Arrowhead Publications

June, 2012

Kim DH, Sartor MA, Bain JR, Sandoval D, Stevens RD, Medvedovic M, Newgard CB, Woods SC, Seeley RJ., Rapid and weight-independent improvement of glucose tolerance induced by a Peptide designed to elicit apoptosis in adipose tissue endothelium. Diabetes. 2012 Sep;61(9):2299-310. Epub 2012 Jun 25.

January, 2012

Seeley, R.J. "Treating Obesity Like a Tumor" Cell Metabolism (2012) 15: 1-2

January, 2011

Barnhart KF, Christianson DR, Hanley PW, Driessen WH, Bernacky BJ, Baze WB, Wen S, Tian M, Ma J, Kolonin MG, Saha PK, Do KA, Hulvat JF, Gelovani JG, Chan L, Arap W, Pasqualini R. "A peptidomimetic targeting white fat causes weight loss and improved insulin resistance in obese monkeys." Sci .Transl. Med. (2011) 3(108), 108ra112.
Read: http://stm.sciencemag.org/content/3/108/108ra112.short

Staquicini FI, Cardó-Vila M, Kolonin MG, Trepel M, Edwards JK, Nunes DN, Sergeeva A, Efstathiou E, Sun J, Almeida NF, Tu SM, Botz GH, Wallace MJ, O'Connell DJ, Krajewski S, Gershenwald JE, Molldrem JJ, Flamm AL, Koivunen E,Pentz RD, Dias-Neto E, Setubal JC, Cahill DJ, Troncoso P, Do KA, Logothetis CJ,Sidman RL, Pasqualini R, Arap W. "Vascular ligand-receptor mapping by direct combinatorial selection in cancer patients." Proc. Natl. Acad. Sci. U.S.A. (2011) 108(46), 18637-42
http://www.ncbi.nlm.nih.gov/pmc/articles/PMC3219136/?tool=pubmed

January, 2010

Kim DH, Woods SC, Seeley RJ. "Peptide designed to elicit apoptosis in adipose tissue endothelium reduces food intake and body weight." Diabetes (2010) 59(4), 907-15.
http://diabetes.diabetesjournals.org/content/59/4/907.long

Giordano RJ, Cardó-Vila M, Salameh A, Anobom CD, Zeitlin BD, Hawke DH, Valente AP, Almeida FC, Nör JE, Sidman RL, Pasqualini R, Arap W. "From combinatorial peptide selection to drug prototype (I): targeting the vascular endothelial growth factor receptor pathway." Proc. Natl. Acad. Sci. U.S.A. (2010) 107(11), 5112-7.
http://www.ncbi.nlm.nih.gov/pmc/articles/PMC2841949/?tool=pmcentrez

January, 2009

Zhang Y, Daquinag A, Traktuev DO, Amaya-Manzanares F, Simmons PJ, March KL, Pasqualini R, Arap W, Kolonin MG. "White adipose tissue cells are recruited by experimental tumors and promote cancer {rogression in mouse models." Cancer Res. (2009) 69(12), 5259-66.
http://cancerres.aacrjournals.org/content/69/12/5259.long

Dias-Neto E, Nunes DN, Giordano RJ, Sun J, Botz GH, Yang K, Setubal JC, Pasqualini R, Arap W. "Next-Generation Phage Display: Integrating and Comparing Available Molecular Tools to Enable Cost-Effective High-Throughput Analysis." PLoS ONE (2009) 4(12): e8338. doi:10.1371/journal.pone.0008338
http://www.plosone.org/article/info%3Adoi%2F10.1371%2Fjournal.pone.0008338

Lewis VO, Ozawa MG, Deavers MT, Wang G, Shintani T, Arap W, Pasqualini R. "The interleukin-11 receptor alpha as a candidate ligand-directed target in osteosarcoma: consistent data from cell lines, orthotopic models, and human tumor samples." Cancer Res. (2009) 69(5), 1995-9.
http://cancerres.aacrjournals.org/content/69/5/1995.long

January, 2006

Kolonin MG, Bover L, Sun J, Zurita AJ, Do KA, Lahdenranta J, Cardó-Vila M, Giordano RJ, Jaalouk DE, Ozawa MG, Moya CA, Souza GR, Staquicini FI, Kunyiasu A, Scudiero DA, Holbeck SL, Sausville EA, Arap W, Pasqualini R. "Ligand-directed surface profiling of human cancer cells with combinatorial peptide libraries." Cancer Res. (2006), 66(1), 34-40.
http://cancerres.aacrjournals.org/content/66/1/34.long

