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The Rosen Laboratory

PUBLICATIONS

Peer-reviewed journals

  1. Plate L, Cooley CB, Chen JJ, Paxman RJ, Gallagher CM, Madoux F, Genereux JC, Dobbs W, Garza D, Spicer TP, Scampavia L, Brown SJ, Rosen H, Powers ET, Walter P, Hodder P, Wiseman RL, Kelly JW. (2016) Small moleculae proteostasis regulators that reprogram the ER to reduce extracellular protein aggregation. Elife. 2016 Jul 20; 5. pii: e15550. doi: 10.7554/eLife.15550. PMID: 27435961
  2. Ewing H, Fernandez-Vega V, Spicer TP, Chase P, Brown S, Scampavia L, Roush WR, Riley S, Rosen H, Hodder P, Lambeau G, Gelb MH. (2016) Fluorometric High-Throughput Screening Assay for Secreted Phospholipases A2 Using Phospholipid Vesicles. J Biomol Screen. 21(7):713-21 pmid: 27146384
  3. Teijaro JR, Studer S, Leaf N, Kiosses WB, Nguyen N, Matsuki K, Negishi H, Taniguchi T, Oldstone MB, Rosen H. (2016) S1PR1-mediated IFNAR1 degradation modulates plasmacytoid dendritic cell interferon-α autoamplification. Proc Natl Acad Sci USA. 113(5):1351-6.  PMID: 26787880
  4. Sanna MG, Vincent KP, Repetto E, Nguyen N, Brown SJ, Abgaryan L, Riley SW, Leaf NB, Cahalan SM, Kiosses WB, Kohno Y, Brown JH, McCulloch AD, Rosen H, Gonzalez-Cabrera PJ.(2016) Bitopic Sphingosine 1-Phosphate Receptor 3 (S1P3) Antagonist Rescue from Complete Heart Block: Pharmacological and Genetic Evidence for Direct S1P3 Regulation of Mouse Cardiac Conduction. Mol Pharmacol. 2016 Jan;89(1):176-86. doi: 10.1124/mol.115.100222. Epub 2015 Oct 22.PMID: 26494861
  5. Blanc CA, Grist JJ, Rosen H, Sears-Kraxberger I, Steward O, Lane TE (2015) Sphingosine-1-phosphate receptor antagonism enhances proliferation and migration of engrafted neural progenitor cells in a model of viral-induced demyelination..Am J Pathol. 2015 Oct;185(10):2819-32. doi: 10.1016/j.ajpath.2015.06.009. PMID: 26435414
  6. Niphakis MJ, Lum KM, Cognetta AB 3rd, Correia BE, Ichu TA, Olucha J, Brown SJ, Kundu S, Piscitelli F, Rosen H, Cravatt BF. (2015) A Global Map of Lipid-Binding Proteins and Their Ligandability in Cells. Cell. 2015 Jun 18;161(7):1668-80. doi: 10.1016/j.cell.2015.05.045. PMID: 26091042
  7. Skerry C, Scanlon K, Rosen H, Carbonetti NH. (2014) Sphingosine-1-phosphate receptor agonism reduces Bordetella pertussis-mediated lung pathology. J Infect Dis. 2014 Dec 23. pii: jiu823. [Epub ahead of print] PMID: 25538274
  8. Blanc CA, Rosen H, Lane TE. (2014) FTY720 (fingolimod) modulates the severity of viral-induced encephalomyelitis and demyelination. J Neuroinflammation. 2014 Aug 20;11:138. doi: 10.1186/s12974-014-0138-y. PMID: 25138356
  9. Sarkisyan G, Gay LH, Nguyen H, Felding BH, Rosen H. Host endothelial S1PR1 regulation of vascular permeability modulates tumor growth.  Am J Physiol Cell Physiol. 2014 Jul 1;307(1):C14-24. PMID:24740542
  10. Chang MR, Rosen H, Griffin PR. RORs in Autoimmune Disease. Curr Top Microbiol Immunol. 2014;378:171-82. doi: 10.1007/978-3-319-05879-5_8. PMID: 24728598
  11. Oldstone MB, Rosen H. Cytokine Storm Plays a Direct Role in the Morbidity and Mortality from Influenza Virus Infection and is Chemically Treatable with a Single Sphingosine-1-Phosphate Agonist Molecule. Curr Top Microbiol Immunol. 2014;378:129-47. doi: 10.1007/978-3-319-05879-5_6. PMID: 24728596
  12. Rosen H, Germana Sanna M, Gonzalez-Cabrera PJ, Roberts E. The organization of the sphingosine 1-phosphate signaling system. Curr Top Microbiol Immunol. 2014;378:1-21. doi: 10.1007/978-3-319-05879-5_1.  PMID: 24728591
  13. Walsh KB, Teijaro JR, Brock LG, Fremgen DM, Collins PL, Rosen H, Oldstone MB. Animal model of respiratory syncytial virus: CD8+ T cells cause a cytokine storm that is chemically tractable by sphingosine-1-phosphate 1 receptor agonist therapy. J Virol. 2014 Jun;88(11):6281-93. doi: 10.1128/JVI.00464-14. Epub 2014 Mar 26. PMID: 24672024
