2022

• AR-V7 exhibits non-canonical mechanisms of nuclear import and chromatin engagement in castrate-resistant prostate cancer.

  Kim S, Au CC, Jamalruddin MAB, Abou-Ghali NE, Mukhtar E, Portella L, Berger A, Worroll D, Vatsa P, Rickman DS, Nanus DM, Giannakakou P. Elife. 2022 Jul 18;11:e73396. doi: 10.7554/eLife.73396.PMID: 35848798

2021

• CLIP-170S is a microtubule +TIP variant that confers resistance to taxanes by impairing drug-target engagement.

Thakkar PV, Kita K, del Castillo U, Galletti G, Madhukar N, Navarro EV, Barasoain I, Goodson HV, Sackett D, Díaz JF, Lu Y, RoyChoudhury A, Molina H, Elemento O, Shah MA, Giannakakou P.Dev Cell. 2021 Dec 6;56(23):3264-3275.e7. doi: 10.1016/j.devcel.2021.09.023. Epub 2021 Oct 20.PMID: 34672971

• Androgen receptor variant shows heterogeneous expression in prostate cancer according to differentiation stage.

  Gjyrezi A, Galletti G, Zhang J, Worroll D, Sigouros M, Kim S, Cooley V, Ballman KV, Ocean AJ, Shah MA, Scandura JM, Sboner A, Nanus DM, Beltran H, Tagawa S, Giannakakou P.Commun Biol. 2021 Jun 24;4(1):785. doi: 10.1038/s42003-021-02321-9.PMID: 34168263

• Circulating tumor cell chromosomal instability and neuroendocrine phenotype by immunomorphology and poor outcomes in men with mCRPC treated with abiraterone or enzalutamide

  Brown LC, Halabi S, Schonhoft JD, Yang Q, Luo J, Nanus DM, Giannakakou P, Szmulewitz RZ, Danila DC, Barnett ES, Carbone EA, Zhao JL, Healy P, Anand M, Gill A, Jendrisak A, Berry WR, Gupta S, Gregory SG, Wenstrup R, Antonarakis ES, George DJ, Scher HI, Armstrong AJ.Clin Cancer Res. 2021 Apr 5:clincanres.3471.2020. doi: 10.1158/1078-0432.CCR-20-3471. Online ahead of print.PMID: 33820782

• Circulating Tumor Cell Genomic Evolution and Hormone Therapy Outcomes in Men with Metastatic Castration-Resistant Prostate Cancer

  Gupta S, Halabi S, Kemeny G, Anand M, Giannakakou P, Nanus DM, George DJ, Gregory SG, Armstrong AJ.Mol Cancer Res. 2021 Mar 26. doi: 10.1158/1541-7786.MCR-20-0975. Online ahead of print.PMID: 33771885

2020

• Prospective Multicenter Study of Circulating Tumor Cell AR-V7 and Taxane Versus Hormonal Treatment Outcomes in Metastatic Castration-Resistant Prostate Cancer.

  Armstrong AJ, Luo J, Nanus DM, Giannakakou P, Szmulewitz RZ, Danila DC, Healy P, Anand M, Berry WR, Zhang T, Harrison MR, Lu C, Chen Y, Galletti G, Schonhoft JD, Scher HI, Wenstrup R, Tagawa ST, Antonarakis ES, George DJ, Halabi S.JCO Precis Oncol. 2020 Oct 28;4:PO.20.00200. doi: 10.1200/PO.20.00200. eCollection 2020.PMID: 33154984

• Quantitative analysis of taxane drug target engagement of microtubules in circulating tumor cells from metastatic castration resistant prostate cancer patients treated with CRXL301, a nanoparticle of docetaxel.

  Mukhtar E, Worroll D, Galletti G, Schuster S, Piha-Paul SA, Giannakakou P.Cancer Drug Resist. 2020;3:636-646. doi: 10.20517/cdr.2019.116. Epub 2020 Apr 17.PMID: 33062959

• Multicenter Phase II Study of Cabazitaxel in Advanced Gastroesophageal Cancer: Association of HER2 Expression and M2-Like Tumor-Associated Macrophages with Patient Outcome.

  Shah MA, Enzinger P, Ko AH, Ocean AJ, Philip PA, Thakkar PV, Cleveland K, Lu Y, Kortmansky J, Christos PJ, Zhang C, Kaur N, Elmonshed D, Galletti G, Sarkar S, Bhinder B, Pittman ME, Plotnikova OM, Kotlov N, Frenkel F, Bagaev A, Elemento O, Betel D, Giannakakou P, Lenz HJ.Clin Cancer Res. 2020 Sep 15;26(18):4756-4766. doi: 10.1158/1078-0432.CCR-19-3920. Epub 2020 Jul 8.PMID: 32641434

• Taxane resistance in prostate cancer is mediated by decreased drug-target engagement.

  Gjyrezi A, Xie F, Voznesensky O, Khanna P, Calagua C, Bai Y, Kung J, Wu J, Corey E, Montgomery B, Mace S, Gianolio DA, Bubley GJ, Balk SP, Giannakakou P, Bhatt RS.J Clin Invest. 2020 Jun 1;130(6):3287-3298. doi: 10.1172/JCI132184.PMID: 32478682

• Microtubule Engagement with Taxane Is Altered in Taxane-Resistant Gastric Cancer.

  Galletti G, Zhang C, Gjyrezi A, Cleveland K, Zhang J, Powell S, Thakkar PV, Betel D, Shah MA, Giannakakou P.Clin Cancer Res. 2020 Jul 15;26(14):3771-3783. doi: 10.1158/1078-0432.CCR-19-3018. Epub 2020 Apr 22.PMID: 32321717

2019

• A Bayesian machine learning approach for drug target identification using diverse data types.