January, 2004

Kolonin MG, Saha PK, Chan L, Pasqualini R, Arap W. "Reversal of obesity by targeted ablation of adipose tissue." Nat Med. (2004) 10(6),625-32.
http://www.nature.com/nm/journal/v10/n6/full/nm1048.html

Arap MA, Lahdenranta J, Mintz PJ, Hajitou A, Sarkis AS, Arap W, Pasqualini R. "Cell surface expression of the stress response chaperone GRP78 enables tumor targeting by circulating ligands." Cancer Cell. (2004) 6(3), 275-84.
http://www.cell.com/cancer-cell/retrieve/pii/S1535610804002405

Zurita AJ, Troncoso P, Cardó-Vila M, Logothetis CJ, Pasqualini R, Arap W. "Combinatorial screenings in patients: the interleukin-11 receptor alpha as a candidate target in the progression of human prostate cancer." Cancer Res. (2004) 64(2), 435-9.
http://cancerres.aacrjournals.org/content/64/2/435.long

January, 2002

Arap W, Kolonin MG, Trepel M, Lahdenranta J, Cardó-Vila M, Giordano RJ, Mintz PJ, Ardelt PU, Yao VJ, Vidal CI, Chen L, Flamm A, Valtanen H, Weavind LM, Hicks ME, Pollock RE, Botz GH, Bucana CD, Koivunen E, Cahill D, Troncoso P, Baggerly KA, Pentz RD, Do KA, Logothetis CJ, Pasqualini R. "Steps toward mapping the human vasculature by phage display." Nat Med. (2002) 8(2), 121-7.
http://www.nature.com/nm/journal/v8/n2/full/nm0202-121.html

January, 1999

Ellerby HM, Arap W, Ellerby LM, Kain R, Andrusiak R, Rio GD, Krajewski S, Lombardo CR, Rao R, Ruoslahti E, Bredesen DE, Pasqualini R. "Anti-cancer activity of targeted pro-apoptotic peptides." Nat Med. (1999) 5(9), 1032-8.
http://www.nature.com/nm/journal/v5/n9/full/nm0999_1032.html

January, 1998

Arap W, Pasqualini R, Ruoslahti E. "Cancer treatment by targeted drug delivery to tumor vasculature in a mouse model." Science (1998) 279(5349), 377-80.
http://www.sciencemag.org/content/279/5349/377.abstract

RNAi Literature

February, 2013

Christine I Wooddell, David B Rozema, Markus Hossbach, Matthias John, Holly L Hamilton, Qili Chu, Julia O Hegge, Jason J Klein, Darren H Wakefield, Claudia E Oropeza, Jochen Deckert, Ingo Roehl, Kerstin Jahn-Hofmann, Philipp Hadwiger, Hans-Peter Vornlocher, Alan McLachlan and David L Lewis, "Hepatocyte-targeted RNAi Therapeutics for the Treatment of Chronic Hepatitis B Virus Infection." Molecular Therapy. advance online publication 26 February 2013; doi: 10.1038/mt.2013.31.

September, 2012

Britta Schneider, Michael Grote, Matthias John, Alexander Haas, Birgit Bramlage, Ludger M lckenstein, Kerstin Jahn-Hofmann, Frieder Bauss, Weijun Cheng, Rebecca Croasdale, Karin Daub, Simone Dill, Eike Hoffmann, Wilma Lau, Helmut Burtscher, James L Ludtke, Silke Metz, Olaf Mundigl, Zane C Neal, Werner Scheuer, Jan Stracke, Hans Herweijerand Ulrjch Brinkmann, "Targeted siRNA Delivery and mRNA Knockdown Mediated by Bispecific Digoxigenin-binding Antibodies." Molecular Therapy Nucleic Acids (2012) 1, e46; doi:10.1038/mtna.2012.39, Published online 18 September 2012.