  14. Ohotski J, Rosen H, Bittman R, Pyne S, Pyne NJ.  Sphingosine kinase 2 prevents the nuclear translocation of sphingosine 1-phosphate receptor-2 and tyrosine 416 phosphorylated c-Src and increases estrogen receptor negative MDA-MB-231 breast cancer cell growth: The role of sphingosine 1-phosphate receptor-4.. Cell Signal. 2014 May;26(5):1040-7. doi: 10.1016/j.cellsig.2014.01.023. Epub 2014 Jan 29. PMID: 24486401
  15. Urbano M, Guerrero M, Rosen H, Roberts E. Antagonists of the kappa opioid receptor. Bioorg Med Chem Lett. 2014 May 1;24(9):2021-32. doi: 10.1016/j.bmcl.2014.03.040. Epub 2014 Mar 24. PMID: 24690494
  16. Teijaro JR, Walsh KB, Long JP, Tordoff KP, Stark GV, Eisfeld AJ, Kawaoka Y, Rosen H, Oldstone MB. Protection of ferrets from pulmonary injury due to H1N1 2009 influenza virus infection: immunopathology tractable by sphingosine-1-phosphate 1 receptor agonist therapy. Virology. 2014 Mar;452-453:152-7. doi: 10.1016/j.virol.2014.01.003. Epub 2014 Jan 31. PMID: 24606692
  17. Teijaro JR, Walsh KB, Rice S, Rosen H, Oldstone MB. Mapping the innate signaling cascade essential for cytokine storm during influenza virus infection. Proc Natl Acad Sci U S A. 2014 Mar 11;111(10):3799-804. doi: 10.1073/pnas.1400593111. Epub 2014 Feb 26. PMID: 24572573
  18. Rosen BR, Simke LR, Thuy-Boun PS, Dixon DD, Yu JQ, Baran PS. C-H functionalization logic enables synthesis of (+)-hongoquercin A and related compounds. Angew Chem Int Ed Engl. 2013 Jul 8;52(28):7317-20. doi: 10.1002/anie.201303838. Epub 2013 Jun 5. PMID: 23740529
  19. Guerrero M, Poddutoori R, Urbano M, Peng X, Spicer TP, Chase PS, Hodder PS, Schaeffer MT, Brown S, Rosen H, Roberts E. (2013) Discovery, design and synthesis of a selective S1P3 receptor allosteric agonist. Bioorg Med Chem Lett. 2013 Dec 1;23(23):6346-9. doi: 10.1016/j.bmcl.2013.09.075. Epub 2013 Oct 1. PMID: 24135724
  20. Urbano M, Guerrero M, Rosen H, and Roberts E (2013) Modulators of the Sphingosine 1-phosphate receptor 1. Bioorg Med Chem Lett. 2013 Dec 1; 23(23):6377-89. PMID: 24125884
  21. Satsu H, Schaeffer MT, Guerrero M, Saldana A, Eberhart C, Hodder P, Cayanan C, Schürer S, Bhhatarai B, Roberts E, Rosen H, Brown SJ. (2013) A sphingosine 1-phosphate receptor 2 selective allosteric agonist. Bioorg Med Chem. 2013 Sep 1;21(17):5373-82. doi: 10.1016/j.bmc.2013.06.012. Epub 2013 Jun 15.
  22. George Cisar EA, Nguyen N, Rosen H. (2013) A GTP affinity probe for proteomics highlights flexibility in purine nucleotide selectivity. J Am Chem Soc. 2013 Mar 27;135(12):4676-9. doi: 10.1021/ja400839e. Epub 2013 Mar 13. PMID: 23473570 [PubMed - indexed for MEDLINE]
  23. Guerrero M, Urbano M, Schaeffer MT, Brown S, Rosen H, Roberts E. (2013) SAR analysis of novel non-peptidic NPBWR1 (GPR7) antagonists. Bioorg Med Chem Lett. 2013 Feb 1;23(3):614-9. doi: 10.1016/j.bmcl.2012.12.030. Epub 2012 Dec 20. PMID: 23287738 [PubMed - indexed for MEDLINE]
  24. Nagano JM, Hsu KL, Whitby LR, Niphakis MJ, Speers AE, Brown SJ, Spicer T, Fernandez-Vega V, Ferguson J, Hodder P, Srinivasan P, Gonzalez TD, Rosen H, Bahnson BJ, Cravatt BF. (2013) Selective inhibitors and tailored activity probes for lipoprotein-associated phospholipase A(2). Bioorg Med Chem Lett. 2013 Feb 1;23(3):839-43. doi: 10.1016/j.bmcl.2012.11.061. Epub 2012 Dec 2. PMID: 23260346
  25. Stevens RC, Cherezov V, Katritch V, Abagyan R, Kuhn P, Rosen H, Wüthrich K. (2013) The GPCR Network: a large-scale collaboration to determine human GPCR structure and function. Nat Rev Drug Discov. 2013 Jan;12(1):25-34. doi: 10.1038/nrd3859. Epub 2012 Dec 14. PMID: 23237917
  26. Hulleman JD, Brown SJ, Rosen H, Kelly JW. (2013) A high-throughput cell-based Gaussia luciferase reporter assay for identifying modulators of fibulin-3 secretion. J Biomol Screen. 2013 Jul;18(6):647-58. doi: 10.1177/1087057112469405. Epub 2012 Dec 10. PMID: 23230284
  27. Oldstone MB, Teijaro JR, Walsh KB, Rosen H. (2013) Dissecting influenza virus pathogenesis uncovers a novel chemical approach to combat the infection. Virology. 2013 Jan 5;435(1):92-101. doi: 10.1016/j.virol.2012.09.039. Review. PMID: 23217619
