from Trypanosoma brucei. A heterodimer of 61- and 65-kda subunits as a new target for antiparasite therapeutics,” Journal of Biological Chemistry. 273(41): 26497-505, Oct 1998. reprint.pdf
Jang, G. F. and Gelb, M. H. (1998) “Substrate specificity of mammalian prenyl protein-specific endoprotease activity,” Biochemistry. 37(13): 4473-81, reprint.pdf
Yokoyama, K., Trobridge, P., Buckner, F. S., Scholten, J., Stuart, K. D., Van Voorhis, W. C., and Gelb, M. H. (1998) “The effects of protein farnesyltransferase inhibitors on trypanosomatids: inhibition of protein farnesylation and cell growth.” Molecular and Biochemical Parasitology, 94:87-97. reprint.pdf
Yokoyama, K., Lin, Y., Stuart, K. D., and Gelb, M .H. (1997) “Prenylation of proteins in Trypanosoma brucei.” Molecular & Biochemical Parasitology, 87:61-69. reprint.pdf
Yokoyama, K., Zimmerman, K., Scholten, J. and Gelb M. H. (1997) “Differential prenyl pyrophosphate binding to mammalian protein geranylgeranyltransferase-I and protein farnesyltransferase and its consequence on the specificity of protein prenylation,” J Biol Chem 272: 3944-52 reprint.pdf
Dudler T. and Gelb M. H. (1996) “Palmitoylation of Ha-Ras facilitates membrane binding, activation of downstream effectors, and meiotic maturation in Xenopus oocytes,” J Biol Chem. 271:11541-7. reprint.pdf
McGeady, P., Kuroda, S., Shimizu, K., Takai, Y., Gelb, M. H. (1995) “The farnesyl group of H-Ras facilitates the activation of a soluble upstream activator of mitogen-activated protein kinase,” J Biol Chem. 270: 26347-51 reprint.pdf
Publications & Patents Links