  Madhukar NS, Khade PK, Huang L, Gayvert K, Galletti G, Stogniew M, Allen JE, Giannakakou P, Elemento O.Nat Commun. 2019 Nov 19;10(1):5221. doi: 10.1038/s41467-019-12928-6.PMID: 31745082 

• Clinical Significance of AR-V567es in Prostate Cancer-Response.

  Tagawa ST, Antonarakis ES, Gjyrezi A, Galletti G, Giannakakou P.Clin Cancer Res. 2019 Oct 1;25(19):6010-6011. doi: 10.1158/1078-0432.CCR-19-1820.PMID: 31575715 

• Pharmacodynamic study of radium-223 in men with bone metastatic castration resistant prostate cancer.

  Armstrong AJ, Gupta S, Healy P, Kemeny G, Leith B, Zalutsky MR, Spritzer C, Davies C, Rothwell C, Ware K, Somarelli JA, Wood K, Ribar T, Giannakakou P, Zhang J, Gerber D, Anand M, Foo WC, Halabi S, Gregory SG, George DJ.PLoS One. 2019 May 28;14(5):e0216934. doi: 10.1371/journal.pone.0216934. eCollection 2019.PMID: 31136607  

• Prospective Multicenter Validation of Androgen Receptor Splice Variant 7 and Hormone Therapy Resistance in High-Risk Castration-Resistant Prostate Cancer: The PROPHECY Study.

  Armstrong AJ, Halabi S, Luo J, Nanus DM, Giannakakou P, Szmulewitz RZ, Danila DC, Healy P, Anand M, Rothwell CJ, Rasmussen J, Thornburg B, Berry WR, Wilder RS, Lu C, Chen Y, Silberstein JL, Kemeny G, Galletti G, Somarelli JA, Gupta S, Gregory SG, Scher HI, Dittamore R, Tagawa ST, Antonarakis ES, George DJ.J Clin Oncol. 2019 May 1;37(13):1120-1129. doi: 10.1200/JCO.18.01731. Epub 2019 Mar 13.PMID: 30865549 

• Androgen receptor nuclear localization correlates with AR-V7 mRNA expression in circulating tumor cells (CTCs) from metastatic castration resistance prostate cancer patients.Worroll D, Galletti G, Gjyrezi A, Nanus DM, Tagawa ST, Giannakakou P.Phys Biol. 2019 Mar 22;16(3):036003. doi: 10.1088/1478-3975/ab073a.PMID: 30763921 

2018

• Expression of AR-V7 and ARv567es in Circulating Tumor Cells Correlates with Outcomes to Taxane Therapy in Men with Metastatic Prostate Cancer Treated in TAXYNERGY.

  Tagawa ST, Antonarakis ES, Gjyrezi A, Galletti G, Kim S, Worroll D, Stewart J, Zaher A, Szatrowski TP, Ballman KV, Kita K, Tasaki S, Bai Y, Portella L, Kirby BJ, Saad F, Eisenberger MA, Nanus DM, Giannakakou P.Clin Cancer Res. 2019 Mar 15;25(6):1880-1888. doi: 10.1158/1078-0432.CCR-18-0320. Epub 2018 Oct 9.PMID: 30301829

• Identification of distinct nanoparticles and subsets of extracellular vesicles by asymmetric flow field-flow fractionation.

  Zhang H, Freitas D, Kim HS, Fabijanic K, Li Z, Chen H, Mark MT, Molina H, Martin AB, Bojmar L, Fang J, Rampersaud S, Hoshino A, Matei I, Kenific CM, Nakajima M, Mutvei AP, Sansone P, Buehring W, Wang H, Jimenez JP, Cohen-Gould L, Paknejad N, Brendel M, Manova-Todorova K, Magalhães A, Ferreira JA, Osório H, Silva AM, Massey A, Cubillos-Ruiz JR, Galletti G, Giannakakou P, Cuervo AM, Blenis J, Schwartz R, Brady MS, Peinado H, Bromberg J, Matsui H, Reis CA, Lyden D.Nat Cell Biol. 2018 Mar;20(3):332-343. doi: 10.1038/s41556-018-0040-4. Epub 2018 Feb 19.PMID: 29459780 

2017

• Randomized, Noncomparative, Phase II Trial of Early Switch From Docetaxel to Cabazitaxel or Vice Versa, With Integrated Biomarker Analysis, in Men With Chemotherapy-Naïve, Metastatic, Castration-Resistant Prostate Cancer.

  Antonarakis ES, Tagawa ST, Galletti G, Worroll D, Ballman K, Vanhuyse M, Sonpavde G, North S, Albany C, Tsao CK, Stewart J, Zaher A, Szatrowski T, Zhou W, Gjyrezi A, Tasaki S, Portella L, Bai Y, Lannin TB, Suri S, Gruber CN, Pratt ED, Kirby BJ, Eisenberger MA, Nanus DM, Saad F, Giannakakou P; TAXYNERGY Investigators.J Clin Oncol. 2017 Oct 1;35(28):3181-3188. doi: 10.1200/JCO.2017.72.4138. Epub 2017 Jun 20.PMID: 28632486 

• Widespread Mitotic Bookmarking by Histone Marks and Transcription Factors in Pluripotent Stem Cells.

