Journal of Medicinal and Pharmaceutical Chemistry, 1520-4804

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  1. 2018
  2. Elucidation of Hydrogen Bonding Patterns in Ligand-Free, Lactose- and Glycerol-Bound Galectin-3C by Neutron Crystallography to Guide Drug Design

    Manzoni, F., Johan Wallerstein, Schrader, T. E., Ostermann, A., Coates, L., Mikael Akke, Blakeley, M. P., Oksanen, E. & Derek T Logan, 2018 May 24, In : Journal of Medicinal Chemistry. 61, 10, p. 4412-4420 9 p.

    Research output: Contribution to journalArticle

  3. Systematic Tuning of Fluoro-galectin-3 Interactions Provides Thiodigalactoside Derivatives with Single-Digit nM Affinity and High Selectivity

    Peterson, K., Rohit Kumar, Olof Stenström, Verma, P., Verma, P. R., Håkansson, M., Kahl-Knutsson, B., Zetterberg, F., Hakon Leffler, Mikael Akke, Derek T. Logan & Ulf J. Nilsson, 2018 Feb 8, In : Journal of Medicinal Chemistry. 61, 3, p. 1164-1175 12 p.

    Research output: Contribution to journalArticle

  4. 2017
  5. Fragment-Based Discovery and Optimization of Enzyme Inhibitors by Docking of Commercial Chemical Space

    Rudling, A., Gustafsson, R., Almlöf, I., Homan, E., Scobie, M., Warpman Berglund, U., Helleday, T., Pål Stenmark & Carlsson, J., 2017 Oct 12, In : Journal of Medicinal Chemistry. 60, 19, p. 8160-8169

    Research output: Contribution to journalArticle

  6. 2016
  7. Active Site Mapping of an Aspartic Protease by Multiple Fragment Crystal Structures: Versatile Warheads to Address a Catalytic Dyad

    Radeva, N., Schiebel, J., Wang, X., Krimmer, S. G., Fu, K., Stieler, M., Ehrmann, F. R., Metz, A., Rickmeyer, T., Betz, M., Winquist, J., Park, A. Y., Huschmann, F. U., Weiss, M. S., Uwe Müller, Heine, A. & Klebe, G., 2016 Nov 10, In : Journal of Medicinal Chemistry. 59, 21, p. 9743-9759 17 p.

    Research output: Contribution to journalArticle

  8. A Selective Galactose-Coumarin-Derived Galectin-3 Inhibitor Demonstrates Involvement of Galectin-3-glycan Interactions in a Pulmonary Fibrosis Model

    Rajput, V. K., MacKinnon, A., Mandal, S., Collins, P., Blanchard, H., Hakon Leffler, Sethi, T., Schambye, H., Mukhopadhyay, B. & Nilsson, U. J., 2016 Sep 8, In : Journal of Medicinal Chemistry. 59, 17, p. 8141-8147 7 p.

    Research output: Contribution to journalArticle

  9. Inhibitors of the Cysteine Synthase CysM with Antibacterial Potency against Dormant Mycobacterium tuberculosis

    Brunner, K., Selma Maric, Reshma, R. S., Almqvist, H., Seashore-Ludlow, B., Gustavsson, A-L., Poyraz, Ö., Yogeeswari, P., Lundbäck, T., Vallin, M., Sriram, D., Schnell, R. & Schneider, G., 2016 Jul 28, In : Journal of Medicinal Chemistry. 59, 14, p. 6848-59 12 p.

    Research output: Contribution to journalArticle

  10. Experimental Active-Site Mapping by Fragments - Hot Spots Remote from the Catalytic Center of Endothiapepsin

    Radeva, N., Krimmer, S. G., Stieler, M., Fu, K., Wang, X., Ehrmann, F. R., Metz, A., Huschmann, F. U., Weiss, M. S., Mueller, U., Schiebel, J., Heine, A. & Klebe, G., 2016 Jul 27, In : Journal of Medicinal Chemistry.

