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Design, synthesis, and immunologic evaluation of vaccine adjuvant conjugates based on QS-21 and tucaresol.

Fernández-Tejada A, Chea EK, George C, Gardner JR, Livingston PO, Ragupathi G, Tan DS, Gin DY.

Bioorg Med Chem. 2014 Nov 1;22(21):5917-23. doi: 10.1016/j.bmc.2014.09.016. Epub 2014 Sep 17.


Development of a minimal saponin vaccine adjuvant based on QS-21.

Fernández-Tejada A, Chea EK, George C, Pillarsetty N, Gardner JR, Livingston PO, Ragupathi G, Lewis JS, Tan DS, Gin DY.

Nat Chem. 2014 Jul;6(7):635-43. doi: 10.1038/nchem.1963. Epub 2014 Jun 1.


Applying PET to broaden the diagnostic utility of the clinically validated CA19.9 serum biomarker for oncology.

Viola-Villegas NT, Rice SL, Carlin S, Wu X, Evans MJ, Sevak KK, Drobjnak M, Ragupathi G, Sawada R, Scholz WW, Livingston PO, Lewis JS.

J Nucl Med. 2013 Nov;54(11):1876-82. doi: 10.2967/jnumed.113.119867. Epub 2013 Sep 12.


Accelerated tumor growth mediated by sublytic levels of antibody-induced complement activation is associated with activation of the PI3K/AKT survival pathway.

Wu X, Ragupathi G, Panageas K, Hong F, Livingston PO.

Clin Cancer Res. 2013 Sep 1;19(17):4728-39. doi: 10.1158/1078-0432.CCR-13-0088. Epub 2013 Jul 5.


Synthesis and preclinical evaluation of QS-21 variants leading to simplified vaccine adjuvants and mechanistic probes.

Chea EK, Fernández-Tejada A, Damani P, Adams MM, Gardner JR, Livingston PO, Ragupathi G, Gin DY.

J Am Chem Soc. 2012 Aug 15;134(32):13448-57. doi: 10.1021/ja305121q. Epub 2012 Aug 6.


Immunization with N-propionyl polysialic acid-KLH conjugate in patients with small cell lung cancer is safe and induces IgM antibodies reactive with SCLC cells and bactericidal against group B meningococci.

Krug LM, Ragupathi G, Hood C, George C, Hong F, Shen R, Abrey L, Jennings HJ, Kris MG, Livingston PO.

Cancer Immunol Immunother. 2012 Jan;61(1):9-18. doi: 10.1007/s00262-011-1083-6. Epub 2011 Aug 3.


Natural and synthetic saponin adjuvant QS-21 for vaccines against cancer.

Ragupathi G, Gardner JR, Livingston PO, Gin DY.

Expert Rev Vaccines. 2011 Apr;10(4):463-70. doi: 10.1586/erv.11.18. Review.


Human monoclonal antibodies to sialyl-Lewis (CA19.9) with potent CDC, ADCC, and antitumor activity.

Sawada R, Sun SM, Wu X, Hong F, Ragupathi G, Livingston PO, Scholz WW.

Clin Cancer Res. 2011 Mar 1;17(5):1024-32. doi: 10.1158/1078-0432.CCR-10-2640. Epub 2011 Feb 22.


Chemical and genetic assessment of variability in commercial Radix Astragali (Astragalus spp.) by ion trap LC-MS and nuclear ribosomal DNA barcoding sequence analyses.

Xiao WL, Motley TJ, Unachukwu UJ, Lau CB, Jiang B, Hong F, Leung PC, Wang QF, Livingston PO, Cassileth BR, Kennelly EJ.

J Agric Food Chem. 2011 Mar 9;59(5):1548-56. doi: 10.1021/jf1028174. Epub 2011 Feb 15.


Impact of minimal tumor burden on antibody response to vaccination.

Kim SK, Wu X, Ragupathi G, Gathuru J, Koide F, Cheung NK, Panageas K, Livingston PO.