  Liu Y, Pelham-Webb B, Di Giammartino DC, Li J, Kim D, Kita K, Saiz N, Garg V, Doane A, Giannakakou P, Hadjantonakis AK, Elemento O, Apostolou E.Cell Rep. 2017 May 16;19(7):1283-1293. doi: 10.1016/j.celrep.2017.04.067.PMID: 28514649 

• Using circulating tumor cells to advance precision medicine in prostate cancer.

  Galletti G, Worroll D, Nanus DM, Giannakakou P.J Cancer Metastasis Treat. 2017;3:190-205. doi: 10.20517/2394-4722.2017.45. Epub 2017 Sep 27.PMID: 29707651 

2016

• A SIRT2-Selective Inhibitor Promotes c-Myc Oncoprotein Degradation and Exhibits Broad Anticancer Activity.

  Jing H, Hu J, He B, Negrón Abril YL, Stupinski J, Weiser K, Carbonaro M, Chiang YL, Southard T, Giannakakou P, Weiss RS, Lin H.Cancer Cell. 2016 May 9;29(5):767-768. doi: 10.1016/j.ccell.2016.04.005. Epub 2016 May 9.PMID: 27165747 

2015

• CANCER. Cancer therapies that are gone with the Wnt.Nanus DM, Giannakakou P.Science. 2015 Sep 18;349(6254):1283-4. doi: 10.1126/science.aad2448.

  PMID: 26383936

• Cytotoxic chemotherapy in the treatment of advanced renal cell carcinoma in the era of targeted therapy.

  Diamond E, Molina AM, Carbonaro M, Akhtar NH, Giannakakou P, Tagawa ST, Nanus DM.Crit Rev Oncol Hematol. 2015 Dec;96(3):518-26. doi: 10.1016/j.critrevonc.2015.08.007. Epub 2015 Aug 13.

  PMID: 26321263 Review.

• β-1 tubulin R307H SNP alters microtubule dynamics and affects severity of a hereditary thrombocytopenia.

  Basciano PA, Matakas J, Pecci A, Civaschi E, Cagioni C, Bompiani N, Burger P, Christos P, Snyder JP, Bussel J, Balduini CL, Giannakakou P, Noris P.J Thromb Haemost. 2015 Apr;13(4):651-9. doi: 10.1111/jth.12824. Epub 2015 Jan 22.

  PMID: 25529050  

2014

• ERG induces taxane resistance in castration-resistant prostate cancer.

  Galletti G, Matov A, Beltran H, Fontugne J, Miguel Mosquera J, Cheung C, MacDonald TY, Sung M, O'Toole S, Kench JG, Suk Chae S, Kimovski D, Tagawa ST, Nanus DM, Rubin MA, Horvath LG, Giannakakou P, Rickman DS.Version 2. Nat Commun. 2014 Nov 25;5:5548. doi: 10.1038/ncomms6548.PMID: 25420520 

• Decade in review-funding in cancer research: National Cancer Institute awards-a work in progress.

  Fojo T, Giannakakou P.Nat Rev Clin Oncol. 2014 Nov;11(11):634-6. doi: 10.1038/nrclinonc.2014.173. Epub 2014 Oct 14.PMID: 25311348 

• Circulating tumor cells in prostate cancer diagnosis and monitoring: an appraisal of clinical potential.

  Galletti G, Portella L, Tagawa ST, Kirby BJ, Giannakakou P, Nanus DM.Mol Diagn Ther. 2014 Aug;18(4):389-402. doi: 10.1007/s40291-014-0101-8.PMID: 24809501 

• RABbing cancer the wrong way.

  Khade PK, Giannakakou P.Proc Natl Acad Sci U S A. 2014 Aug 5;111(31):11230-1. doi: 10.1073/pnas.1410788111. Epub 2014 Jul 22.PMID: 25053807 

• NAD+ and SIRT3 control microtubule dynamics and reduce susceptibility to antimicrotubule agents.

  Harkcom WT, Ghosh AK, Sung MS, Matov A, Brown KD, Giannakakou P, Jaffrey SR.Proc Natl Acad Sci U S A. 2014 Jun 17;111(24):E2443-52. doi: 10.1073/pnas.1404269111. Epub 2014 Jun 2.PMID: 24889606 

• Androgen receptor splice variants determine taxane sensitivity in prostate cancer.

  Thadani-Mulero M, Portella L, Sun S, Sung M, Matov A, Vessella RL, Corey E, Nanus DM, Plymate SR, Giannakakou P.Cancer Res. 2014 Apr 15;74(8):2270-2282. doi: 10.1158/0008-5472.CAN-13-2876. Epub 2014 Feb 20.PMID: 24556717 

2013

• Circulating tumor cells from prostate cancer patients interact with E-selectin under physiologic blood flow.

  Gakhar G, Navarro VN, Jurish M, Lee GY, Tagawa ST, Akhtar NH, Seandel M, Geng Y, Liu H, Bander NH, Giannakakou P, Christos PJ, King MR, Nanus DM.PLoS One. 2013 Dec 27;8(12):e85143. doi: 10.1371/journal.pone.0085143. eCollection 2013.PMID: 24386459 

• Isolation of breast cancer and gastric cancer circulating tumor cells by use of an anti HER2-based microfluidic device.

  Galletti G, Sung MS, Vahdat LT, Shah MA, Santana SM, Altavilla G, Kirby BJ, Giannakakou P.Lab Chip. 2014 Jan 7;14(1):147-56. doi: 10.1039/c3lc51039e. Epub 2013 Nov 7.PMID: 24202699 

• BRCA1 regulates microtubule dynamics and taxane-induced apoptotic cell signaling.

