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PUBLICATIONS

Leukocyte Trafficking

  1. Rosen H, Gonzalez-Cabrera PJ, Sanna MG, Brown S. (2008) Sphingosine 1-phosphate receptor signaling.  Annual Rev Biochem (In Press)
  2. Gonzalez-Cabrera PJ, Jo E, Sanna MG, Brown S, Leaf N, Marsolais D, Schaeffer MT, Chapman J, Cameron M, Guerrero M, Roberts E, Rosen H. (2008) Full pharmacological efficacy of a novel S1P1 agonist that does not require S1P-like head-group interactions. Mol Pharm (In Press)
  3. Schurer SC, Brown SJ, Gonzalez-Cabrera P, Schaeffer MT, Chapman J, Chase P, Spicer T, Hodder P, Rosen H.  (2008) Ligand-binding pocket shape differences between S1P1 and S1P3 determine efficiency of chemical probe identification by uHTS.  Amer Chem Soc Chem Biol  3(8):486-498
  4. Marsolais D, Hahm B, Edelmann KH, Walsh KB, Guerrero M, Hatta Y, Kawaoka Y, Roberts E, Oldstone MBA, Rosen H.  (2008) Local not systemic modulation of dendritic cell S1P receptors in lung blunts virus-specific immune responses to influenza.  Mol Pharm 74(3):896-903
  5. Rosen H, Gonzalez-Cabrera P, Marsolais D, Cahalan S, Don AS, Sanna MG.  (2008) Modulating tone: the overture of S1P receptor immunotherapeutics.  Immunol Rev 223: 221-235
  6. Nakai R, Salisbury CM, Rosen H, Cravatt BF. (2008) Ranking the selectivity of PubChem screening hits by activity-based protein profiling: MMP13 as a case study. Bioorg med Chem (In Press, Epublished)
  7. Don AS, Rosen H. (2008) A fluorescent plate reader assay for ceramide kinase. Anal Biochem (In Press)
  8. Niessen F, Schaffner F, Furlan-Freguia C, Pawlinski R, Bhattacharjee G, Chun J, Derian CK, Andrade-Gordon P, Rosen H, Ruf W (2008) Dendritic cell PAR1-S1P3 signalling couples coagulation and inflammation. Nature (In Press)
  9. Tsukada YT, Sanna MG, Rosen H, Gottlieb RA (2007) S1P1-Selective agonist SEW2871 exacerbates reperfusion arrhythmias.  J Cardiovasc Pharmacol 50(6):660-669
  10. Lee H-K, Brown SJ, Rosen H, Tobias PS (2007) Application of â-Lactamase Enzyme Complementation to the High-Throughput Screening of Toll-Like Receptor Signaling Inhibitors. Am Soc Pharm Exp Ther 72(4):868-75
  11. Don AS, Martinez-Lamenca C, Webb WR, Proia RL, Roberts E, Rosen H (2007) Essential requirement for sphingosine kinase 2 in a sphingolipid apoptosis pathway activated by FTY720 analogs. J Biol Chem 282(21):15833-42
  12. Gonzalez-Cabrera P, Hla T, Rosen H (2007) Mapping pathways downstream of sphingosine 1-phosphate subtype 1 by differential chemical perturbation and proteomics. J Biol Chem 282(10):7254-64
  13. Rosen H, Sanna MG, Cahalan S, Gonzalez-Cabrera P (2007) Tipping the gatekeeper: S1P regulation of stromal barrier function.  Trends Immunol. 28(3):102-7
  14. Chun, J. and H. Rosen (2006). "Lysophospholipid receptors as potential drug targets in tissue transplantation and autoimmune diseases." Curr. Pharm. Des. 12(2):161-71.
  15. Sanna MG, Wang SK, Gonzalez-Cabrera P, Don A, Marsolais D, Jo E, Cheng WC, Wong CH, Rosen H. (2006) Enhancement of capillary leakage and restoration of lymphocyte egress by a chiral S1P1 antagonist in vivo.  Nat. Chem. Biol. 2(8):434-441

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                  NATURE CHEMICAL BIOLOGY NEWS & VIEWS: Schultz C:  Lipid-induced phenotypes

                  NIMH Review: New Tool Can Boost or Block the Body’s Protective Inner Barriers

  1. Alfonso C, McHeyzer-Williams MG, Rosen H. (2006) CD69 down-modulation and inhibition of thymic egress by short and long-term selective chemical agonism of S1P1 receptors. Eur J Immunol  36(1):149-59
  2. Wei SH, Rosen H, Matheu MP, et al. (2005) Sphingosine 1-phosphate type 1 receptor agonism inhibits transendothelial migration of medullary T cells to lymphatic sinuses.  Nat Immunol 6:1228-35

