2013
Basciano PA, Bussel J, Hafeez Z, Christos PJ, Giannakakou P. The beta 1 tubulin R307H single nucleotide polymorphism is associated with treatment failures in immune thrombocytopenia (ITP) Br J Haematol. 2013 Jan
2012
Diamond E, Lee GY, Akhtar NH, Kirby BJ, Giannakakou P, Tagawa ST, Nanus DM. Isolation and characterization of circulating tumor cells in prostate cancer. Front Oncol. 2012
Kong KY, Marcus AI, Giannakakou P, Wang MD. Integrating image analysis algorithms in a web interface for the quantification of microtubule dynamics. Int J Comput Biol Drug Des. 2012;
Thadani-Mulero M, Nanus DM, Giannakakou P. Androgen receptor on the move: boarding the microtubule expressway to the nucleus. Cancer Res. 2012 Sep 15
Kirby BJ, Jodari M, Loftus MS, Gakhar G, Pratt ED, Chanel-Vos C, Gleghorn JP, Santana SM, Liu H, Smith JP, Navarro VN, Tagawa ST, Bander NH, Nanus DM, Giannakakou P. Functional characterization of circulating tumor cells with a prostate-cancer-specific microfluidic device. PLoS One 2012 April 27
Carbonaro M, Escuin D, O'Brate A, Thadani-Mulero M, Giannakakou P. Microtubules Regulate Hypoxia-inducible Factor-1α Protein Trafficking and Activity: IMPLICATIONS FOR TAXANE THERAPY. J Biol Chem. 2012 Apr 6
2011
Darshan MS, Loftus MS, Thadani-Mulero M, Levy BP, Escuin D, Zhou XK, Gjyrezi A, Chanel-Vos C, Shen R, Tagawa ST, Bander NH, Nanus DM, Giannakakou P.. Taxane-induced blockade to nuclear accumulation of the androgen receptor predicts clinical responses in metastatic prostate cancer Cancer Res. 2011,Sep 15
Wang X, Li J, Wang Y, Koenig L, Gjyrezi A, Giannakakou P., Shin EH, Tighiouart M, Chen ZG, Nie S, Shin DM. A folate receptor-targeting nanoparticle minimizes drug resistance in a human cancer model. ACS Nano. 2011, Aug 23
Kanakkanthara A, Wilmes A, O'Brate A, Escuin D, Chan A, Gjyrezi A, Crawford J, Rawson P, Kivell B, Northcote PT, Hamel E, Giannakakou P., Miller JH. Peloruside- and laulimalide-resistant human ovarian carcinoma cells have {beta}I-tubulin mutations and altered expression of {beta}II- and {beta}III-tubulin isotypes. Mol Cancer Ther. 2011, Jun 8.
Kauh J, Chanel-Vos C, Escuin D, Fanucchi MP, Harvey RD, Saba N, Shin DM, Gal A, Pan L, Kutner M, Ramalingam SS, Bender L, Marcus A, Giannakakou P, Khuri FR. Farnesyl transferase expression determines clinical response to the docetaxel-lonafarnib combination in patients with advanced malignancies. Cancer. 2011, Sept 1.
Carbonaro M, O'Brate A, Giannakakou P.Microtubule disruption targets HIF-1alpha mRNA to cytoplasmic P-bodies for translational repression J Cell Biol. 2011 .192(1):83-99.
2010
Jeske S, Tagawa ST, Olowokure O, Selzer J, Giannakakou P, Nanus DM. Carboplatin plus paclitaxel therapy after docetaxel in men with metastatic castrate resistant prostate cancer. Urol Oncol. 2010, May 5
Chanel-Vos C, Giannakakou P. CENP-E checks in microtubule-drug resistance Cell Cycle. 2010, 9(8):1456.
Gleghorn JP, Pratt ED, Denning D, Liu H, Bander NH, Tagawa ST, Nanus DM, Giannakakou P, Kirby BJ.Capture of circulating tumor cells from whole blood of prostate cancer patients using geometrically enhanced differential immunocapture (GEDI) and a prostate-specific antibody. Lab Chip. 2010, 10(1):27-9.