Cancer Immunol Immunother. 2011 May;60(5):621-7. doi: 10.1007/s00262-011-0975-9. Epub 2011 Jan 26.


The known immunologically active components of Astragalus account for only a small proportion of the immunological adjuvant activity when combined with conjugate vaccines.

Hong F, Xiao W, Ragupathi G, Lau CB, Leung PC, Yeung KS, George C, Cassileth B, Kennelly E, Livingston PO.

Planta Med. 2011 May;77(8):817-24. doi: 10.1055/s-0030-1250574. Epub 2010 Dec 2.


A high-throughput O-glycopeptide discovery platform for seromic profiling.

Blixt O, Cló E, Nudelman AS, Sørensen KK, Clausen T, Wandall HH, Livingston PO, Clausen H, Jensen KJ.

J Proteome Res. 2010 Oct 1;9(10):5250-61. doi: 10.1021/pr1005229. Erratum in: J Proteome Res. 2011 Mar 4;10(3):1436.


Preclinical evaluation of the synthetic adjuvant SQS-21 and its constituent isomeric saponins.

Ragupathi G, Damani P, Deng K, Adams MM, Hang J, George C, Livingston PO, Gin DY.

Vaccine. 2010 Jun 11;28(26):4260-7. doi: 10.1016/j.vaccine.2010.04.034. Epub 2010 May 5.


Cancer biomarkers defined by autoantibody signatures to aberrant O-glycopeptide epitopes.

Wandall HH, Blixt O, Tarp MA, Pedersen JW, Bennett EP, Mandel U, Ragupathi G, Livingston PO, Hollingsworth MA, Taylor-Papadimitriou J, Burchell J, Clausen H.

Cancer Res. 2010 Feb 15;70(4):1306-13. doi: 10.1158/0008-5472.CAN-09-2893. Epub 2010 Feb 2.


Design and synthesis of potent Quillaja saponin vaccine adjuvants.

Adams MM, Damani P, Perl NR, Won A, Hong F, Livingston PO, Ragupathi G, Gin DY.

J Am Chem Soc. 2010 Feb 17;132(6):1939-45. doi: 10.1021/ja9082842.


From synthesis to biologics: preclinical data on a chemistry derived anticancer vaccine.

Zhu J, Wan Q, Lee D, Yang G, Spassova MK, Ouerfelli O, Ragupathi G, Damani P, Livingston PO, Danishefsky SJ.

J Am Chem Soc. 2009 Jul 8;131(26):9298-303. doi: 10.1021/ja901415s.


Biologics through chemistry: total synthesis of a proposed dual-acting vaccine targeting ovarian cancer by orchestration of oligosaccharide and polypeptide domains.

Zhu J, Wan Q, Ragupathi G, George CM, Livingston PO, Danishefsky SJ.

J Am Chem Soc. 2009 Mar 25;131(11):4151-8. doi: 10.1021/ja810147j.


Synthesis of sialyl Lewis(a) (sLe (a), CA19-9) and construction of an immunogenic sLe(a) vaccine.

Ragupathi G, Damani P, Srivastava G, Srivastava O, Sucheck SJ, Ichikawa Y, Livingston PO.

Cancer Immunol Immunother. 2009 Sep;58(9):1397-405. doi: 10.1007/s00262-008-0654-7. Epub 2009 Feb 4.


Phase I/II study of GM-CSF DNA as an adjuvant for a multipeptide cancer vaccine in patients with advanced melanoma.

Perales MA, Yuan J, Powel S, Gallardo HF, Rasalan TS, Gonzalez C, Manukian G, Wang J, Zhang Y, Chapman PB, Krown SE, Livingston PO, Ejadi S, Panageas KS, Engelhorn ME, Terzulli SL, Houghton AN, Wolchok JD.

Mol Ther. 2008 Dec;16(12):2022-9. doi: 10.1038/mt.2008.196. Epub 2008 Sep 16.