      NATURE IMMUNOLOGY NEWS & VIEWS: Ley K,  Morris M:  Signals for lymphocyte egress

  1. Rosen H, Goetzl EJ. (2005) Sphingosine 1-phosphate and its receptors: an autocrine and paracrine network. Nat Rev Immunol. 5(7):560-570
  2. Jo E, Sanna MG, Gonzalez-Cabrera PJ, Thangada S, Tigy G, Osborne DA, Hla T, Parrill AL, Rosen H. (2005) S1P1-selective in vivo-active agonist from high throughput screening: Off-the-shelf chemical probes of receptor interactions, signaling and fate. Chem Biol  12(6):703-715

      TSRI News & Views: July 4, 2005 Scientists Discover New Key to Pulmonary Edema in Respiratory Distress Syndrome

  1. Martinez X, Kreuwel HTC, Redmond WL, Trenney R, Hunter K, Rosen H, Sarvetnick N, Wicker LS, Sherman LA. (2005) CD8+ T cell tolerance in NOD mice is restored by insulin dependent diabetes (Idd) resistance alleles. J. Exp. Med. 175(3):1677-1685
  2. Rosen H. (2005) Chemical approaches to the lysophospholipid receptors. Prostaglandins & Other Lipid Mediators. 77(1-4):179-184
  3. Gong Q, Ou Q, Ye S, Lee WP, Cornelius J, Diehl L, Lin WY, Hu Z, Lu Y, Chen Y, Wu Y, Meng YG, Gribling P, Lin Z, Nguyen K, Tran T, Zhang Y, Rosen H, Martin F, Chan AC. (2005) Importance of cellular microenvironment and circulatory dynamics in B cell immunotherapy. J. Imm. 174(2):817-26
  4. Goetzl E.J., Rosen H. (2004) Regulation of immunity by lysosphingolipids and their G protein-coupled receptors. J Clin Invest. 2004 Dec;114(11):1531-7
  5. Yan L, Hale JJ, Lynch CL, Budhu R, Gentry A, Mills SG, Hajdu R, Keohane CA, Rosenbach MJ, Milligan JA, Shei GJ, Chrebet G, Bergstrom J, Card D, Rosen H, Mandala SM. Design and synthesis of conformationally constrained 3-(N-alkylamino)propylphosphonic acids as potent agonists of sphingosine-1-phosphate (S1P) receptors. Bioorg Med Chem Lett. 2004 Oct 4;14(19):4861-6.
  6. Hale JJ, Yan L, Neway WE, Hajdu R, Bergstrom JD, Milligan JA, Shei GJ, Chrebet GL, Thornton RA, Card D, Rosenbach M, Rosen H, Mandala S. Synthesis, stereochemical determination and biochemical characterization of the enantiomeric phosphate esters of the novel immunosuppressive agent FTY720. Bioorg. Med. Chem. 2004 Aug 6; 12:4803-7.
  7. Hale, J., Doherty, G., Toth, L., Mills, S., Hajdu, R., Keohane, C., Rosenbach, M., Milligan, J., Shei, G., Chrebet, G., Bergstrom, J., Card, D., Forrest, M., Sun, S., West, S., Xie, H., Nomura, N, Rosen, H., Mandala, S. (2004) Selecting against S1P3 enhances the acute cardiovascular tolerability of 3-(N-benzyl)aminopropylphosphonic acid S1P receptor agonists. Bio. Med. Chem. Ltrs. (in press)
  8. Hale, J., Doherty, G., Toth, L., Li, Z., Mills, S., Hajdu, R., Keohane, C., Rosenbach, M., Milligan, J., Shei, G., Chrebet, G., Bergstrom, J., Card, D., Rosen, H., Mandala, S. (2004) The discovery of 3-(N-alkyl)aminopropylphosphonic acids as potent S1P receptor agonists. Bio. Med. Chem. Ltrs. (in press)
  9. Hale, J., Neway, W., Mills, S., Hajdu, R., Keohane, C., Rosenbach, M., Milligan, J., Shei, G., Chrebet, G., Bergstrom, J., Card, D., Koo, G., Koprak, S., Jackson, J., Rosen, H., Mandala, S. (2004) Potent S1P receptor agonists replicate the pharmacologic actions of the novel immune modulator FTY720. Bio. Med. Chem. Ltrs. 14:3351-3355
  10. Forrest, M., Sun, S.-Y., Hajdu, R., Bergstrom, J., Card, D., Doherty, G., Hale, J., Keohane, C., Meyers, C., Milligan, J., Mills, S., Nomura, N., Rosen, H., Rosenbach, M., Shei, G.-J., Singer, I., Tain, M., West, S., White, V., Xie, J., Proia, R., Mandala, S. (2004) Immune cell regulation and cardiovascular effects of sphingosine 1-phosphate receptor agonists in rodents are mediated via distinct receptor sub-types. J. Pharmacol. Exp. Therap. 309:758
  11. Sanna, G., Liao, J., Jo, E., Alfonso, C., Ahn, M., Peterson, M., Webb, B., Lefebvre, S., Chun, J., Gray, N., Rosen, H. (2004) Spingosine 1-phosphate (S1P) receptor subtypes S1P1 and S1P3, respectively, regulate lymphocyte recirculation and heart rate. J. Biol. Chem. 279:13839-13848