  28. Cahalan SM, Gonzalez-Cabrera PJ, Nguyen N, Guerrero M, Cisar EA, Leaf NB, Brown SJ, Roberts E, Rosen H. (2012) Sphingosine 1-phosphate receptor 1 (S1P(1)) upregulation and amelioration of experimental autoimmune encephalomyelitis by an S1P(1) antagonist. Mol Pharmacol. 2013 Feb;83(2):316-21. doi: 10.1124/mol.112.082958. Epub 2012 Nov 30. PMID: 23204443
  29. Urbano M, Guerrero M, Zhao J, Velaparthi S, Adrian Saldanha S, Chase P, Wang Z, Civelli O, Hodder P, Schaeffer MT, Brown S, Rosen H, Roberts E. (2012) Design, synthesis and SAR analysis of novel potent and selective small molecule antagonists of NPBWR1 (GPR7). Bioorg Med Chem Lett. 2012 Dec 1;22(23):7135-41. PMID: 23079522
  30. Jo E, Bhhatarai B, Repetto E, Guerrero M, Riley S, Brown SJ, Kohno Y, Roberts E, Schürer SC, Rosen H. (2012) Novel Selective Allosteric and Bitopic Ligands for the S1P(3) Receptor. ACS Chem Biol. 2012 Dec 21;7(12):1975-83. PMID: 22971058
  31. Guerrero M, Urbano M, Wang Z, Zhao J, Velaparthi S, Schaeffer MT, Brown SJ, Saldanha SA, Chase P, Ferguson J, Civelli O, Roberts E, Hodder P, Rosen H. (2012) Optimization and Characterization of an Antagonist for G-Protein Coupled Receptor 7 (GPR7). Probe Reports from the NIH Molecular Libraries Program [Internet]. Bethesda (MD): National Center for Biotechnology Information (US); 2010-.2010 Oct 13 [updated 2011 Nov 21]. PMID: 22834040
  32. Tsuboi K, Bachovchin DA, Speers AE, Brown SJ, Spicer T, Fernandez-Vega V, Ferguson J, Cravatt BF, Hodder P, Rosen H. (2012) Optimization and Characterization of an Inhibitor for Glutathione S-Tranferase Omega 1 (GSTO1). Probe Reports from the NIH Molecular Libraries Program [Internet]. Bethesda (MD): National Center for Biotechnology Information (US); 2010-.2010 Aug 31 [updated 2011 Dec 12].PMID: 22834034
  33. Guerrero M, Urbano M, Velaparthi S, Zhao J, Schaeffer MT, Brown SJ, Crisp M, Ferguson J, Roberts E, Oldstone M, Hodder P, Rosen H. (2012) Probe Development Efforts to Identify Novel Agonists of the Sphingosine 1-phosphate Receptor 4 (S1P4). Probe Reports from the NIH Molecular Libraries Program [Internet]. Bethesda (MD): National Center for Biotechnology Information (US); 2010-.2010 Oct 12 [updated 2011 Dec 12]. PMID: 22834032
  34. Adibekian A, Martin BR, Chang JW, Hsu KL, Tsuboi K, Bachovchin DA, Speers AE, Brown SJ, Spicer T, Fernandez-Vega V, Ferguson J, Hodder PS, Rosen H, Cravatt BF. (2012) Confirming target engagement for reversible inhibitors in vivo by kinetically tuned activity-based probes. J Am Chem Soc. 2012 Jun 27;134(25):10345-8. Epub 2012 Jun 12. PMID: 22690931
  35. Dillon MB, Bachovchin DA, Brown SJ, Finn MG, Rosen H, Cravatt BF, Mowen KA. (2012) Novel inhibitors for PRMT1 discovered by high-throughput screening using activity-based fluorescence polarization. ACS Chem Biol. 2012 Jul 20;7(7):1198-204. Epub 2012 Apr 20. PMID: 22506763
  36. Sarkisyan G, Cahalan S, Gonzalez-Cabrera P, Leaf N, Rosen H. (2012)  Real-time differential labeling of blood, interstitium and lymphatic and single-field analysis of vasculature dynamics in vivo.  Am J Physiol Cell Physiol. 302(10):C1460-8. PMID: 22357735
  37. Hanson M, Roth C, Jo E, et al. (2012) Crystal Structure of a Lipid G-protein Coupled Receptor. Science 335(6070):851-5.  PMID: 22344443
  38. Gonzalez-Cabrera PJ, Cahalan SM, Nguyen N, Sarkisyan G, Leaf NB, Cameron MD, Kago T, Rosen H. (2012) S1P(1) receptor modulation with cyclical recovery from lymphopenia ameliorates mouse model of multiple sclerosis. Mol. Pharmacol. 2012 Feb; 81(2);166-74. PMID:22031473; PMCID: PMC3263953
  39. Guerrero M, Urbano M, Zhao J, et al. Discovery, design and synthesis of novel potent and selective sphingosine-1-phosphate 4 receptor (S1P(4)-R) agonists. Bioorg Med Chem Lett. 2012 Jan 1;22(1):537-42.
  40. Walsh KB, Teijaro JR, Wilker PR, et al. Suppression of cytokine storm with a sphingosine analog provides protection against pathogenic influenza virus. Proc Natl Acad Sci U S A. 2011 Jul 19;108(29):12018-23.