2009
Escuin D, Burke PA, McMahon-Tobin G, Hembrough T, Wang Y, Alcaraz AA, Leandro-García LJ, Rodríguez-Antona C, Snyder JP, Lavallee TM, Giannakakou P. The hematopoietic-specific beta1-tubulin is naturally resistant to 2-methoxyestradiol and protects patients from drug-induced myelosuppression.Cell Cycle. 2009 ,8(23):3914-24.
Wang X, Li J, Wang Y, Cho KJ, Kim G, Gjyrezi A, Koenig L, Giannakakou P, Shin HJ, Tighiouart M, Nie S, Chen ZG, Shin DM. HFT-T, a targeting nanoparticle, enhances specific delivery of paclitaxel to folate receptor-positive tumors. ACS Nano. 2009 ,3(10):3165-74.
Zhou J, Chanel Vos C, Gjyrezi A, YoshidaM, Khuri FR, Tamanoi F, Giannakakou P. The protein farnesyltransferase regulates HDAC6 Activity in a microtubule-dependent manner J Biol Chem, 2009, 284(15):9648-55.
2008
Thomas SL, Zhong D, Zhou W, Malik S, Liotta D, Snyder JP, Hamel E, Giannakakou P. EF24, a novel curcumin analog, disrupts the microtubule cytoskeleton and inhibits HIF-1 . Cell Cycle, 2009, 7(15):2409-17.
Mun J, Wang Y, Voll RJ, Escuin-Borras D, Giannakakou P, Goodman MM. Syntheses and biological activities of novel 2-methoxyestradiol analogs, 2-fluoroethoxyestradiol and 2-fluoropropanoxyestradiol, and a radiosynthesis of 2-[(18)F]fluoroethoxyestradiol for positron tomography. Nucl Med Biol, 2008, 35(5):615-22.
2007
Schafer-Hales K, Iaconelli J, Snyder JP, Prussia A, Nettles JH, El-Naggar A, Khuri FR, Giannakakou P, Marcus AI. Farnesyl transferase inhibitors impair chromosomal maintenance in cell lines and human tumors by compromising CENP-E and –F functionality. Mol. Cancer Therapeutics, 2007, 6(4):1317-28.
Ganesh T, Yang C, Norris A, Glass T, Bane S, Ravindra R, Banerjee A, Metaferia B, Thomas SL, Giannakakou P, Alcaraz AA, Lakdawala AS, Snyder JP, Kingston DG. Evaluation of the Tubulin-Bound Paclitaxel Conformation: Synthesis, Biology, and SAR Studies of C-4 to C-3' Bridge Paclitaxel Analogues. J Med Chem. 2007, 50(4):713-725.
2006
Kang SH, Cho HT, Devi S, Zhang Z, Escuin D, Liang Z, Mao H, Brat DJ, Olson JJ, Simons JW, Lavallee TM, Giannakakou P, Van Meir EG, Shim H. Antitumor effect of 2-methoxyestradiol in a rat orthotopic brain tumor model. Cancer Research, 2006, 66(24):11991-7.
Marcus AI, O’Brate A, Buey R, Zhou, J, Thomas S, Khuri FR, Diaz F , and Giannakakou P. Farnesyl transferase inhibitors reverse resistance to taxanes. Cancer Research, 2006, 66(17):8838-46.
K.C. Nicolaou, B.A. Pratt, S. Arseniyadis, M. Wartmann, A. O’Brate, P. Giannakakou. Molecular Design and Chemical Synthesis of a Highly Potent Epothilone. ChemMedChem, 2006, 1(1):41-44.
2005
Y. Wang, A. O’Brate, W. Zhou, and P. Giannakakou. Resistance to microtubule-stabilizing drugs involves two events: beta-tubulin mutation in one allele followed by loss of the second allele. Cell Cycle, 2005, 4(12):1847-53.
D. Escuin, E. Kline E., and P. Giannakakou. Both microtubule-stabilizing and microtubule-destabilizing drugs inhibit hypoxia-inducible factor-1alpha accumulation and activity by disrupting microtubule function. Cancer Research, 2005, 65(19):9021-28.
K.C. Nicolaou, M. Zak, S. Rahimipour, AA Estrada, SH Lee, A. O'Brate, P. Giannakakou, MR Ghadiri. Discovery of a biologically active thiostrepton fragment. J Am Chem Soc., 2005, 127(43):15042-15044.