May, 2012

Mohammad Aminur Rahman, A.R.M. Ruhul Amin, Xu Wang, Jonathan E. Zuckerman, Chung Hang J. Choi, Bingsen Zhou, Dongsheng Wang, Sreenivas Nannapaneni, Lydia Koenig, Zhengjia Chen, Zhuo (Georgia) Chen, Yun Yen, Mark E. Davis, Dong M. Shin, Systemic delivery of siRNA nanoparticles targeting RRM2 suppresses head and neck tumor growth, Journal of Controlled Release, Volume 159, Issue 3, 10 May 2012, Pages 384-392, ISSN 0168-3659, 10.1016/j.jconrel.2012.01.045.

February, 2012

Heidel, J. D. and T. Schluep. "Cyclodextrin-containing polymers: versatile platforms of drug delivery materials."  J Drug Deliv. 2012: 262731. Epub 262012 Feb 2, 2012.

January, 2012

So C. Wong, Jason J. Klein, Holly L. Hamilton, Qili Chu, Christina L. Frey, Vladimir S. Trubetskoy, Julia Hegge, Darren Wakefield, David B. Rozema, and David L. Lewis, "Co-Injection of a Targeted, Reversibly Masked Endosomolytic Polymer Dramatically Improves the Efficacy of Cholesterol-Conjugated Small Interfering RNAs In Vivo."  Nucleic Acid Therapeutics. December 2012, 22(6): 380-390. doi:10.1089/nat.2012.0389.   

June, 2010

J Heidel, J. D. and M. E. Davis (2010). "Clinical Developments in Nanotechnology for Cancer Therapy." Pharm Res: 12 June.

January, 2010

Davis, M. E., J. E. Zuckerman, C. H. Choi, D. Seligson, A. Tolcher, C. A. Alabi, Y. Yen, J. D. Heidel and A. Ribas (2010). "Evidence of RNAi in humans from systemically administered siRNA via targeted nanoparticles." Nature 464: 1067-70.

Ribas, A., L. Kalinoski, J. D. Heidel, J. Peterkin, D. B. Seligson, J. E. Zuckerman, C. Choi, Y. Yen, M. E. Davis and A. W. Tolcher (2010). "Systemic delivery of siRNA via targeted nanoparticles in patients with cancer: Results from a first-in-class phase I clinical trial." J Clin Oncol 28(15s): abstr 3022

January, 2009

Oney, S., R. T. Lam, K. M. Bompiani, C. M. Blake, G. Quick, J. D. Heidel, J. Y. Liu, B. C. Mack, M. E. Davis, K. W. Leong and B. A. Sullenger (2009). "Development of universal antidotes to control aptamer activity." Nat Med. 15(10): 1224-8.

Davis, M. E. (2009). "The first targeted delivery of siRNA in humans via a self-assembling, cyclodextrin polymer-based nanoparticle: from concept to clinic." Mol Pharm. 6(3): 659-68.

Brahmamdam, P., E. Watanabe, J. Unsinger, K. C. Chang, W. Schierding, A. S. Hoekzema, T. T. Zhou, J. S. McDonough, H. Holemon, J. D. Heidel, C. M. Coopersmith, J. E. McDunn and R. S. Hotchkiss (2009). "Targeted delivery of siRNA to cell death proteins in sepsis." Shock. 32(2): 131-9.

Alizadeh, D., L. Zhang, J. Hwang, T. Schluep and B. Badie (2009). "Tumor-Associated Macrophages Are Predominant Carriers of Cyclodextrin-Based Nanoparticles into Gliomas." Nanomedicine 14: 14.

Schluep, T., J. Hwang, I. J. Hildebrandt, J. Czernin, C. H. J. Choi, C. A. Alabi, B. C. Mack and M. E. Davis (2009). "Pharmacokinetics and tumor dynamics of the nanoparticle IT-101 from PET imaging and tumor histological measurements."
Proc Natl Acad Sci U S A 106(27): 11394-9.

Schluep, T., P. Gunawan, L. Ma, G. S. Jensen, J. Duringer, S. Hinton, W. Richter and J. Hwang (2009). "Polymeric Tubulysin-Peptide Nanoparticles with Potent Antitumor Activity." Clin Cancer Res 15(1): 181-189.

January, 2008

Bartlett DW, Davis ME (2008). “Impact of tumor-specific targeting and dosing schedule on tumor growth inhibition after intravenous administration of siRNA-containing nanoparticles.” Biotechnology & Bioengineering 99(4):975-85.