  41. Urbano M., M. Guerrero, J. Zhao, S. Velaparthi, M. T. Schaeffer, S. Brown, H. Rosen and E. Roberts (2011) SAR analysis of innovative selective small molecule antagonists of sphingosine-1-phosphate 4 (S1P) receptor. Bioorg Med Chem Lett. 21(18):5470-4
  42. Urbano M, Guerrero M, Velaparthi S, Crisp M, Chase P, Hodder P, Schaeffer MT, Brown S, Rosen H, Roberts E. (2011) Discovery, synthesis and SAR analysis of novel selective small molecule S1P(4)-R agonists based on a (2Z,5Z)-5-((pyrrol-3-yl)methylene)-3-alkyl-2-(alkylimino)thiazolidin-4-one chemotype. Bioorg Med Chem Lett. 2011 Sep 20. [Epub ahead of print] PMID: 21982495
  43. Walsh KB, Teijaro JR, Rosen H, Oldstone MB. (2011) Quelling the storm: utilization of sphingosine-1-phosphate receptor signaling to ameliorate influenza virus-induced cytokine storm. Immunol Res. 2011 Oct;51(1):15-25.PMID: 21901448
  44. Tsuboi K, Bachovchin DA, Speers AE, Spicer TP, Fernandez-Vega V, Hodder P, Rosen H, Cravatt BF. (2011) Potent and selective inhibitors of glutathione s-transferase omega 1 that impair cancer drug resistance. J Am Chem Soc. 2011 Oct 19;133(41):16605-16. Epub 2011 Sep 27. PMID: 21899313
  45. Teijaro JR, Walsh KB, Cahalan S, Fremgen DM, Roberts E, Scott F, Martinborough E, Peach R, Oldstone MB, Rosen H. (2011) Endothelial Cells Are Central Orchestrators of Cytokine Amplification during Influenza Virus Infection.Cell. 2011 Sep 16;146(6):980-91.PMID: 21925319; PMCID: PMC3176439
  46. Rillahan CD, Brown SJ, Register AC, Rosen H, Paulson JC. High-throughput screening for inhibitors of sialyl- and fucosyltransferases. Angew Chem Int Ed Engl. 2011 Dec 23;50(52):12534-7.
  47. Urbano M, Guerrero M, Zhao J, Velaparthi S, Schaeffer MT, Brown S, Rosen H, Roberts E. (2011) SAR analysis of innovative selective small molecule antagonists of sphingosine-1-phosphate 4 (S1P(4)) receptor. Bioorg Med Chem Lett. 2011 Sep 15;21(18):5470-4. Epub 2011 Jul 13.PMID: 21783362
  48. Walsh KB, Teijaro JR, Wilker PR, Jatzek A, Fremgen DM, Das SC, Watanabe T, Hatta M, Shinya K, Suresh M, Kawaoka Y, Rosen H, Oldstone MB. (2011) Suppression of cytokine storm with a sphingosine analog provides protection against pathogenic influenza virus. Proc Natl Acad Sci U S A. 2011 Jul 19;108(29):12018-23. Epub 2011 Jun 29.PMID: 21715659
  49. Lone AM, Bachovchin DA, Westwood DB, Speers AE, Spicer TP, Fernandez-Vega V, Chase P, Hodder PS, Rosen H, Cravatt BF, Saghatelian A. (2011) A Substrate-Free Activity-Based Protein Profiling Screen for the Discovery of Selective PREPL Inhibitors. J Am Chem Soc. 2011 Aug 3;133(30):11665-74. Epub 2011 Jul 12.PMID: 21692504
  50. Bachovchin DA, Zuhl AM, Speers AE, Wolfe MR, Weerapana E, Brown SJ, Rosen H, Cravatt BF. (2011) Discovery and optimization of sulfonyl acrylonitriles as selective, covalent inhibitors of protein phosphatase methylesterase-1. J Med Chem. 2011 Jul 28;54(14):5229-36. Epub 2011 Jun 30.PMID: 21639134
  51. Guerrero M, Urbano M, Velaparthi S, Zhao J, Schaeffer MT, Brown S, Rosen H, Roberts E. (2011) Discovery, design and synthesis of the first reported potent and selective sphingosine-1-phosphate 4 (S1P4) receptor antagonists.  Bioorg Med Chem Lett. 2011 Jun 15;21(12):3632-6. Epub 2011 Apr 28.PMID: 21570287
  52. Cahalan SM, Gonzalez-Cabrera PJ, Sarkisyan G, Nguyen N, Schaeffer MT, Huang L, Yeager A, Clemons B, Scott F, Rosen H. (2011) Actions of a picomolar short-acting S1P₁ agonist in S1P₁-eGFP knock-in mice. Nat Chem Biol. 2011 May;7(5):254-6. Epub 2011 Mar 27.PMID: 21445057; PMCID: PMC3430385
  53. Bachovchin DA, Mohr JT, Speers AE, Wang C, Berlin JM, Spicer TP, Fernandez-Vega V, Chase P, Hodder PS, Schürer SC, Nomura DK, Rosen H, Fu GC, Cravatt BF. (2011) Academic cross-fertilization by public screening yields a remarkable class of protein phosphatase methylesterase-1 inhibitors. Proc Natl Acad Sci U S A. 2011 Apr 26;108(17):6811-6. Epub 2011 Mar 11.PMID: 21398589
  54. Chou TF, Brown SJ, Minond D, Nordin BE, Li K, Jones AC, Chase P, Porubsky PR, Stoltz BM, Schoenen FJ, Patricelli MP, Hodder P, Rosen H, Deshaies RJ. (2011) Reversible inhibitor of p97, DBeQ, impairs both ubiquitin-dependent and autophagic protein clearance pathways.Proc Natl Acad Sci U S A. 2011 Mar 22;108(12):4834-9. Epub 2011 Mar 7.PMID: 21383145
  55. Marsolais D, Yagi S, Kago T, Leaf N, Rosen H. (2011) Modulation of chemokines and allergic airway inflammation by selective local S1P1 agonism in lung.  Mol Pharmacol. 79(1):61-8. PMID: 20935081
  56. Knuckley B, Jones JE, Bachovchin DA, Slack J, Causey CP, Brown SJ, Rosen H, Cravatt BF, Thompson PR. (2010) A fluopol-ABPP HTS assay to identify PAD inhibitors. Chem Commun (Camb). 46(38):7175-7. PMID: 20740228
  57. Gianni D, Taulet N, Zhang H, Dermardirossian C, Kister J, Martinez L, Roush WR, Brown SJ, Bokoch GM, Rosen H. (2010) A Novel and Specific NADPH Oxidase-1 (Nox1) Small-Molecule Inhibitor Blocks the Formation of Functional Invadopodia in Human Colon Cancer Cells. ACS Chem Biol. 5(10):981-93. PMID: 20715845