  Sung M, Giannakakou P.Oncogene. 2014 Mar 13;33(11):1418-28. doi: 10.1038/onc.2013.85. Epub 2013 Mar 25.PMID: 23524581 

2012

• The beta 1 tubulin R307H single nucleotide polymorphism is associated with treatment failures in immune thrombocytopenia (ITP).

  Basciano PA, Bussel J, Hafeez Z, Christos PJ, Giannakakou P.Br J Haematol. 2013 Jan;160(2):237-43. doi: 10.1111/bjh.12124. Epub 2012 Nov 15.PMID: 23157319 

•  Isolation and characterization of circulating tumor cells in prostate cancer.Diamond E, Lee GY, Akhtar NH, Kirby BJ, Giannakakou P, Tagawa ST, Nanus DM.Front Oncol. 2012 Oct 11;2:131. doi: 10.3389/fonc.2012.00131. eCollection 2012.PMID: 23087897 

• Androgen receptor on the move: boarding the microtubule expressway to the nucleus.

  Thadani-Mulero M, Nanus DM, Giannakakou P.Cancer Res. 2012 Sep 15;72(18):4611-5. doi: 10.1158/0008-5472.CAN-12-0783.PMID: 22987486 

• Microtubules regulate hypoxia-inducible factor-1α protein trafficking and activity: implications for taxane therapy.

  Carbonaro M, Escuin D, O'Brate A, Thadani-Mulero M, Giannakakou P.J Biol Chem. 2012 Apr 6;287(15):11859-69. doi: 10.1074/jbc.M112.345587. Epub 2012 Feb 24.PMID: 22367210 

• Integrating image analysis algorithms in a web interface for the quantification of microtubule dynamics.Kong KY, Marcus AI, Giannakakou P, Wang MD.Int J Comput Biol Drug Des. 2012;5(3-4):298-313. doi: 10.1504/IJCBDD.2012.049211. Epub 2012 Sep 24.PMID: 23013655

• Functional characterization of circulating tumor cells with a prostate-cancer-specific microfluidic device.

  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.PLoS One. 2012;7(4):e35976. doi: 10.1371/journal.pone.0035976. Epub 2012 Apr 27.PMID: 22558290

2011

• Taxane-induced blockade to nuclear accumulation of the androgen receptor predicts clinical responses in metastatic prostate cancer.

  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.Cancer Res. 2011 Sep 15;71(18):6019-29. doi: 10.1158/0008-5472.CAN-11-1417. Epub 2011 Jul 28.PMID: 21799031 

• A folate receptor-targeting nanoparticle minimizes drug resistance in a human cancer model.

  Wang X, Li J, Wang Y, Koenig L, Gjyrezi A, Giannakakou P, Shin EH, Tighiouart M, Chen ZG, Nie S, Shin DM.ACS Nano. 2011 Aug 23;5(8):6184-94. doi: 10.1021/nn200739q. Epub 2011 Jul 11.PMID: 21728341 

• Peloruside- and laulimalide-resistant human ovarian carcinoma cells have βI-tubulin mutations and altered expression of βII- and βIII-tubulin isotypes.

  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.Mol Cancer Ther. 2011 Aug;10(8):1419-29. doi: 10.1158/1535-7163.MCT-10-1057. Epub 2011 Jun 8.PMID: 21653684 

• Farnesyl transferase expression determines clinical response to the docetaxel-lonafarnib combination in patients with advanced malignancies.

  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.Cancer. 2011 Sep 1;117(17):4049-59. doi: 10.1002/cncr.26004. Epub 2011 Mar 1.PMID: 21365629 

• Microtubule disruption targets HIF-1alpha mRNA to cytoplasmic P-bodies for translational repression.

  Carbonaro M, O'Brate A, Giannakakou P.J Cell Biol. 2011 Jan 10;192(1):83-99. doi: 10.1083/jcb.201004145.PMID: 21220510 

2010

• Carboplatin plus paclitaxel therapy after docetaxel in men with metastatic castrate resistant prostate cancer.

  Jeske S, Tagawa ST, Olowokure O, Selzer J, Giannakakou P, Nanus DM.Urol Oncol. 2011 Nov-Dec;29(6):676-81. doi: 10.1016/j.urolonc.2009.12.023. Epub 2010 May 7.PMID: 20451413

• CENP-E checks in microtubule-drug resistance.

  Chanel-Vos C, Giannakakou P.Cell Cycle. 2010 Apr 15;9(8):1456. doi: 10.4161/cc.9.8.11382. Epub 2010 Apr 15.PMID: 20421712 

2009

• The hematopoietic-specific beta1-tubulin is naturally resistant to 2-methoxyestradiol and protects patients from drug-induced myelosuppression.

  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.Cell Cycle. 2009 Dec;8(23):3914-24. doi: 10.4161/cc.8.23.10105. Epub 2009 Dec 16.PMID: 19901556

• Capture of circulating tumor cells from whole blood of prostate cancer patients using geometrically enhanced differential immunocapture (GEDI) and a prostate-specific antibody.

  Gleghorn JP, Pratt ED, Denning D, Liu H, Bander NH, Tagawa ST, Nanus DM, Giannakakou PA, Kirby BJ.Lab Chip. 2010 Jan 7;10(1):27-9. doi: 10.1039/b917959c. Epub 2009 Nov 16.PMID: 20024046 

• HFT-T, a targeting nanoparticle, enhances specific delivery of paclitaxel to folate receptor-positive tumors.

  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.ACS Nano. 2009 Oct 27;3(10):3165-74. doi: 10.1021/nn900649v.PMID: 19761191 

• The protein farnesyltransferase regulates HDAC6 activity in a microtubule-dependent manner.