    Research output: Contribution to journalArticle

  11. Chiral Dihydrobenzofuran Acids Show Potent Retinoid X Receptor-Nuclear Receptor Related 1 Protein Dimer Activation.

    Sundén, H., Schäfer, A., Scheepstra, M., Leysen, S., Malo, M., Ma, J-N., Burstein, E. S., Ottmann, C., Brunsveld, L. & Roger Olsson, 2016, In : Journal of Medicinal Chemistry. 59, 3, p. 1232-1238

    Research output: Contribution to journalArticle

  12. Studies on Aryl-Substituted Phenylalanines: Synthesis, Activity, and Different Binding Modes at AMPA Receptors

    Szymanska, E., Frydenvang, K. A., Pickering, D. S., Christian Krintel, Nielsen, A-B., Kooshki, A., Zachariassen, L. G., Olsen, L., Kastrup, J. S. J. & Johansen, T. N., 2016, In : Journal of Medicinal Chemistry. 59, 1, p. 448-461

    Research output: Contribution to journalArticle

  13. 2015
  14. Disubstituted Bis-THF Moieties as New P2 Ligands in Nonpeptidal HIV-1 Protease Inhibitors (II)

    Hohlfeld, K., Wegner, J. K., Kesteleyn, B., Linclau, B. & Johan Unge, 2015, In : Journal of Medicinal Chemistry. 58, 9, p. 4029-4038

    Research output: Contribution to journalArticle

  15. Synthesis and Biological Evaluation of Second-Generation Tropanol-Based Androgen Receptor Modulators

    Sunden, H., Holland, M. C., Poutiainen, P. K., Jaaskelainen, T., Pulkkinen, J. T., Palvimo, J. J. & Roger Olsson, 2015, In : Journal of Medicinal Chemistry. 58, 3, p. 1569-1574

    Research output: Contribution to journalArticle

  16. 2014
  17. Synthesis of P1 '-Functionalized Macrocyclic Transition-State Mimicking HIV-1 Protease Inhibitors Encompassing a Tertiary Alcohol

    De Rosa, M., Johan Unge, Motwani, H. V., Rosenquist, A., Vrang, L., Wallberg, H. & Larhed, M., 2014, In : Journal of Medicinal Chemistry. 57, 15, p. 6444-6457

    Research output: Contribution to journalArticle

  18. 2013
  19. Design and Synthesis of P1-P3 Macrocyclic Tertiary-Alcohol-Comprising HIV-1 Protease Inhibitors

    Joshi, A., Veron, J-B., Johan Unge, Rosenquist, A., Wallberg, H., Samuelsson, B., Hallberg, A. & Larhed, M., 2013, In : Journal of Medicinal Chemistry. 56, 22, p. 8999-9007

    Research output: Contribution to journalArticle

  20. Synthesis, pharmacological and structural characterization, and thermodynamic aspects of GluA2-positive allosteric modulators with a 3, 4-dihydro-2 H-1, 2, 4-benzothiadiazine 1, 1-dioxide scaffold

    Nørholm, A-B., Francotte, P., Olsen, L., Christian Krintel, Frydenvang, K., Goffin, E., Challal, S., Danober, L., Botez-Pop, I., Lestage, P., Pirotte, B. & Kastrup, J. S., 2013, In : Journal of Medicinal Chemistry. 56, 21, p. 8736-8745 10 p.

    Research output: Contribution to journalArticle

  21. Tuning the Preference of Thiodigalactoside- and Lactosamine-Based Ligands to Galectin-3 over Galectin-1

    van Hattum, H., Branderhorst, H. M., Moret, E. E., Ulf Nilsson, Hakon Leffler & Pieters, R. J., 2013, In : Journal of Medicinal Chemistry. 56, 3, p. 1350-1354

    Research output: Contribution to journalArticle

  22. 2012
  23. Selective mode of action of guanidine-containing non-peptides at human NPFF receptors