R. M. Buey, I. Barasoain, E. Jackson, A. Meyer, P. Giannakakou, I. Paterson, S. Mooberry, J. M. Andreu and J. F. Díaz. Microtubule interactions with chemically diverse stabilizing agents: thermodynamics of binding to the Paclitaxel site predicts cytotoxicity. Chemistry & Biology, 2005, 12(12):1269-1279.
Y. Gökmen-Polar, D. Escuin, C. D. Walls, S.E. Soule, Y. Wang, K. L. Sanders, T.M. LaVallee, M. Wang, P. Giannakakou, and G. W. Sledge Jr. beta-Tubulin mutations are associated with resistance to 2-methoxyestradiol in MDA-MB-435 cancer cells. Cancer Research, 2005, 65(20):9406-14.
M.C. Edler, R.M. Buey, A.I. Marcus, C.D. Vanderwal, E.J. Sorensen, J.F. Díaz, P. Giannakakou, and E. Hamel. Cyclostreptin (FR182877), an antitumor tubulin-polymerizing agent deficient in enhancing tubulin assembly despite its high affinity for the taxoid site. Biochemistry, 2005 44(34):11525-11538.
Z. N. Demidenko, A. Rapisarda, M. Garayoa, P. Giannakakou, G. Melillo, and M.V. Blagosklonny. Accumulation of hypoxia-inducible factor-1alpha is limited by transcription-dependent depletion. Oncogene, 2005, 24(30):4829-38.
A.I. Marcus, S.L. Thomas, A. Zelnak, U. Peters, T. Kapoor, and P. Giannakakou. Mitotic kinesin inhibitors induce mitotic arrest and cell death in Taxol-resistant and -sensitive cancer cells. Journal of Biological Chemistry, 2005, 280(12):11569-11577.
A. Marcus, J. Zhou, A. O’Brate, E. Hamel, J. Wong, M. Nivens, A. El-Naggar, T.P. Yao, F.R. Khuri, and P. Giannakakou. The synergistic combination of the farnesyl transferase inhibitor lonafarnib and paclitaxel enhances tubulin acetylation and requires a functional tubulin deacetylase. Cancer Research, 2005, 65(9):3883-3893.
J. Zhou and P. Giannakakou. Targeting microtubules for cancer chemotherapy. Current Medicinal Chemistry-Anticancer Agents, 2005, 5(1):65-71.
C. Tan, R.G. de Noronha, A.J. Roecker, B. Pyrzynska, F. Khwaja, Z. Zhang, H. Zhang, P. Giannakakou, W. Zhou, J.J. Olson, K.C. Nicolaou, and E.G. Van Meir. Identification of a novel small-molecule inhibitor of the hypoxia-inducible factor 1 pathway. Cancer Research, 2005, 65(2):605-612.
2004
J. Zhou, A. O’Brate, A. Zelnak, and P. Giannakakou. Survivin deregulation in beta-tubulin mutant ovarian cancer cells underlies their compromised mitotic response to taxol. Cancer Research, 2004, 64(23):8708-14.
D. Escuin, J. Simons, and P. Giannakakou. Exploitation of the HIF axis for cancer therapy. Cancer Biology and Therapy, 2004, 3(7):608-611.
K.C. Nicolaou, S.A. Snyder, N. Giuseppone, X. Huang, M. Bella, M.V. Reddy, P.B. Rao, A.E Koumbis, A. O'Brate, and P. Giannakakou. Studies toward diazonamide A: development of a hetero-pinacol macrocyclization cascade for the construction of the bis-macrocyclic framework of the originally proposed structure. J Am Chem Soc. 2004, 126(32):10174-82.
K.C. Nicolaou, J. Hao, M.V. Reddy, P.B. Rao, G. Rassias, S.A. Snyder, X. Huang, D.Y. Chen, W.E. Brenzovich, N. Giuseppone, A. O'Brate, and P. Giannakakou. Chemistry and biology of diazonamide A: second total synthesis and biological investigations. J Am Chem Soc. 2004, 126 (40):12897-12906.
R. Buey, J.F. Diaz, J.M. Andreu, A. O’Brate, P. Giannakakou, K.C. Nicolaou, P.K. Sasmal, A. Ritzen, and K. Namoto. Interaction of epothilone analogs with the paclitaxel binding site: relationship between binding affinity, microtubule stabilization, and cytotoxicity. Chemistry and Biology, 2004, 11(2):225-236.