  Zhou J, Vos CC, Gjyrezi A, Yoshida M, Khuri FR, Tamanoi F, Giannakakou P.J Biol Chem. 2009 Apr 10;284(15):9648-55. doi: 10.1074/jbc.M808708200. Epub 2009 Feb 18.PMID: 19228685 

2008

• Syntheses and biological activities of novel 2-methoxyestradiol analogs, 2-fluoroethoxyestradiol and 2-fluoropropanoxyestradiol, and a radiosynthesis of 2-[(18)F]fluoroethoxyestradiol for positron emission tomography.

  Mun J, Wang Y, Voll RJ, Escuin-Borras D, Giannakakou P, Goodman MM.Nucl Med Biol. 2008 Jul;35(5):615-22. doi: 10.1016/j.nucmedbio.2008.04.003.PMID: 18589306 

• EF24, a novel curcumin analog, disrupts the microtubule cytoskeleton and inhibits HIF-1.

  Thomas SL, Zhong D, Zhou W, Malik S, Liotta D, Snyder JP, Hamel E, Giannakakou P.Cell Cycle. 2008 Aug;7(15):2409-17. doi: 10.4161/cc.6410. Epub 2008 Jun 9.PMID: 18682687

2007

• Farnesyl transferase inhibitors impair chromosomal maintenance in cell lines and human tumors by compromising CENP-E and CENP-F function.

  Schafer-Hales K, Iaconelli J, Snyder JP, Prussia A, Nettles JH, El-Naggar A, Khuri FR, Giannakakou P, Marcus AI.Mol Cancer Ther. 2007 Apr;6(4):1317-28. doi: 10.1158/1535-7163.MCT-06-0703.PMID: 17431110

• Evaluation of the tubulin-bound paclitaxel conformation: synthesis, biology, and SAR studies of C-4 to C-3' bridged paclitaxel analogues.

  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.J Med Chem. 2007 Feb 22;50(4):713-25. doi: 10.1021/jm061071x. Epub 2007 Jan 31.PMID: 17263521 

2006

• Antitumor effect of 2-methoxyestradiol in a rat orthotopic brain tumor model.

  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.Cancer Res. 2006 Dec 15;66(24):11991-7. doi: 10.1158/0008-5472.CAN-06-1320.PMID: 17178898 

• Farnesyltransferase inhibitors reverse taxane resistance.

  Marcus AI, O'Brate AM, Buey RM, Zhou J, Thomas S, Khuri FR, Andreu JM, Díaz F, Giannakakou P.Cancer Res. 2006 Sep 1;66(17):8838-46. doi: 10.1158/0008-5472.CAN-06-0699.PMID: 16951201 

• Automatic microtubule tracking for QD-based in vivo cell imaging and drug efficacy study.

  Kong KY, Marcus AI, Hong JY, Giannakakou P, Wang MD.Conf Proc IEEE Eng Med Biol Soc. 2006;2006:3321-4. doi: 10.1109/IEMBS.2006.259750.PMID: 17947021

• Molecular design and chemical synthesis of a highly potent epothilone.

  Nicolaou KC, Pratt BA, Arseniyadis S, Wartmann M, O'Brate A, Giannakakou P.ChemMedChem. 2006 Jan;1(1):41-4. doi: 10.1002/cmdc.200500056.PMID: 16892332

2005

• Microtubule interactions with chemically diverse stabilizing agents: thermodynamics of binding to the paclitaxel site predicts cytotoxicity.Buey RM, Barasoain I, Jackson E, Meyer A, Giannakakou P, Paterson I, Mooberry S, Andreu JM, Díaz JF.Chem Biol. 2005 Dec;12(12):1269-79. doi: 10.1016/j.chembiol.2005.09.010.

  PMID: 16356844 

•  Resistance to microtubule-stabilizing drugs involves two events: beta-tubulin mutation in one allele followed by loss of the second allele.

  Wang Y, O'Brate A, Zhou W, Giannakakou P.Cell Cycle. 2005 Dec;4(12):1847-53. doi: 10.4161/cc.4.12.2264. Epub 2005 Dec 18.PMID: 16294009 

• Discovery of a biologically active thiostrepton fragment.

  Nicolaou KC, Zak M, Rahimipour S, Estrada AA, Lee SH, O'Brate A, Giannakakou P, Ghadiri MR.J Am Chem Soc. 2005 Nov 2;127(43):15042-4. doi: 10.1021/ja0552803.PMID: 16248640

• beta-Tubulin mutations are associated with resistance to 2-methoxyestradiol in MDA-MB-435 cancer cells.

  Gökmen-Polar Y, Escuin D, Walls CD, Soule SE, Wang Y, Sanders KL, Lavallee TM, Wang M, Guenther BD, Giannakakou P, Sledge GW Jr.Cancer Res. 2005 Oct 15;65(20):9406-14. doi: 10.1158/0008-5472.CAN-05-0088.PMID: 16230404 

• Both microtubule-stabilizing and microtubule-destabilizing drugs inhibit hypoxia-inducible factor-1alpha accumulation and activity by disrupting microtubule function.

  Escuin D, Kline ER, Giannakakou P.Cancer Res. 2005 Oct 1;65(19):9021-8. doi: 10.1158/0008-5472.CAN-04-4095.PMID: 16204076

• Cyclostreptin (FR182877), an antitumor tubulin-polymerizing agent deficient in enhancing tubulin assembly despite its high affinity for the taxoid site.