Oliver, C. J., Y. Yen, T. Synold, T. Schluep and M. E. Davis (2008). "A dose-finding pharmacokinetic study of IT-101, the first de novo designed nanoparticle therapeutic, in refractory solid tumors." J Clin Oncol (Meeting Abstracts) 26 (May 20 suppl): 14538.

Jensen, G., J. Hwang and T. Schluep (2008). "Antitumor activity of IT-101, a cyclodextrin-containing polymer-camptothecin nanoparticle, in combination with various anticancer agents in human ovarian cancer xenografts." Proceedings of the 99th Annual Meeting of the American Association for Cancer Research: 767.

Hwang J, Rodgers K, Oliver CJ, Schluep T. (2008) "α-Methylprednisolone conjugated cyclodextrin polymer-based nanoparticles for rheumatoid arthritis therapy." Int J Nanomedicine 3:359-71.

January, 2007

Rozema DB, Lewis DL, Wakefield DH, Wong SC, Klein JJ, Roesch PL, Bertin SL, Reppen TW, Chu Q, Blokhin AV, Hagstrom JE, Wolff JA (2007). “Dynamic PolyConjugates for targeted in vivo delivery of siRNA to hepatocytes.” Proceedings of the National Academy of Sciences 104(32): 12982-87.

Bartlett DW, Su H, Hildebrandt IJ, Weber WA, and Davis ME (2007). “Impact of tumor-specific targeting on the biodistribution and efficacy of siRNA nanoparticles measured by multimodality in vivo imaging.” Proceedings of the National Academy of Sciences 104(39):15549-54.

Mullin R (2007). “Delivering RNA: Case Study #2: Two firms partner to make the active ingredient and a delivery component of a cancer therapy.” Chemical & Engineering News 85(14):22-3.

Heidel JD, Yu Z, Liu JY-C, Rele SM, Liang Y, Zeidan RK, Kornbrust DJ, and Davis ME (2007). “Administration in non-human primates of escalating intravenous doses of targeted nanoparticles containing RRM2 siRNA.” Proceedings of the National Academy of Sciences 104(14):5715-21.

Heidel JD, Liu JY-C, Yen Y, Zhou B, Heale BSE, Rossi JJ, Bartlett DW, and Davis ME (2007). “Potent siRNA inhibitors of ribonucleotide reductase subunit RRM2 reduce cell proliferation in vitro and in vivo.” Clinical Cancer Research 13(7):2207-15. Bartlett DW and Davis ME (2007). Physicochemical and biological characterization of targeted, nucleic acid-containing nanoparticles. Bioconjugate Chemistry 18(2):456-68.

Bartlett DW and Davis ME (2007). “Effect of siRNA nuclease stability on the in vitro and in vivo kinetics of siRNA-mediated gene silencing.” Biotechnology and Bioengineering 97(4):909-21.

January, 2006

Heidel JD (2006). “Linear cyclodextrin-containing polymers and their use as delivery agents.” Expert Opinion on Drug Delivery 3(5):641-6.

Mishra S, Heidel JD, Webster P, and Davis ME (2006). “Imidazole groups on a linear, cyclodextrin-containing polycation produce enhanced gene delivery via multiple processes.” Journal of Controlled Release 116:179-91

Bartlett DW and Davis ME (2006). “Insights into the kinetics of siRNA-mediated gene silencing from live-cell and live-animal bioluminescent imaging.” Nucleic Acids Research 34(1):322-33.

Zeidan, R. K., S. A. Kalovidouris, T. Schluep, R. Fazio, R. Andresini and M. E. Davis (2006). "A Solvent-Free Method for Isotopically or Radioactively Labeling Cyclodextrins and Cyclodextrin-Containing Polymers." Bioconjug Chem. 17(6): 1624-1626.

Schluep, T., J. Cheng, K. T. Khin and M. E. Davis (2006). "Pharmacokinetics and biodistribution of the camptothecin-polymer conjugate IT-101 in rats and tumor-bearing mice." Cancer Chemother Pharmacol. 57(5): 654-62. Epub 2005 Aug 26.

Schluep, T., J. Hwang, J. Cheng, J. D. Heidel, D. W. Bartlett, B. Hollister and M. E. Davis (2006). "Preclinical Efficacy of the Camptothecin-Polymer Conjugate IT-101 in Multiple Cancer Models." Clin Cancer Res 12(5): 1606-1614.