2003
K.C. Nicolaou, D.W. Kim, R. Baati, A. O’Brate, and P. Giannakakou. Total synthesis and biological evaluation of (–) apicularen A and analogues thereof. Chemistry, 2003, 9(24):6177-6191.
A. O’Brate and P. Giannakakou. The importance of p53 location: nuclear or cytoplasmic zip code? Drug Resist Updat., 2003, 6(6):313-322.
K.C. Nicolaou, Y. Li, K. Sugita, H. Monenschein, P. Guntupalli, H.J. Mitchell, K.C. Fylaktakidou, D. Vourloumis, P. Giannakakou, and A. O'Brate. Total synthesis of apoptolidin: completion of the synthesis and analogue synthesis and evaluation. J Am Chem Soc, 2003, 125(50):15443-54.
K.C. Nicolaou, P.K. Sasmal, G. Rassias, M.V. Reddy, K.H. Altmann, M. Wartmann, A. O'Brate, and P. Giannakakou. Design, synthesis, and biological properties of highly potent epothilone B analogues. Angew Chem Int Ed Engl., 2003 Aug 4, 42(30):3515-3520.
N.J. Mabjeesh, D. Escuin, T.M. LaVallee, V.S. Pribluda, G.M. Swartz, M.S. Johnson, M.T. Willard, H. Zhong, J. Simons, and P. Giannakakou. 2ME2 inhibits tumor growth and angiogenesis by disrupting microtubules and dysregulating HIF. Cancer Cell, 2003, 3(4):363-375.
2002
P. Giannakakou, M. Nakano, K.C. Nicolaou, A. O’Brate, J. Yu, M.V. Blagosklonny, U.F. Greber, and T. Fojo. Enhanced microtubule-dependent trafficking and p53 nuclear accumulation by suppression of microtubule dynamics. Proc. Natl. Acad. Sci. USA, 2002, 99(16):10855-10860.
J. Zhou, K. Gupta, J. Yao, K. Ye, D. Panda, P. Giannakakou, and H.C. Joshi. Paclitaxel-resistant human ovarian cancer cells undergo c-Jun NH2-terminal kinase-mediated apoptosis in response to noscapine. Journal of Biological Chemistry, 2002, 277(42):39777-39785.
K.C. Nicolaou, A. Ritzén, K. Namoto, R.M. Buey, J.F. Díaz, J.M. Andreu, M. Wartmann, K-H. Altmann, A. O’Brate, and P. Giannakakou. Chemical synthesis and biological evaluation of novel epothilone B and trans-12,13-cyclopropyl epothilone B analogues. Tetrahedron, 2002, 58:6413-6432.
D.E. Pryor, A. O'Brate, G. Bilcer, J.F. Díaz, Y. Wang, Y. Wang, M. Kabaki, M.K. Jung, J.M. Andreu, A.K. Ghosh, P. Giannakakou, and E. Hamel. The microtubule stabilizing agent laulimalide does not bind in the taxoid site, kills cells resistant to paclitaxel and epothilones, and may not require its epoxide moiety for activity. Biochemistry, 2002, 41(29):9109-9115.
2001
P. Giannakakou, R. Robey, T. Fojo, and M.V. Blagosklonny. Low concentrations of paclitaxel induce cell type-dependent p53, p21 and G1/G2 arrest instead of mitotic arrest: molecular determinants of paclitaxel-induced cytotoxicity. Oncogene, 2001, 20(29):3806-13.
K.C. Nicolaou, K. Namoto, A. Ritzén, T. Ulven, M. Shoji, J. Li, G. D’Amico, D. Liotta, C.T. French, and P. Giannakakou. Chemical synthesis and biological evaluation of cis- and trans-12,13-cyclopropyl and 12,13-cyclobutyl epothilones and related pyridine side chain analogues. J Am Chem Soc, 2001, 123(38):9313-23.
K.C. Nicolaou K. Namoto, J. Li, A. Ritzen, T. Ulven, M. Shoji, D. Zaharevitz, R. Gussio, D.L. Sackett, R.D. Ward, A. Hensler, T. Fojo, and P. Giannakakou. Synthesis and biological evaluation of 12,13-cyclopropyl and 12,13-cyclobutyl epothilones. ChemBioChem, 2001, 2(1):69-75.