  58. Bachovchin DA, Wolfe MR, Masuda K, Brown SJ, Spicer TP, Fernandez-Vega V, Chase P, Hodder PS, Rosen H, Cravatt BF. (2010) Oxime esters as selective, covalent inhibitors of the serine hydrolase retinoblastoma-binding protein 9 (RBBP9). Bioorg Med Chem Lett. 20(7):2254-8. Epub 2010 Feb 6. PMID: 20207142
  59. Walsh KB, Marsolais D, Welch MJ, Rosen H, Oldstone MB. (2010) Treatment with a sphingosine analog does not alter the outcome of a persistent virus infection. Virology. 2010 Feb 20;397(2):260-9. Epub 2009 Dec 3. PMID: 19962171
  60. Bachovchin DA, Brown SJ, Rosen H, Cravatt BF. (2009) Identification of selective inhibitors of uncharacterized enzymes by high-throughput screening with fluorescent activity-based probes. Nat Biotechnol. 27(4):387-94.  PMID: 19329999
  61. Fazilleau N, McHeyzer-Williams LJ, Rosen H, McHeyzer-Williams MG.  (2009) The function of follicular helper T cells is regulated by the strength of T cell antigen receptor binding.  Nature Immunology 10(4):375-84  PMID: 19252493
  62. Avni, D., M. Goldsmith, O. Ernst, R. Mashiach, T. Tuntland, M. Meijler, N. Gray, H. Rosen, and T. Zor. (2009) Modulation of TNFα, IL-10 and IL-12p40 levels by a ceramide-1-phosphate analog, PCERA-1, in vivo and ex vivo in primary macrophages. Immunol. Lett. Bachovchin, D et al (2009) Identification of selective inhibitors of uncharacterized enzymes by high-throughput screening with fluorescent activity-based probes. Nat Biotechnol 27:387-94.  PMID: 19329999
  63. Goldsmith, M., D. Avni, G. Levy-Rimler, R. Mashiach, O. Ernst, M. Levi, B. Webb, M. Meijler, N. Gray, H. Rosen, and T. Zor. (2009) A ceramide-1-phosphate analogue, PCERA-1, simultaneously suppresses tumour necrosis factor-alpha and induces interleukin-10 production in activated macrophages. Immunology 127:103-115.  PMID: 18793216
  64. Marsolais D, Hahm B, Walsh KB, Edelmann KH, McGavern D, Hatta Y, Kawaoka Y, Rosen H, Oldstone MBA. (2009) A critical role for the sphingosine analog AAL-R in dampening the cytokine response during influenza virus infection. PNAS 106(5):1560-5. PMID: 19164548
  65. Rosen H and Don A. (2009) A lipid binding domain in sphingosine kinase 2.  Biochemical and Biophysical Research Communications 380(1):87-92. PMID: 19168031
  66. Niessen F, Furlan-Freguia C, Fernández JA, Mosnier LO, Castellino FJ, Weiler H, Rosen H, Griffin JH, Ruf W (2009)  Endogenous EPCR/aPC-PAR1 Signaling prevents Inflammation-induced Vascular Leakage and Lethality.  Blood  113(12):2859-66 PMID: 19141861
  67. Nakai R, Salisbury CM, Rosen H, Cravatt BF. (2009) Ranking the selectivity of PubChem screening hits by activity-based protein profiling: MMP13 as a case study. Bioorg Med Chem 17(3):1101-8 PMID: 18364257
  68. 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 75(5):1308-18. PMID: 18708635
  69. 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. PMID: 18590333
  70. 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. PMID: 18577684
  71. Don AS, Rosen H. (2008) A fluorescent plate reader assay for ceramide kinase. Anal Biochem 375(2):265-71. PMID: 18206978
  72. 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 452(7187):654-8. PMID: 18305483
  73. Tsukada YT, Sanna MG, Rosen H, Gottlieb RA. (2007) S1P1-selective agonist SEW2871 exacerbates reperfusion arrhythmias. J Cardiovasc Pharmacol. 50(6):660-9. PMID: 18091583
  74. Lee H-K, Brown SJ, Rosen H, Tobias PS (2007) Application of β-Lactamase Enzyme Complementation to the High-Throughput Screening of Toll-Like Receptor Signaling Inhibitors. Mol Pharm 72(4):868-75.
  75. Don A, 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
  76. 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
  77. Rosen H, Sanna MG, Cahalan S, Gonzalez-Cabrera P. (2007) Tipping the gatekeeper: S1P regulation of stromal barrier function. Trends Immunol.  28(3):102-107
  78. 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
  79. 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
  80. 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
  81. Li Z, Chen W, Hale JJ, Lynch CL, Mills SG, Hajdu R, Keohane CA, Rosenbach MJ, Milligan JA, Shei GJ, Chrebet G, Parent SA, Bergstrom J, Card D, Forrest M, Quackenbush EJ, Wickham LA, Vargas H, Evans RM, Rosen H, Mandala S. (2005) Discovery of Potent 3,5-Diphenyl-1,2,4-oxadiazole Sphingosine-1-phosphate-1 (S1P1) Receptor Agonists with Exceptional Selectivity against S1P2 and S1P3.  J. Med. Chem. 48(20):6169-6173
  82. 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
  83. 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
  84. Rosen H. (2005) Chemical approaches to the lysophospholipid receptors. Prostaglandins & Other Lipid Mediators. 77(1-4):179-184
  85. 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
  86. Hale JJ, Lynch CL, Neway W, Mills SG, Hajdu R, Keohane CA, Rosenbach MJ, Milligan JA, Shei GJ, Parent SA, Chrebet G, Bergstrom J, Card D, Ferrer M, Hodder P, Strulovici B, Rosen H, Mandala S         (2004) A rational utilization of high-throughput screening affords selective, orally bioavailable 1-benzyl-3-carboxyazetidine sphingosine-1-phosphate-1 receptor agonists. J. Med. Chem. 47(27)6662-6665
  87. 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
  88. 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.