  12. Rosen, H., Alfonso, C., Surh, C.D., McHeyzer-Williams, M.G. (2003) Rapid induction of medullary thymocyte phenotypic maturation and inhibition of thymic egress at low nanomolar concentrations of sphingosine 1-phosphate receptor agonist. PNAS 100:10907-10912.
  13. Rosen, H., Sanna, G., Alfonso, C. (2003) Egress: a receptor-regulated step in lymphocyte trafficking. Imm. Rev. 195:160-177.
  14. Rosen, H., Kozarich, J.W. (2003) Next-generation therapeutics. Balancing on the uneasy cusp: integrating linear and parallel approaches to new generation therapeutics. Curr. Opin. Chem. Biology 7:443-445.
  15. Rosen, H., Liao, J. (2003) Sphingosine 1-phosphate pathway therapeutics: a lipid ligand-receptor paradigm. Curr. Opin. Chem. Bio. 7:461-468.
  16. J. Xie, N. Nomura, E. Quackenbush, M. Forrest and H. Rosen (2003) Sphingosine-1-Phosphate Receptor Agonists Impair the Efficiency of the Local Immune Response by Altering Trafficking of Naïve and Antigen-Activated CD4+ T Cells. J. Immunol. 170: 3662-3670.
  17. Parent, S.A., T. Zhang, G. Chrebet, J.A. Clemas, D.J. Figueroa, B. Ky, R.A. Blevins, C.P. Austin, and H. Rosen. (2002). Molecular characterization of the murine SIGNR1 gene encoding a C-type lectin homologous to human DC-SIGN and DC-SIGNR. Gene 293:33.
  18. Mandala, S., Hajdu, R., Bergstrom, J., Quackenbush E., Xie J., Milligan, J., Thornton, R., Shei, G-J., Card, D., Keohane, C., Rosenbach, M., Hale, J., Lynch, C., Rupprecht, K., Parsons, W., and Rosen, H. (2002) Alteration of Lymphocyte Trafficking by Sphingosine 1-Phosphate Receptor Agonists. Science 296:346-9. Published online 28 March 2002;10.1126/science.1070238
  19. Beck, L.A. et al. (1997). Cutaneous injection of RANTES causes eosinophil recruitment: comparison of non-allergic and allergic human subjects. Journal Immunol. 159: 2962-2972.
  20. Zheng, H., D. Fletcher, W. Kozak et al (1995). Resistance to fever induction and impaired acute phase response in Interleukin-1? deficient mice. Immunity 3:9-19.
  21. Gordon, E.J., K.J. Myers, J.P.Dougherty, H. Rosen and Y. Ron. (1995) “Both anti-CD11a and anti-CD11b therapy delay the onset and diminish the severity of experimental autoimmune encephalitis. Neuroimmunol. Nov; 62(2): 153-60
  22. Konteatis Z, Siciliano S, VanRiper G, et al. (1994) Development of C5a receptor antagonists: differential loss of functional responses. J. Immunol. 153:4200-5.
  23. DeMartino, J., G. Van Riper, S. Siciliano, Z. Konteatis, H. Rosen and M. Springer 1994 “The amino-terminus of the human C5a receptor is required for high affinity C5a binding but not for signal transduction.” J.Biol.Chem. 269:14446-50.
  24. Van Riper, G., D. Nicholson, M. Scheid, P. Fischer, M. Springer and H. Rosen 1994 “Induction, characterization and functional coupling of the high affinity chemokine receptor for Rantes and MIP-1a upon differentiation of an eosinophilic HL-60 line.” J.Immunol. 152: 4055-61.
  25. Meurer, R., G. Van Riper, W. Feeney, P. Cunningham, D. Hora, M. Springer, D. E. MacIntyre and H. Rosen 1993 “Rapid formation of eosinophilic intradermal inflammatory sites in the dog by injection of human Rantes but not hMCP-1, hMIP-1a or hIL-8.” J.Exp.Med. 178:1913-21
  26. Siciliano, S., J. DeMartino, Z. Konteatis, L. Malkowits, G. Van Riper, T. Rollins, S. Bondy, H. Rosen and M. Springer 1994 “Two-site binding of C5a by its receptor: A new binding paradigm for G protein-coupled receptors.” Proc. Natl. Acad. Sci. U.S.A. 91: 1214-8.
  27. Koo, G., H. Rosen, A. Sirotina, X.-D. Ma and L. Shultz 1993 “Prevention of immunopathologic changes in viable motheaten bone marrow chimeras with anti-CD11b antibody.” J. Immunol. 151: 6733-41.
  28. Van Riper, G., S. Siciliano, P.A. Fischer, R. Meurer, M. Springer, and H. Rosen. 1993. "Characterization and species distribution of high affinity GTP-coupled receptors for human Rantes and monocyte-chemoattractant protein-1". J. Exp. Med. 177: 851-6.