M.S. Poruchynsky, P. Giannakakou, Y. Ward, J.C. Bulinski, W.G. Telford, R.W. Robey, and T. Fojo. Accompanying protein alterations in malignant cells with a microtubule-polymerizing drug-resistance phenotype and a primary resistance mechanism. Biochem Pharmacol, 2001, 62(11):1469-80.
M.I. Nicoletti, G. Valoti, P. Giannakakou, Z. Zhan, J-H. Kim, V. Lucchini, F. Landoni, J.G. Mayo, R. Giavazzi, and T. Fojo. Expression of beta-tubulin isotypes in human ovarian carcinoma xenografts and in a sub-panel of human cancer cell lines from the NCI-Anticancer Drug Screen: correlation with sensitivity to microtubule active agents. Clinical Cancer Research, 2001, 7(9):2912-2922.
M.V. Blagosklonny, P. Giannakakou, K.M. Ryan, K.H. Vousden, and T. Fojo. Inhibition of HIF-1 and wild-type p53-stimulated transcription by codon Arg175 p53 mutants with selective loss of functions. Carcinogenesis, 2001, 22(6):861-867.
2000
P. Giannakakou, D.L. Sackett, Y. Ward, K. Webster, M. Blagosklonny, and T. Fojo. p53 is associated with cellular microtubules and is transported to the nucleus by dynein. Nature Cell Biology, 2000, 2(10):709-717.
P. Giannakakou, R. Gussio, E. Nogales, K.H. Downing, D. Zaharevitz, B. Bollbuck, G. Poy, D. Sackett, K.C. Nicolaou, and T. Fojo. A common pharmacophore for epothilone and taxanes: molecular basis for drug resistance-conferred by tubulin mutations in human cancer cells. Proc. Natl. Acad. Sci. USA, 2000, 97(6):2904-2909.
P. Giannakakou, G. Poy, Z. Zhan, M. Blagosklonny, and T. Fojo. Paclitaxel selects for mutant or pseudo-null p53 in drug resistance associated with tubulin mutations in human cancer cells. Oncogene, 2000, 19(27):3078-3085.
P. Giannakakou, D.L. Sackett, and T. Fojo. Tubulin/Microtubules: still a promising target for new chemotherapeutic agents. Journal of the National Cancer Institute, 2000; 92(3):182-183.
P. Giannakakou and T. Fojo. Discodermolide: just another microtubule-stabilizing agent? No! A lesson in synergy. Clinical Cancer Research, 2000, 6(5):1613-15.
K.C. Nicolaou, R. Scarpelli, B. Bollbuck, B. Werschkun, A. Pereira, M. Wartmann, K-H. Altmann, D. Zaharevitz, R. Gussio, and P. Giannakakou. Chemical synthesis and biological properties of pyridine epothilones. Chemistry and Biology, 2000, 7(8):593-599.
T. Fojo and P. Giannakakou. Taxol and other microtubule-interacting agents. Current Opinion in Oncologic, Endocrine and Metabolic Investigational Drugs, 2000, 2(3):293-304.
R. Gussio, T. Fojo, and P. Giannakakou. Reply to “Mutants yield a pharmacophore model for the tubulin-paclitaxel binding site.” Trends in Pharmacological Sciences, 2000, 21(9):323-324.
1999
L. Gabriele, J. Phung, J. Fukumoto, D. Segal, I.M. Wang, P. Giannakakou, N.A. Giese, K. Ozato, and H.C. Morse III. Regulation of apoptosis in myeloid cells by interferon consensus sequence-binding protein. Journal of Experimental Medicine, 1999, 190(3):411-21.
1998
P. Giannakakou, L. Villalba, H. Li, M. Poruchynsky, and T. Fojo. Combinations of paclitaxel and vinblastine and their effects on tubulin polymerization and cellular cytotoxicity: characterization of a synergistic schedule. International Journal of Cancer, 1998, 75(1):57-63.