Synthesis of QS-21-xylose: establishment of the immunopotentiating activity of synthetic QS-21 adjuvant with a melanoma vaccine.

Deng K, Adams MM, Damani P, Livingston PO, Ragupathi G, Gin DY.

Angew Chem Int Ed Engl. 2008;47(34):6395-8. doi: 10.1002/anie.200801885. No abstract available.


Safety and immunogenicity of tyrosinase DNA vaccines in patients with melanoma.

Wolchok JD, Yuan J, Houghton AN, Gallardo HF, Rasalan TS, Wang J, Zhang Y, Ranganathan R, Chapman PB, Krown SE, Livingston PO, Heywood M, Riviere I, Panageas KS, Terzulli SL, Perales MA.

Mol Ther. 2007 Nov;15(11):2044-50. Epub 2007 Aug 28.


Pilot study of a heptavalent vaccine-keyhole limpet hemocyanin conjugate plus QS21 in patients with epithelial ovarian, fallopian tube, or peritoneal cancer.

Sabbatini PJ, Ragupathi G, Hood C, Aghajanian CA, Juretzka M, Iasonos A, Hensley ML, Spassova MK, Ouerfelli O, Spriggs DR, Tew WP, Konner J, Clausen H, Abu Rustum N, Dansihefsky SJ, Livingston PO.

Clin Cancer Res. 2007 Jul 15;13(14):4170-7.


Immunological validation of the EpitOptimizer program for streamlined design of heteroclitic epitopes.

Houghton CS, Engelhorn ME, Liu C, Song D, Gregor P, Livingston PO, Orlandi F, Wolchok JD, McCracken J, Houghton AN, Guevara-Patiño JA.

Vaccine. 2007 Jul 20;25(29):5330-42. Epub 2007 Jun 4.


Immunization of high-risk breast cancer patients with clustered sTn-KLH conjugate plus the immunologic adjuvant QS-21.

Gilewski TA, Ragupathi G, Dickler M, Powell S, Bhuta S, Panageas K, Koganty RR, Chin-Eng J, Hudis C, Norton L, Houghton AN, Livingston PO.

Clin Cancer Res. 2007 May 15;13(10):2977-85.


A phase I pilot study of autologous heat shock protein vaccine HSPPC-96 in patients with resected pancreatic adenocarcinoma.

Maki RG, Livingston PO, Lewis JJ, Janetzki S, Klimstra D, Desantis D, Srivastava PK, Brennan MF.

Dig Dis Sci. 2007 Aug;52(8):1964-72. Epub 2007 Apr 10.


Cancer vaccines targeting carbohydrate antigens.

Livingston PO, Ragupathi G.

Hum Vaccin. 2006 May-Jun;2(3):137-43. Epub 2006 May 16.


Phase II study of temozolomide plus pegylated interferon-alpha-2b for metastatic melanoma.

Hwu WJ, Panageas KS, Menell JH, Lamb LA, Aird S, Krown SE, Williams LJ, Chapman PB, Livingston PO, Wolchok JD, Houghton AN.

Cancer. 2006 Jun 1;106(11):2445-51.


Preparation and evaluation of unimolecular pentavalent and hexavalent antigenic constructs targeting prostate and breast cancer: a synthetic route to anticancer vaccine candidates.

Ragupathi G, Koide F, Livingston PO, Cho YS, Endo A, Wan Q, Spassova MK, Keding SJ, Allen J, Ouerfelli O, Wilson RM, Danishefsky SJ.

J Am Chem Soc. 2006 Mar 1;128(8):2715-25.


Identification of DHBcAg as a potent carrier protein comparable to KLH for augmenting MUC1 antigenicity.

Gathuru JK, Koide F, Ragupathi G, Adams JL, Kerns RT, Coleman TP, Livingston PO.

Vaccine. 2005 Sep 15;23(39):4727-33.


Selection of GM2, fucosyl GM1, globo H and polysialic acid as targets on small cell lung cancers for antibody mediated immunotherapy.