  89. 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.
  90. 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. 14(13):3501-3505
  91. 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.
  92. 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
  93. 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
  94. 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
  95. 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.
  96. Rosen, H., Sanna, G., Alfonso, C. (2003) Egress: a receptor-regulated step in lymphocyte trafficking. Imm. Rev. 195:160-177.
  97. 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.
  98. Ferrer M, Kolodin GD, Zuck P, Peltier R, Berry K, Mandala SM, Rosen H, Ota H, Ozaki S, Inglese J, Strulovici B. (2003) A fully automated S-35 GTP gamma S scintillation proximity assay for the high-throughput screening of G(i)-linked G protein-coupled receptors. Assay and Drug Development Technologies 1(2):261-273
  99. Rosen, H., Liao, J. (2003) Sphingosine 1-phosphate pathway therapeutics: a lipid ligand-receptor paradigm. Curr. Opin. Chem. Bio. 7:461-468.
  100. Xie J, 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.
  101. 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.
  102. 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
  103. 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.
  104. 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.
  105. 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.
  106. 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.
  107. 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.
  108. 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.
  109. 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.
  110. 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.
  111. 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.
  112. 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
  113. Konteatis Z, Siciliano S, VanRiper G, et al. (1994) Development of C5a receptor antagonists: differential loss of functional responses. J. Immunol. 153:4200-5.
  114. 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.
  115. 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.
  116. 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
  117. 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.
  118. 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.
  119. 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.
  120. 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.
  121. 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
  122. 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
  123. 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.
  124. 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.
  125. 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.
  126. 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.
  127. 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.
  128. 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.
  129. 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.
  130. 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.
  131. 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.
  132. 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.
  133. 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.
  134. 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.
  135. 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.
  136. 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.
  137. 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.

Invited reviews and chapters

  1. Schreiber SL, Kotz JD, Li M, Aubé J, Austin CP, Reed JC, Rosen H, White EL, Sklar LA, Lindsley CW, Alexander BR, Bittker JA, Clemons PA, de Souza A, Foley MA, Palmer M, Shamji AF, Wawer MJ, McManus O, Wu M, Zou B, Yu H, Golden JE, Schoenen FJ, Simeonov A, Jadhav A, Jackson MR, Pinkerton AB, Chung TD, Griffin PR, Cravatt BF, Hodder PS, Roush WR, Roberts E, Chung DH, Jonsson CB, Noah JW, Severson WE, Ananthan S, Edwards B, Oprea TI, Conn PJ, Hopkins CR, Wood MR, Stauffer SR, Emmitte KA; NIH Molecular Libraries Project Team. (2015) Advancing Biological Understanding and Therapeutics Discovery with Small-Molecule Probes. Cell. 2015 Jun 4;161(6):1252-65. doi: 10.1016/j.cell.2015.05.023. Review.PMID: 26046436
  2. Gonzalez-Cabrera PJ, Brown S, Studer SM, Rosen H. (2014) S1P signaling: new therapies and opportunities. F1000 Prime Rep. 2014 Dec 1;6:109. doi: 10.12703/P6-109. eCollection 2014. Review. PMID: 25580263 [PubMed]
  3. Oldstone MB, Rosen H. Cytokine Storm Plays a Direct Role in the Morbidity and Mortality from Influenza Virus Infection and is Chemically Treatable with a Single Sphingosine-1-Phosphate Agonist Molecule. Curr Top Microbiol Immunol. 2014;378:129-47. doi: 10.1007/978-3-319-05879-5_6. PMID: 24728596
  4. Rosen H, Germana Sanna M, Gonzalez-Cabrera PJ, Roberts E. The organization of the sphingosine 1-phosphate signaling system. Curr Top Microbiol Immunol. 2014;378:1-21. doi: 10.1007/978-3-319-05879-5_1.  PMID: 24728591
  5. Urbano M, Guerrero M, Rosen H, Roberts E. Antagonists of the kappa opioid receptor. Bioorg Med Chem Lett. 2014 May 1;24(9):2021-32. doi: 10.1016/j.bmcl.2014.03.040. Epub 2014 Mar 24. PMID: 24690494
  6. Roberts E, Guerrero M, Urbano M, Rosen H. (2013) Sphingosine 1-phosphate receptor agonists: a patent review (2010-2012). Expert Opin Ther Pat. 2013 Jul;23(7):817-41. doi: 10.1517/13543776.2013.783022. Epub 2013 Apr 1.  PMID: 23541049 [PubMed - in process]