  Edler MC, Buey RM, Gussio R, Marcus AI, Vanderwal CD, Sorensen EJ, Díaz JF, Giannakakou P, Hamel E.Biochemistry. 2005 Aug 30;44(34):11525-38. doi: 10.1021/bi050660m.PMID: 16114889

• Accumulation of hypoxia-inducible factor-1alpha is limited by transcription-dependent depletion.

  Demidenko ZN, Rapisarda A, Garayoa M, Giannakakou P, Melillo G, Blagosklonny MV.Oncogene. 2005 Jul 14;24(30):4829-38. doi: 10.1038/sj.onc.1208636.PMID: 15897903

• The synergistic combination of the farnesyl transferase inhibitor lonafarnib and paclitaxel enhances tubulin acetylation and requires a functional tubulin deacetylase.

  Marcus AI, Zhou J, O'Brate A, Hamel E, Wong J, Nivens M, El-Naggar A, Yao TP, Khuri FR, Giannakakou P.Cancer Res. 2005 May 1;65(9):3883-93. doi: 10.1158/0008-5472.CAN-04-3757.PMID: 15867388

• Identification of a novel small-molecule inhibitor of the hypoxia-inducible factor 1 pathway.Tan C, de Noronha RG, Roecker AJ, Pyrzynska B, Khwaja F, Zhang Z, Zhang H, Teng Q, Nicholson AC, Giannakakou P, Zhou W, Olson JJ, Pereira MM, Nicolaou KC, Van Meir EG.Cancer Res. 2005 Jan 15;65(2):605-12.PMID: 15695405 

• Mitotic kinesin inhibitors induce mitotic arrest and cell death in Taxol-resistant and -sensitive cancer cells.

  Marcus AI, Peters U, Thomas SL, Garrett S, Zelnak A, Kapoor TM, Giannakakou P.J Biol Chem. 2005 Mar 25;280(12):11569-77. doi: 10.1074/jbc.M413471200. Epub 2005 Jan 13.PMID: 15653676

• Computer assisted analysis of microtubule dynamics in living cells.

  Yin Kong K, Marcus A, Young Hong J, Giannakakou P, Wang M.Conf Proc IEEE Eng Med Biol Soc. 2005;2005:3982-5. doi: 10.1109/IEMBS.2005.1615334.PMID: 17281104

• Targeting microtubules for cancer chemotherapy.

  Zhou J, Giannakakou P.Curr Med Chem Anticancer Agents. 2005 Jan;5(1):65-71. doi: 10.2174/1568011053352569.PMID: 15720262 

2004

• Survivin deregulation in beta-tubulin mutant ovarian cancer cells underlies their compromised mitotic response to taxol.

  Zhou J, O'brate A, Zelnak A, Giannakakou P.Cancer Res. 2004 Dec 1;64(23):8708-14. doi: 10.1158/0008-5472.CAN-04-2538.PMID: 15574781

• Chemistry and biology of diazonamide A: second total synthesis and biological investigations.

  Nicolaou KC, Hao J, Reddy MV, Rao PB, Rassias G, Snyder SA, Huang X, Chen DY, Brenzovich WE, Giuseppone N, O'Brate A, Giannakakou P.J Am Chem Soc. 2004 Oct 13;126(40):12897-906. doi: 10.1021/ja040093a.PMID: 15469287

• Chemistry and biology of diazonamide A: second total synthesis and biological investigations.

  Nicolaou KC, Hao J, Reddy MV, Rao PB, Rassias G, Snyder SA, Huang X, Chen DY, Brenzovich WE, Giuseppone N, O'Brate A, Giannakakou P.J Am Chem Soc. 2004 Oct 13;126(40):12897-906. doi: 10.1021/ja040093a.PMID: 15469287

• Exploitation of the HIF axis for cancer therapy.

  Escuin D, Simons JW, Giannakakou P.Cancer Biol Ther. 2004 Jul;3(7):608-11. doi: 10.4161/cbt.3.7.954. Epub 2004 Jul 29.PMID: 15197342

• Interaction of epothilone analogs with the paclitaxel binding site: relationship between binding affinity, microtubule stabilization, and cytotoxicity.

  Buey RM, Díaz JF, Andreu JM, O'Brate A, Giannakakou P, Nicolaou KC, Sasmal PK, Ritzén A, Namoto K.Chem Biol. 2004 Feb;11(2):225-36. doi: 10.1016/j.chembiol.2004.01.014.PMID: 15123284

2003

• Total synthesis of apoptolidin: completion of the synthesis and analogue synthesis and evaluation.

  Nicolaou KC, Li Y, Sugita K, Monenschein H, Guntupalli P, Mitchell HJ, Fylaktakidou KC, Vourloumis D, Giannakakou P, O'Brate A.J Am Chem Soc. 2003 Dec 17;125(50):15443-54. doi: 10.1021/ja030496v.PMID: 14664590

• Total synthesis and biological evaluation of (-)apicularen A and analogues thereof.

  Nicolaou KC, Kim DW, Baati R, O'Brate A, Giannakakou P.Chemistry. 2003 Dec 15;9(24):6177-91. doi: 10.1002/chem.200305230.PMID: 14679529

• The importance of p53 location: nuclear or cytoplasmic zip code?

  O'Brate A, Giannakakou P.Drug Resist Updat. 2003 Dec;6(6):313-22. doi: 10.1016/j.drup.2003.10.004.PMID: 14744495 

• Design, synthesis, and biological properties of highly potent epothilone B analogues.

  Nicolaou KC, Sasmal PK, Rassias G, Reddy MV, Altmann KH, Wartmann M, O'Brate A, Giannakakou P.Angew Chem Int Ed Engl. 2003 Aug 4;42(30):3515-20. doi: 10.1002/anie.200351819.PMID: 12900969 

• 2ME2 inhibits tumor growth and angiogenesis by disrupting microtubules and dysregulating HIF.