    21) Cervia,J.S., H.Rosen and H.W.Murray. (1993) "Effector role of the blood monocyte in experimental visceral Leishmaniasis." Infection and Immunity 61: 1330-3.
  29. Whitcup,S., L.R.DeBarge, H.Rosen, R.B.Nussenblatt and C-C. Chan. (1993) "Monoclonal antibody against CD11b/CD18 inhibits endotoxin-induced uveitis." Invest. Ophth. Vis. Sci. 34(3):673-681
  30. Piguet, P.F., H. Rosen, C. Vesin and G.E.Grau (1993) "Antibody to the leukocyte integrins CD11a or CD11b prevents or cures pulmonary fibrosis elicited in mice by bleomycin or silica." Am. Rev.Resp.Dis. 147: 445-451
  31. Al Attiyah, R, H. Rosen and G.A.W. Rook. (1992) "A model for the investigation of factors influencing TNF-mediated haemorrhagic necrosis in tissue sites primed with mycobacterial antigen preparations." Clin.Exp.Immunol. 88: 537-42.
  32. Mielke, M., H. Rosen, S. Brocke, C. Peters and H. Hahn (1992) “Protective immunity and granuloma formation are mediated by two distinct TNF-alpha and Gamma Interferon-dependent T cell-phagocyte interactions in murine listeriosis: Dissociation on the basis of Phagocyte adhesion mechanisms.” Infect. Immun. 60: 1875-82.
  33. Robinson MK, D Andrew, H Rosen, D Brown, S Ortlepp, P Stephens and EC Butcher (1992) "Antibody against the Leu-CAM ?-chain (CD18) promotes both LFA-1- and CR3-dependent adhesion events." J.Immunol 148:1080-5.
  34. Grau G., P. Pointaire, P.-F. Piguet, H. Rosen, I. Stamenkovic, F. Takei and P. Vassalli (1991). “Late administration of monoclonal antibody to leukocyte function-antigen abrogates incipient murine cerebral malaria.” Eur.J.Immunol. 21: 2265-7.
  35. Blankenstein, T., Z. Qin, K. Uberla, W. Muller, H. Rosen, D.-T. Volk and T. Diamantstein (1991). “Tumor suppression after tumor cell targeted TNF alpha gene transfer.” J.Exp.Med.173: 1047-52.
  36. Hutchings, P., H. Rosen, L. O'Reilly, E. Simpson, S. Gordon and A. Cooke (1990). “Transfer of diabetes in mice prevented by blockade of adhesion-promoting receptor on macrophages.” Nature. 348: 639-42.
  37. Rosen, H. and S. Gordon (1990). “Adoptive transfer of fluorescence-labelled cells shows that resident peritoneal macrophages are able to migrate into specialized lymphoid organs and inflammatory sites in the mouse.” Eur.J.Immunol. 20: 1251-8.
  38. Lunn, E., V. Perry, M. Brown, H. Rosen and S. Gordon (1989). “Absence of Wallerian degeneration does not hinder regeneration in peripheral nerves.” Eur.J.Neurosci. 1: 27-33.
  39. Rosen, H., S. Gordon and R. North (1989). “Exacerbation of murine listeriosis by a monoclonal antibody specific for the type 3 complement receptor of myelomonocytic cells.” J.Exp.Med. 170: 27.
  40. Rosen, H., G. Milon and S. Gordon (1989). “Antibody to the murine type 3 complement receptor inhibits T lymphocyte-dependent recruitment of myelomonocytic cells in vivo.” J.Exp.Med. 169: 535.
  41. Cooper, A., H. Rosen and J. Blackwell (1988). “Monoclonal antibodies that recognize distinct epitopes of the macrophage type 3 complement receptor differ in their ability to inhibit the binding of Leishmania promastigotes harvested at different phases of their growth cycle.” Immunology. 65: 511-4.
  42. Rosen, H. and S. Gordon (1987). “Monoclonal antibody to the murine type 3 complement receptor inhibits adhesion of myelomonocytic cells in vitro and inflammatory cell recruitment in vivo.” J.Exp.Med. 166: 1685-1702.
  43. Rosen, H. and S. Gordon (1987). “Surface events in polymorphonuclear leukocyte activation: insights from a hydrophobic membrane antigen that triggers the respiratory burst.” J.Cell Sci. 88: 591-601.
  44. Berton, G., H. Rosen, R. Ezekowitz, P. Bellavite, M. Serra, F. Rossi and S. Gordon (1986). “Monoclonal antibodies to a particulate superoxide-forming system stimulate a respiratory burst in intact guinea pig neutrophils.” Proc.Natl.Acad.Sci.U.S.A. 83: 4002-6.
  45. Millar, R., H. Rosen, M. Badminton, C. Pesqualini and B. Kerdelhue (1983). “Luteinizing-hormone releasing-hormone binding to purified rat pituitary nuclei.” FEBS Lett. 153: 382-6.