  7. Rosen H, Stevens RC, Hanson M, Roberts E, Oldstone MB. (2013) Sphingosine-1-phosphate and its receptors: structure, signaling, and influence. Annu Rev Biochem. 2013;82:637-62. doi: 10.1146/annurev-biochem-062411-130916. Epub 2013 Mar 18.  PMID: 23527695 [PubMed - in process]
  8. Gentry PR, Bridges TM, Daniels JS, Lamsal A, Vinson PN, Niswender CM, Hodder PS, Rosen H, Conn PJ, Engers J, Lindsley CW, Wood MR.(2012)Development and characterization of a highly selective M5 PAM probe molecule with improved potency.Probe Reports from the NIH Molecular Libraries Program [Internet]. Bethesda (MD): National Center for Biotechnology Information (US); 2010-2012 Dec 13 [updated 2013 Mar 22]. PMID: 23885365 [PubMed]
  9. Pinello C, Guerrero M, Eberhart C, Volmar CH, Saldanha SA, Cayanan C, Urbano M, Brown SJ, Ferguson J, Gomes I, Devi LA, Roberts E, Hodder P, Rosen H. (2012) Characterization of an agonist probe for opioid receptor mu 1 (OPRM1)-opioid receptor delta 1 (OPRD1) heterodimerization. Probe Reports from the NIH Molecular Libraries Program [Internet]. Bethesda (MD): National Center for Biotechnology Information (US); 2010-2012 Dec 17 [updated 2013 Apr 5]. PMID: 23833799 [PubMed]
  10. Zuhl AM, Mohr JT, Speers AE, Bachovchin DA, Berlin JM, Spicer T, Fernandez-Vega V, Brown SJ, Ferguson J, Fu GC, Cravatt BF, Hodder P, Rosen H. (2012) Probe Development Efforts to Identify Novel Inhibitors of ABHD10. Probe Reports from the NIH Molecular Libraries Program [Internet]. Bethesda (MD): National Center for Biotechnology Information (US); 2010-2011 Dec 6 [updated 2013 Mar 7]. PMID: 23762952 [PubMed]
  11. Guerrero M, Urbano M, Wang Z, Zhao J, Velaparthi S, Schaeffer MT, Brown SJ, Saldanha SA, Chase P, Ferguson J, Hodder P, Rosen H, Civelli O, Roberts E. (2012) Optimization and Characterization of a Second Antagonist for G-protein Coupled Receptor 7 (GPR7). Probe Reports from the NIH Molecular Libraries Program [Internet]. Bethesda (MD): National Center for Biotechnology Information (US); 2010-.  PMID: 23762933 [PubMed]
  12. Guerrero M, Urbano M, Velaparthi S, Schaeffer MT, Brown SJ, Crisp M, Ferguson J, Hodder P, Rosen H, Oldstone M, Roberts E. (2012) Identification of a Novel Agonist of the Sphingosine 1-phosphate Receptor 4 (S1P4). Probe Reports from the NIH Molecular Libraries Program [Internet]. Bethesda (MD): National Center for Biotechnology Information (US); 2010-.  PMID: 23762926 [PubMed]
  13. Guerrero M, Poddutoori R, Pinacho-Crisostomo F, Schaeffer MT, Brown SJ, Spicer T, Chase P, Ferguson J, Roberts E, Sanna G, Hodder P, Rosen H. (2012) Probe Development Efforts for an Allosteric Agonist of the Sphingosine 1-phosphate Receptor 3 (S1P3). Probe Reports from the NIH Molecular Libraries Program [Internet]. Bethesda (MD): National Center for Biotechnology Information (US); 2010-2011 Aug 31 [updated 2013 Feb 25]. PMID: 23658964 [PubMed]
  14. Cahalan, S, Rosen, H (2009) S1P1 signaling just keeps going and going and going… Nature Chem. Biol. 5(6):377-8)
  15. Marsolais D, Rosen H (2009) Chemical modulators of S1P receptors as barrier-oriented therapeutic molecules. Nature Rev Drug Disc. 8(4):297-307 PMID: 19300460
  16. Rosen H, Gonzalez-Cabrera PJ, Sanna MG, Brown S. 2009 Sphingosine 1-phosphate receptor signaling. Annu Rev Biochem. 78:743-68  PMID: 19231986
  17. 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. PMID: 18613839
  18. Chun J, Rosen H. (2006) Lysophospholipid receptors as potential drug targets in tissue transplantation and autoimmune diseases. Curr. Pharm. Des. 12(2):161-171
  19. Rosen H, Goetzl EJ. (2005) Sphingosine 1-phosphate and its receptors: an autocrine and paracrine network. Nat Rev Immunol. 5(7):560-570
  20. Rosen, H., Kozarich, JW. (2003) Balancing on the uneasy cusp: integrating linear and parallel approaches to new generation therapeutics.  Curr. Opin. Chem. Biol. 7:443.
  21. Rosen, H., Liao, J. (2003) Sphingosine 1-phosphate pathway therapeutics: a lipid receptor paradigm. Curr. Opin. Chem. Biol. 7:461.
  22. Rosen, H., Sanna, M., Alfonso, C. (2003) Egress: a receptor-regulated step in lymphocyte trafficking.  Immunol. Rev. 195:160-177.
  23. Rosen, H. (2003) The macrophage as validated pharmaceutical target. Handbook Exp. Pharm. Ed. S. Gordon. Springer, Berlin. 158:4-10.
  24. Rosen, H., D. Horn and A. Shaw. (1995) “Perspectives on the control of Tuberculosis”. Therapeutic Immunology 2:105-13.
  25. Rosen, H. and D.A. Hughes (1996). "Migration and adhesion in vivo: Myeloid cells". Hand book of Experimental Immunology, 5th Edition. Editors LA Hertzenberg and DM Weir, Blackwell Scientific Publishers, Oxford.
  26. Gordon, S., D.A.Hughes, H. Rosen, V.H. Perry and D. Wong (1994). "The role of the leukocyte integrin CR3 in macrophage migration and modulation in the mouse." International Review of Cytology
  27. Rosen,H and S.Gordon.(1992) The contribution and limitations of CR3-dependent recruitment of macrophages to inflammatory and lymphoid sites. "Mononuclear Phagocytes: Biology of Monocytes and Macrophages". Editor: R. van Furth. Kluwer Academic Publishers, Dordrecht and Boston. pp 21-30
  28. Rosen, H. (1991)  "Monocyte-endothelial interactions and their inhibition". In Research monographs on cell and tissue physiology 17: Vascular endothelium: interactions with circulating cells. Editor: JL Gordon. Elsevier, Amsterdam.pp 189-97
  29. Rosen, H. (1990). “Role of CR3 in induced myelomonocytic recruitment: insights from in vivo monoclonal antibody studies in the mouse.”J.Leuk.Biol. 48: 465-9.