  Mabjeesh NJ, Escuin D, LaVallee TM, Pribluda VS, Swartz GM, Johnson MS, Willard MT, Zhong H, Simons JW, Giannakakou P.Cancer Cell. 2003 Apr;3(4):363-75. doi: 10.1016/s1535-6108(03)00077-1.PMID: 12726862

2002

• Paclitaxel-resistant human ovarian cancer cells undergo c-Jun NH2-terminal kinase-mediated apoptosis in response to noscapine.

  Zhou J, Gupta K, Yao J, Ye K, Panda D, Giannakakou P, Joshi HC.J Biol Chem. 2002 Oct 18;277(42):39777-85. doi: 10.1074/jbc.M203927200. Epub 2002 Aug 14.PMID: 12183452

• Enhanced microtubule-dependent trafficking and p53 nuclear accumulation by suppression of microtubule dynamics.

  Giannakakou P, Nakano M, Nicolaou KC, O'Brate A, Yu J, Blagosklonny MV, Greber UF, Fojo T.Proc Natl Acad Sci U S A. 2002 Aug 6;99(16):10855-60. doi: 10.1073/pnas.132275599. Epub 2002 Jul 26.PMID: 12145320 

• 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.

  Pryor DE, O'Brate A, Bilcer G, Díaz JF, Wang Y, Wang Y, Kabaki M, Jung MK, Andreu JM, Ghosh AK,Giannakakou P, Hamel E.Biochemistry. 2002 Jul 23;41(29):9109-15. doi: 10.1021/bi020211b.PMID: 12119025

2001

• Accompanying protein alterations in malignant cells with a microtubule-polymerizing drug-resistance phenotype and a primary resistance mechanism.

  Poruchynsky MS, Giannakakou P, Ward Y, Bulinski JC, Telford WG, Robey RW, Fojo T.Biochem Pharmacol. 2001 Dec 1;62(11):1469-80. doi: 10.1016/s0006-2952(01)00804-8.PMID: 11728383

• Chemical synthesis and biological evaluation of cis- and trans-12,13-cyclopropyl and 12,13-cyclobutyl epothilones and related pyridine side chain analogues.

  Nicolaou KC, Namoto K, Ritzén A, Ulven T, Shoji M, Li J, D'Amico G, Liotta D, French CT, Wartmann M, Altmann KH, Giannakakou P.J Am Chem Soc. 2001 Sep 26;123(38):9313-23. doi: 10.1021/ja011338b.PMID: 11562214

• 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.

  Nicoletti MI, Valoti G, Giannakakou P, Zhan Z, Kim JH, Lucchini V, Landoni F, Mayo JG, Giavazzi R, Fojo T.Clin Cancer Res. 2001 Sep;7(9):2912-22.PMID: 11555610

• Low concentrations of paclitaxel induce cell type-dependent p53, p21 and G1/G2 arrest instead of mitotic arrest: molecular determinants of paclitaxel-induced cytotoxicity.

  Giannakakou P, Robey R, Fojo T, Blagosklonny MV.Oncogene. 2001 Jun 28;20(29):3806-13. doi: 10.1038/sj.onc.1204487.PMID: 11439344

• Inhibition of HIF-1- and wild-type p53-stimulated transcription by codon Arg175 p53 mutants with selective loss of functions.

  Blagosklonny MV, Giannakakou P, Romanova LY, Ryan KM, Vousden KH, Fojo T.Carcinogenesis. 2001 Jun;22(6):861-7. doi: 10.1093/carcin/22.6.861.PMID: 11375890

• Synthesis and biological evaluation of 12,13-cyclopropyl and 12,13-cyclobutyl epothilones.

  Nicolaou KC, Namoto K, Li J, Ritzén A, Ulven T, Shoji M, Zaharevitz D, Gussio R, Sackett DL, Ward RD, Hensler A, Fojo T, Giannakakou P.Chembiochem. 2001 Jan 8;2(1):69-75. doi: 10.1002/1439-7633(20010105)2:1<69::AID-CBIC69>3.0.CO;2-8.PMID: 11828429 

2000

• p53 is associated with cellular microtubules and is transported to the nucleus by dynein.

  Giannakakou P, Sackett DL, Ward Y, Webster KR, Blagosklonny MV, Fojo T.Nat Cell Biol. 2000 Oct;2(10):709-17. doi: 10.1038/35036335.PMID: 11025661

• Reply.Gussio R, Fojo T, Giannakakou P.Trends Pharmacol Sci. 2000 Sep;21(9):323-4. doi: 10.1016/s0165-6147(00)01522-4.PMID: 10973075 

•  Chemical synthesis and biological properties of pyridine epothilones.Nicolaou KC, Scarpelli R, Bollbuck B, Werschkun B, Pereira MM, Wartmann M, Altmann KH, Zaharevitz D, Gussio R, Giannakakou P.Chem Biol. 2000 Aug;7(8):593-9. doi: 10.1016/s1074-5521(00)00006-5.PMID: 11048950

• Paclitaxel selects for mutant or pseudo-null p53 in drug resistance associated with tubulin mutations in human cancer.

  Giannakakou P, Poy G, Zhan Z, Knutsen T, Blagosklonny MV, Fojo T.Oncogene. 2000 Jun 22;19(27):3078-85. doi: 10.1038/sj.onc.1203642.PMID: 10871860

• Discodermolide: just another microtubule-stabilizing agent? No! A lesson in synergy.