 

Infectious Diseases

  1. Bowman, J.C., P.S. Hicks, M.B. Kurtz, H. Rosen, D.M. Schmatz, P.A. Liberator, and C.M. Douglas. 2002. The Antifungal Echinocandin Caspofungin Acetate Kills Growing Cells of Aspergillus fumigatus In Vitro. Antimicrob. Agents Chemother. 46: 3001.
  2. Abruzzo, G.K., Gill, C.J., Flattery, A.M., Kong, L., Leighton, C., Smith, J.G., Pikounis, V.B., Bartizal, K., and H. Rosen. (2000). Efficacy of the echinocandin Caspofungin against aspergillosis and candidiasis in cuyclophosphamide-induced immunosuppressed mice. Antimicrob. Agents Chemother. 44:2310-8.
  3. Kohler, J., K.L. Dorso, K. Young, G.G. Hammond, H. Rosen, H. Kropp and L.L. Silver (1999) In vitro activities of the potent, broad-spectrum carbapenem MK-0826 against broad-spectrum ?-lactamase- and Extended-spectrum ?-lactamase-producing Klebsiella pneumoniae and Escherichia coli clinical isolates. Antimicrob. Agents Chemother. 43:1170-6.
  4. Rosen, H., R. Hajdu, L. Silver, H.Kropp, K. Dorso, J. Kohler, J. G. Sundelof, J. Huber, G. G. Hammond, J. J. Jackson, C. J. Gill, R. Thompson, B. A. Pelak, J. H. Epstein-Toney, G. Lankas, R. R. Wilkening, K. J. Wildonger, T. A. Blizzard, F. P. DiNinno, R. W. Ratcliffe, J. V. Heck, J. W. Kozarich, M. L. Hammond (1999) Reduced Immunotoxicity and Preservation of Antibacterial Activity in a Releasable Side-Chain Carbapenem Antibiotic. Science 283:703-6.
  5. Gill, C.J., J.J. Hackson, L.S. Gerckens, B.A. Pelak, R.K. Thompson, J.G. Sundelof, H. Kropp and H. Rosen. (1998) In vivo activity and phramacokinetic evaluation of a novel long-acting carbapenem MK-826. Antimicrob. Agents. Chemother. 42:1996-2001.
  6. Abruzzo, G.K., A.M. Flattery, C.J. Gill, L. Kong, J.G. Smith, V. Pikounis, J. Balkovec, A. Bouffard, J. Dropinski, H. Rosen, H. Kropp & K. Bartizal. (1997) Evaluation of the echinocandin antifungal MK-0991 efficacies in mouse models of disseminated aspergillosis, candidiasis and cryptococcosis. Antimicrob. Agents. Chemother. 41:2333-8.
  7. Sundelof, J.G., R. Hajdu, C.J. Gill. R. Thompson, H. Rosen and H. Kropp. (1997) Pharmacokinetics of L-749,345, a long-acting carbapenem antibiotic in primates. Antimicrob. Agents. Chemother. 41:1743-8.