  30. Rosen, H. (1990). “Cell adhesion and myelomonocytic recruitment.”Local Immun. 6: 89-102.
  31. Rosen, H. and S. Gordon (1990). “The role of the type 3 complement receptor in the induced recruitment of myelomonocytic cells to inflammatory sites in the mouse.”Am.J.Resp.Cell Molec.Biol.  3: 3-10.
  32. Rosen, H. and S. Gordon (1989). “Cell adhesion and myelomonocytic cell-endothelial interactions.”Br.J.Exp.Path. 70: 385-94.
  33. Rosen, H. and S. Law (1989). “The leukocyte cell surface receptors for the iC3b product of complement.”Curr.Top.Microbiol.Immunol. 153: 99-123.
  34. Gordon, S., V. Perry, S. Rabinowitz, L. Chung and H. Rosen (1988). “Plasma membrane receptors of the mononuclear phagocyte system.”J.Cell Sci. Suppl. 9: 1-26.

Probe Reports

  1. Gentry PR, Kokubo M, Bridges TM,      Daniels JS, Niswender CM, Smith E, Chase P, Hodder PS, Rosen H, Conn PJ,      Engers J, Brewer KA, Wood MR, Lindsley CW. Development of a Novel,      Orthosteric M5 Antagonist Possessing a High Degree of Muscarinic Subtype      Selectivity. Probe Reports from the NIH Molecular Libraries Program      [Internet]. Bethesda (MD): National Center for Biotechnology Information      (US); 2010-2013 Dec 15 [updated 2015 Feb 11]. PMID: 25834910
  2. Gentry PR, Kokubo M, Bridges TM,      Daniels JS, Niswender CM, Smith E, Chase P, Hodder PS, Rosen H, Conn PJ,      Engers J, Brewer KA, Wood MR, Lindsley CW. Development of the First      Potent, Selective and CNS penetrant M5 Negative Allosteric Modulator      (NAM). Probe Reports from the NIH Molecular Libraries Program [Internet].      Bethesda (MD): National Center for Biotechnology Information (US);      2010-2013 Dec 09 [updated 2014 Sep 18]. PMID: 25506971
  3. Mittapalli G, Argaryan L, Brown      SJ, Saldanha SA, Volmar CH, Ferguson J, Roberts E, Hodder P, Rosen H.  Optimization and characterization of an      antagonist for vasopressin 1a (V1a) receptor. Probe Reports from the NIH      Molecular Libraries Program [Internet]. Bethesda (MD): National Center for      Biotechnology Information (US); 2010-2013 Dec 11 [updated 2014 Sep 18].      PMID: 25506967
  4. Guerrero M, Urbano M, Brown SJ, Cayanan C, Ferguson J, Cameron M, Devi LA, Roberts E, Rosen H.  Optimization and characterization of an opioid kappa receptor (OPRK1) antagonist. Probe Reports from the NIH Molecular Libraries Program [Internet]. Bethesda (MD): National Center for Biotechnology Information (US); 2010-2013 Apr 15 [updated 2014 Sep 18]. PMID: 24479196
  5. Pinello C, Guerrero M, Eberhart C, Volmar CH, Saldanha SA, Cayanan C, Urbano M, Brown SJ, Ferguson J, Gomes I, Devi LA, Roberts E, Hodder P, Rosen H. Characterization of an agonist probe for opioid receptor mu 1 (OPRM1)-opioid receptor delta 1 (OPRD1) heterodimerization.  Probe Reports from the NIH Molecular Libraries Program [Internet]. Bethesda (MD): National Center for Biotechnology Information (US); 2010-2012 Dec 17 [updated 2013 Apr 5].  PMID: 23833799
  6. Gentry PR, Bridges TM, Daniels JS, Lamsal A, Vinson PN, Niswender CM, Hodder PS, Rosen H, Conn PJ, Engers J, Lindsley CW, Wood MR.  Development and characterization of a highly selective M5 PAM probe molecule with improved potency.  Probe Reports from the NIH Molecular Libraries Program [Internet]. Bethesda (MD): National Center for Biotechnology Information (US); 2010-2012 Dec 13 [updated 2013 Mar 22].  PMID: 23885365
  7. Zuhl AM, Mohr JT, Speers AE, Bachovchin DA, Berlin JM, Spicer T, Fernandez-Vega V, Brown SJ, Ferguson J, Fu GC, Cravatt BF, Hodder P, Rosen H. (2012) Probe Development Efforts to Identify Novel Inhibitors of ABHD10. Probe Reports from the NIH Molecular Libraries Program [Internet]. Bethesda (MD): National Center for Biotechnology Information (US); 2010-2011 Dec 6 [updated 2013 Mar 7]. PMID: 23762952 [PubMed]
  8. Guerrero M, Urbano M, Wang Z, Zhao J, Velaparthi S, Schaeffer MT, Brown SJ, Saldanha SA, Chase P, Ferguson J, Hodder P, Rosen H, Civelli O, Roberts E. (2012) Optimization and Characterization of a Second Antagonist for G-protein Coupled Receptor 7 (GPR7). Probe Reports from the NIH Molecular Libraries Program [Internet]. Bethesda (MD): National Center for Biotechnology Information (US); 2010-.  PMID: 23762933 [PubMed]
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