  Giannakakou P, Fojo T.Clin Cancer Res. 2000 May;6(5):1613-5.PMID: 10815877 

• A common pharmacophore for epothilone and taxanes: molecular basis for drug resistance conferred by tubulin mutations in human cancer cells.

  Giannakakou P, Gussio R, Nogales E, Downing KH, Zaharevitz D, Bollbuck B, Poy G, Sackett D, Nicolaou KC, Fojo T.Proc Natl Acad Sci U S A. 2000 Mar 14;97(6):2904-9. doi: 10.1073/pnas.040546297.PMID: 10688884 

• Tubulin/microtubules: still a promising target for new chemotherapeutic agents.

  Giannakakou P, Sackett D, Fojo T.J Natl Cancer Inst. 2000 Feb 2;92(3):182-3. doi: 10.1093/jnci/92.3.182.PMID: 10655426 

1999

• Regulation of apoptosis in myeloid cells by interferon consensus sequence-binding protein.

  Gabriele L, Phung J, Fukumoto J, Segal D, Wang IM, Giannakakou P, Giese NA, Ozato K, Morse HC 3rd.J Exp Med. 1999 Aug 2;190(3):411-21. doi: 10.1084/jem.190.3.411.PMID: 10430629

1998

• Synthesis and biological evaluation of 2-acyl analogues of paclitaxel (Taxol).

  Kingston DG, Chaudhary AG, Chordia MD, Gharpure M, Gunatilaka AA, Higgs PI, Rimoldi JM, Samala L, Jagtap PG, Giannakakou P, Jiang YQ, Lin CM, Hamel E, Long BH, Fairchild CR, Johnston KA.J Med Chem. 1998 Sep 10;41(19):3715-26. doi: 10.1021/jm980229d.PMID: 9733497

• Effects of p53-expressing adenovirus on the chemosensitivity and differentiation of anaplastic thyroid cancer cells.

  Blagosklonny MV, Giannakakou P, Wojtowicz M, Romanova LY, Ain KB, Bates SE, Fojo T.J Clin Endocrinol Metab. 1998 Jul;83(7):2516-22. doi: 10.1210/jcem.83.7.4984.PMID: 9661637

• Microtubule-interfering agents activate c-Jun N-terminal kinase/stress-activated protein kinase through both Ras and apoptosis signal-regulating kinase pathways.

  Wang TH, Wang HS, Ichijo H, Giannakakou P, Foster JS, Fojo T, Wimalasena J.J Biol Chem. 1998 Feb 27;273(9):4928-36. doi: 10.1074/jbc.273.9.4928.PMID: 9478937

• Combinations of paclitaxel and vinblastine and their effects on tubulin polymerization and cellular cytotoxicity: characterization of a synergistic schedule.

  Giannakakou P, Villalba L, Li H, Poruchynsky M, Fojo T.Int J Cancer. 1998 Jan 5;75(1):57-63. doi: 10.1002/(sici)1097-0215(19980105)75:1<57::aid-ijc10>3.0.co;2-a.PMID: 9426691

1997

• 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.

  Kowalski RJ, Giannakakou P, Gunasekera SP, Longley RE, Day BW, Hamel E.Mol Pharmacol. 1997 Oct;52(4):613-22.PMID: 9380024

• Paclitaxel-resistant human ovarian cancer cells have mutant beta-tubulins that exhibit impaired paclitaxel-driven polymerization.

  Giannakakou P, Sackett DL, Kang YK, Zhan Z, Buters JT, Fojo T, Poruchynsky MS.J Biol Chem. 1997 Jul 4;272(27):17118-25. doi: 10.1074/jbc.272.27.17118.PMID: 9202030

• Synthesis of epothilones A and B in solid and solution phase.

  Nicolaou KC, Winssinger N, Pastor J, Ninkovic S, Sarabia F, He Y, Vourloumis D, Yang Z, Li T,Giannakakou P, Hamel E.Nature. 1997 May 15;387(6630):268-72. doi: 10.1038/387268a0.PMID: 9153390

• Activities of the microtubule-stabilizing agents epothilones A and B with purified tubulin and in cells resistant to paclitaxel (Taxol(R)).

  Kowalski RJ, Giannakakou P, Hamel E.J Biol Chem. 1997 Jan 24;272(4):2534-41. doi: 10.1074/jbc.272.4.2534.PMID: 8999970

• Tubulin from paclitaxel-resistant cells as a probe for novel antimicrotubule agents.

  Sackett DL, Giannakakou P, Poruchynsky M, Fojo A.Cancer Chemother Pharmacol. 1997;40(3):228-32. doi: 10.1007/s002800050651.PMID: 9219506

• Raf-1/bcl-2 phosphorylation: a step from microtubule damage to cell death.

  Blagosklonny MV, Giannakakou P, el-Deiry WS, Kingston DG, Higgs PI, Neckers L, Fojo T.Cancer Res. 1997 Jan 1;57(1):130-5.PMID: 8988053

1996

• Effect of calcium channel blockers on the action of various antitumour agents in the yeast Saccharomyces cerevisiae.

  Tillgada E, Giannakakou P, Karavokyros I, Delitheos A.J Appl Bacteriol. 1996 Nov;81(5):481-5. doi: 10.1111/j.1365-2672.1996.tb03536.x.PMID: 8939026

• Brain-derived neurotrophic factor protects neuroblastoma cells from vinblastine toxicity.

  Scala S, Wosikowski K, Giannakakou P, Valle P, Biedler JL, Spengler BA, Lucarelli E, Bates SE, Thiele CJ.Cancer Res. 1996 Aug 15;56(16):3737-42.PMID: 8706017