January, 2005

Hu-Lieskovan S, Heidel JD, Bartlett DW, Davis ME, and Triche TJ (2005). “Sequence-specific knockdown of EWS-FLI1 by targeted, nonviral delivery of small interfering RNA inhibits tumor growth in a murine model of metastatic Ewing's Sarcoma.” Cancer Research 65(19):8984-92.

Rose SD, Kim D-H, Amarzguioui M, Heidel JD, Collingwood MA, Davis ME, Rossi JJ, and Behlke MA (2005). “Functional polarity is introduced by Dicer processing of short substrate RNAs.” Nucleic Acids Research 33:4140-56.

January, 2004

Heidel JD, Hu S, Liu XF, Triche TJ, and Davis ME (2004). “Lack of interferon response in animals to naked siRNAs.” Nature Biotechnology 22(12):1579-82.

Davis ME and Brewster ME (2004). “Cyclodextrin-based pharmaceutics: past, present and future.” Nature Reviews. Drug Discovery 3(12):1023-35.

Davis ME, Pun SH, Bellocq NC, Reineke TM, Popielarski SR, Mishra S, and Heidel JD (2004). “Self-assembling nucleic acid delivery vehicles via linear, water-soluble, cyclodextrin-containing polymers.” Current Medicinal Chemistry 11(2):179-97.

Cheng J, Khin KT, Davis ME (2004) “Antitumor Activity of b-Cyclodextrin Polymer-Campthothecin Conjugates.” Molecular Pharmaceutics 1: 183-193

Pun SH, Tack F, Bellocq NC, Cheng J, Grubbs BH, Jensen GS, Davis ME, Brewster M, Janicot M, Janssens B, Floren W, Bakker A (2004) “Targeted Delivery of RNA-Cleaving DNA Enzyme (DNAzyme) to Tumor Tissue by Transferrin-Modified, Cyclodextrin-Based Particles. “Cancer Biol Ther 3: 641-50.

Pun SH, Bellocq NC, Liu A, Jensen G, Machemer T, Quijano E, Schluep T, Wen S, Engler H, Heidel J, Davis ME (2004) “Cyclodextrin-modified polyethylenimine polymers for gene delivery.” Bioconjug Chem 15: 831-40.

Bellocq NC, Kang DW, Wang X, Jensen GS, Pun SH, Schluep T, Zepeda ML, Davis ME (2004) “Synthetic Biocompatible Cyclodextrin-Based Constructs for Local Gene Delivery to Improve Cutaneous Wound Healing.” Bioconjug Chem 15: 1201-1211.

January, 2003

Cheng J, Khin KT, Jensen GS, Liu A and Davis ME (2003) “Synthesis of linear, beta-cyclodextrin-based polymers and their camptothecin conjugates.” Bioconjug Chem 14(5): 1007-17.

Bellocq NC, Pun SH, Jensen GS, Davis ME (2003) “Transferrin-containing, cyclodextrin polymer-based particles for tumor-targeted gene delivery.” Bioconjug Chem 14: 1122-32.

Bellocq NC, Davis ME, Engler H, Jensen GS, Liu A, Machemer T, Maneval D, Quijano E, Hwang SJ, Schluep T, Wen SF (2003) “Transferrin-Targeted, Cyclodextrin Polycation-Based Gene Vector for Systemic Delivery.” Mol Ther 7: S290

January, 2002

Hwang Pun, S. and Davis, M.E. (2002) “Development of a Nonviral Gene Delivery Vehicle for Systemic Application.” Bioconjugate Chemistry 13: 630-639.

January, 2001

Davis, M.E. (2001) “Cyclodextrin-containing Polymers for Drug Delivery.” PharmaTech, 185.

Hwang, S.J., Bellocq, N.C., and Davis, M.E. (2001) “Effects of Structure of beta-cyclodextrin-containing Polymers on Gene Delivery.” Bioconjugate Chemistry 12(2): 280-290.

Hwang, S.J., and Davis, M.E. (2001) “Cationic Polymers for Gene Delivery: Designs for Overcoming Barriers to Systemic Administration.” Current Opinion in Molecular Therapeutics 3(2): 183-191.

January, 1999

Gonzalez, H., Hwang, S.J., and Davis, M.E. (1999) “New Class of Polymers for the Delivery of Macromolecular Therapeutics.” Bioconjugate Chemistry 10: 1068-1074.