Livingston PO, Hood C, Krug LM, Warren N, Kris MG, Brezicka T, Ragupathi G.

Cancer Immunol Immunother. 2005 Oct;54(10):1018-25. Epub 2005 May 31.


Temozolomide plus thalidomide in patients with brain metastases from melanoma: a phase II study.

Hwu WJ, Lis E, Menell JH, Panageas KS, Lamb LA, Merrell J, Williams LJ, Krown SE, Chapman PB, Livingston PO, Wolchok JD, Houghton AN.

Cancer. 2005 Jun 15;103(12):2590-7.


Synthesis of selected LeY and KH-1 analogues: a medicinal chemistry approach to vaccine optimization.

Spassova MK, Bornmann WG, Ragupathi G, Sukenick G, Livingston PO, Danishefsky SJ.

J Org Chem. 2005 Apr 29;70(9):3383-95.


Antibodies against tumor cell glycolipids and proteins, but not mucins, mediate complement-dependent cytotoxicity.

Ragupathi G, Liu NX, Musselli C, Powell S, Lloyd K, Livingston PO.

J Immunol. 2005 May 1;174(9):5706-12.


Comparison of antigen constructs and carrier molecules for augmenting the immunogenicity of the monosaccharide epithelial cancer antigen Tn.

Kagan E, Ragupathi G, Yi SS, Reis CA, Gildersleeve J, Kahne D, Clausen H, Danishefsky SJ, Livingston PO.

Cancer Immunol Immunother. 2005 May;54(5):424-30. Epub 2004 Dec 30.


Vaccination of patients with small-cell lung cancer with synthetic fucosyl GM-1 conjugated to keyhole limpet hemocyanin.

Krug LM, Ragupathi G, Hood C, Kris MG, Miller VA, Allen JR, Keding SJ, Danishefsky SJ, Gomez J, Tyson L, Pizzo B, Baez V, Livingston PO.

Clin Cancer Res. 2004 Sep 15;10(18 Pt 1):6094-100.


Sequential immunization of melanoma patients with GD3 ganglioside vaccine and anti-idiotypic monoclonal antibody that mimics GD3 ganglioside.

Chapman PB, Wu D, Ragupathi G, Lu S, Williams L, Hwu WJ, Johnson D, Livingston PO.

Clin Cancer Res. 2004 Jul 15;10(14):4717-23.


A fully synthetic therapeutic vaccine candidate targeting carcinoma-associated Tn carbohydrate antigen induces tumor-specific antibodies in nonhuman primates.

Lo-Man R, Vichier-Guerre S, Perraut R, Dériaud E, Huteau V, BenMohamed L, Diop OM, Livingston PO, Bay S, Leclerc C.

Cancer Res. 2004 Jul 15;64(14):4987-94.


A phase II trial comparing five dose levels of BEC2 anti-idiotypic monoclonal antibody vaccine that mimics GD3 ganglioside.

Chapman PB, Williams L, Salibi N, Hwu WJ, Krown SE, Livingston PO.

Vaccine. 2004 Jul 29;22(21-22):2904-9.


Vaccination of small cell lung cancer patients with polysialic acid or N-propionylated polysialic acid conjugated to keyhole limpet hemocyanin.

Krug LM, Ragupathi G, Ng KK, Hood C, Jennings HJ, Guo Z, Kris MG, Miller V, Pizzo B, Tyson L, Baez V, Livingston PO.

Clin Cancer Res. 2004 Feb 1;10(3):916-23.


Selective CD4+ lymphopenia in melanoma patients treated with temozolomide: a toxicity with therapeutic implications.

Su YB, Sohn S, Krown SE, Livingston PO, Wolchok JD, Quinn C, Williams L, Foster T, Sepkowitz KA, Chapman PB.

J Clin Oncol. 2004 Feb 15;22(4):610-6. Epub 2004 Jan 15. Erratum in: J Clin Oncol. 2004 May 15;22(10):2038.