D.G.I. Kingston, A.G. Chaudhary, M.D. Chordia, M. Gharpure, A.A.L. Gunatilaka, P.I. Higgs, J.M. Rimoldi, L. Samala, P.G. Jagtap, P. Giannakakou, Y.Q. Jiang, C.M. Lin, E. Hamel, B.H. Long, C.R. Fairchild, and K.A. Johnston. Synthesis and biological evaluation of 2-acyl analogues of paclitaxel (Taxol). Journal of Medicinal Chemistry, 1998, 41(19):3715-3726.
M.V. Blagosklonny, P. Giannakakou, M. Wojtowicz, L.Y. Romanova, K.B. Ain, S.E. Bates, and T. Fojo. Effects of p53-expressing adenovirus on the chemosensitivity and differentiation of anaplastic thyroid cancer cells. Journal of Clinical Endocrinology and Metabolism, 1998, 83(7):2516-2522.
T-H. Wang, H-S. Wang, H. Ichijo, P. Giannakakou, J.S. Foster, T. Fojo, and J. Wimalasena. Microtubule-interfering agents activate c-Jun N-terminal kinase/stress-activated protein kinase through both Ras and apoptosis signal-regulating kinase pathways. Journal of Biological Chemistry, 1998, 273(9):4928-4936.
1997
P. Giannakakou, D.L. Sackett, Y-K. Kang, Z. Zhan, J. Regis, T. Fojo, and M. Poruchynsky. Paclitaxel-resistant human ovarian cancer cells have mutant beta-tubulins that exhibit impaired paclitaxel-driven tubulin polymerization. Journal of Biological Chemistry, 1997, 272(27):17118-17125.
M. Blagosklonny, P. Giannakakou, W. S. El-Deiry, D. G. I. Kingston, P. I. Higgs, L. Neckers, and T. Fojo. Raf-1/bcl-2 phosphorylation: a step from microtubule damage to cell death. Cancer Research, 1997, 57(1):130-135.
R.J. Kowalski, P. Giannakakou, and E. Hamel. Activities of the microtubule-stabilizing agents epothilones A and B with purified tubulin and in cells resistant to paclitaxel (Taxol(R)). Journal of Biological Chemistry, 1997, 272(4):2534-2541.
D.L. Sackett, P. Giannakakou, M. Poruchynsky, and T. Fojo. Tubulin from paclitaxel-resistant cells as a probe for novel anti microtubule agents. Cancer Chemotherapy and Pharmacology, 1997, 40(3):228-232.
R.J. Kowalski, P. Giannakakou, S.P. Guanasekera, R.E. Longley, B.W. Day, and E. Hamel. The microtubule-stabilizing agent discodermolide competitively inhibits the binding of paclitaxel (Taxol) to tubulin polymers, enhances tubulin nucleation reactions more potently than paclitaxel, and inhibits the growth of paclitaxel-resistant cells. Molecular Pharmacology, 1997, 52(4):613-622.
K.C. Nicolaou, D. Vourloumis, T. Li, J. Pastor, N. Wissinger, Y. He, S. Nikovic, F. Sarabia, H. Vallberg, F. Roschangar, N.P. King, M. Ray, V. Finlay, P. Giannakakou, P. Verdier-Pinard, and E. Hamel. Designed Epothilones: combinatorial synthesis, tubulin assembly properties, and cytotoxic action against Taxol-resistant tumor cells. Angew. Chem. Int. Ed. Engl., 1997, 36(19):2097-2103.
K.C. Nicolaou, N. Winssinger, J. Pastor, S. Ninkovic, F. Sarabla, Y. He, D. Vourloumis, Z. Yang, T. Li, P. Giannakakou, and E. Hamel. Synthesis of epothilones A and B in solid and solution phase. Nature, 1997, 387(6630):268-272.
1996
S. Scala, K. Wosikowski, P. Giannakakou, P. Valle, J. Biedler, B. Spengler, E. Lucarelli, S.E. Bates, and C. Thiele. Brain-derived neurotrophic factor protects neuroblastoma cells from vinblastine toxicity. Cancer Research, 1996, 56(16):3737-42.
A. Tiligada, P. Giannakakou, I. Karavokyros, and A. Delitheos. Effect of calcium channel blockers on the action of various antitumour agents in the yeast Saccharomyces cerevisiae. Journal of Applied Bacteriology, 1996, 81(5):481-485.
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