Fully synthetic carbohydrate-based vaccines in biochemically relapsed prostate cancer: clinical trial results with alpha-N-acetylgalactosamine-O-serine/threonine conjugate vaccine.

Slovin SF, Ragupathi G, Musselli C, Olkiewicz K, Verbel D, Kuduk SD, Schwarz JB, Sames D, Danishefsky S, Livingston PO, Scher HI.

J Clin Oncol. 2003 Dec 1;21(23):4292-8.


Consistent antibody response against ganglioside GD2 induced in patients with melanoma by a GD2 lactone-keyhole limpet hemocyanin conjugate vaccine plus immunological adjuvant QS-21.

Ragupathi G, Livingston PO, Hood C, Gathuru J, Krown SE, Chapman PB, Wolchok JD, Williams LJ, Oldfield RC, Hwu WJ.

Clin Cancer Res. 2003 Nov 1;9(14):5214-20.


Phase II study of temozolomide plus thalidomide for the treatment of metastatic melanoma.

Hwu WJ, Krown SE, Menell JH, Panageas KS, Merrell J, Lamb LA, Williams LJ, Quinn CJ, Foster T, Chapman PB, Livingston PO, Wolchok JD, Houghton AN.

J Clin Oncol. 2003 Sep 1;21(17):3351-6.


A preclinical study comparing approaches for augmenting the immunogenicity of a heptavalent KLH-conjugate vaccine against epithelial cancers.

Ragupathi G, Koide F, Sathyan N, Kagan E, Spassova M, Bornmann W, Gregor P, Reis CA, Clausen H, Danishefsky SJ, Livingston PO.

Cancer Immunol Immunother. 2003 Oct;52(10):608-16. Epub 2003 Jun 17.


Phase I trial of high dose paracetamol and carmustine in patients with metastatic melanoma.

Wolchok JD, Williams L, Pinto JT, Fleisher M, Krown SE, Hwu WJ, Livingston PO, Chang C, Chapman PB.

Melanoma Res. 2003 Apr;13(2):189-96.


On the power of chemical synthesis: immunological evaluation of models for multiantigenic carbohydrate-based cancer vaccines.

Ragupathi G, Coltart DM, Williams LJ, Koide F, Kagan E, Allen J, Harris C, Glunz PW, Livingston PO, Danishefsky SJ.

Proc Natl Acad Sci U S A. 2002 Oct 15;99(21):13699-704. Epub 2002 Oct 1.


Clinical results using biochemotherapy as a standard of care in advanced melanoma.

Chapman PB, Panageas KS, Williams L, Wolchok JD, Livingston PO, Quinn C, Hwu WJ.

Melanoma Res. 2002 Aug;12(4):381-7.


Temozolomide plus thalidomide in patients with advanced melanoma: results of a dose-finding trial.

Hwu WJ, Krown SE, Panageas KS, Menell JH, Chapman PB, Livingston PO, Williams LJ, Quinn CJ, Houghton AN.

J Clin Oncol. 2002 Jun 1;20(11):2610-5. Erratum in: J Clin Oncol 2002 Aug 1;20(15):3361.


T-cell responses against tyrosinase 368-376(370D) peptide in HLA*A0201+ melanoma patients: randomized trial comparing incomplete Freund's adjuvant, granulocyte macrophage colony-stimulating factor, and QS-21 as immunological adjuvants.

Schaed SG, Klimek VM, Panageas KS, Musselli CM, Butterworth L, Hwu WJ, Livingston PO, Williams L, Lewis JJ, Houghton AN, Chapman PB.

Clin Cancer Res. 2002 May;8(5):967-72.


Vaccination with CD20 peptides induces a biologically active, specific immune response in mice.

Roberts WK, Livingston PO, Agus DB, Pinilla-Ibarz J, Zelenetz A, Scheinberg DA.

Blood. 2002 May 15;99(10):3748-55.


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