    Findeisen, M., Würker, C., Rathmann, D., Meier, R., Meiler, J., Roger Olsson & Beck-Sickinger, A. G., 2012 Jul 12, In : Journal of Medicinal Chemistry. 55, 13, p. 6124-6136

    Research output: Contribution to journalArticle

  24. Synthesis, X-ray Analysis, and Biological Evaluation of a New Class of Stereopure Lactam-Based HIV-1 Protease Inhibitors

    Wu, X., Ohrngren, P., Joshi, A. A., Trejos, A., Persson, M., Arvela, R. K., Wallberg, H., Vrang, L., Rosenquist, A., Samuelsson, B. B., Johan Unge & Larhed, M., 2012, In : Journal of Medicinal Chemistry. 55, 6, p. 2724-2736

    Research output: Contribution to journalArticle

  25. 2011
  26. Difluoromethylbenzoxazole Pyrimidine Thioether Derivatives: A Novel Class of Potent Non-Nucleoside HIV-1 Reverse Transcriptase Inhibitors

    Boyer, J., Arnoult, E., Medebielle, M., Guillemont, J., Johan Unge & Jochmans, D., 2011, In : Journal of Medicinal Chemistry. 54, 23, p. 7974-7985

    Research output: Contribution to journalArticle

  27. Molecular Wipes: Application to Epidemic Keratoconjuctivitis

    Aplander, K., Marttila, M., Sophie Manner, Arnberg, N., Olov Sterner & Ulf Ellervik, 2011, In : Journal of Medicinal Chemistry. 54, 19, p. 6670-6675

    Research output: Contribution to journalArticle

  28. 2009
  29. Discovery of selective nonpeptidergic neuropeptide FF2 receptor agonists

    Gaubert, G., Bertozzi, F., Kelly, N. M., Pawlas, J., Scully, A. L., Nash, N. R., Gardell, L. R., Lameh, J. & Roger Olsson, 2009 Nov 12, In : Journal of Medicinal Chemistry. 52, 21, p. 6511-6514

    Research output: Contribution to journalArticle

  30. Synthesis, structure-activity relationships, and characterization of novel nonsteroidal and selective androgen receptor modulators

    Schlienger, N., Lund, B. W., Pawlas, J., Badalassi, F., Bertozzi, F., Lewinsky, R., Fejzic, A., Thygesen, M. B., Tabatabaei, A., Bradley, S. R., Gardell, L. R., Piu, F. & Roger Olsson, 2009 Oct 26, In : Journal of Medicinal Chemistry. 52, 22, p. 7186-7191

    Research output: Contribution to journalArticle

  31. Synthesis and evaluation of dibenzothiazepines: A novel class of selective cannabinoid-1 receptor inverse agonists

    Pettersson, H., Bülow, A., Fredrik Ek, Jensen, J., Ottesen, L. K., Fejzic, A., Ma, J. N., Tredici, A. L. D., Currier, E. A., Gardell, L. R., Tabatabaei, A., Craig, D., McFarland, K., Ott, T. R., Piu, F., Burstein, E. S. & Roger Olsson, 2009 Apr 9, In : Journal of Medicinal Chemistry. 52, 7, p. 1975-1982 8 p.

    Research output: Contribution to journalArticle

  32. Design, synthesis, and structure-activity analysis of isoform-selective retinoic acid receptor β ligands

    Lund, B. W., Knapp, A. E., Piu, F., Gauthier, N. K., Begtrup, M., Hacksell, U. & Roger Olsson, 2009 Mar 26, In : Journal of Medicinal Chemistry. 52, 6, p. 1540-1545 6 p.

    Research output: Contribution to journalArticle

  33. 2008
  34. Discovery of potent and selective small-molecule PAR-2 agonists

    Seitzberg, J. G., Knapp, A. E., Lund, B. W., Bertozzi, S. M., Currier, E. A., Ma, J. N., Sherbukhin, V., Burstein, E. S. & Roger Olsson, 2008 Sep 25, In : Journal of Medicinal Chemistry. 51, 18, p. 5490-5493 4 p.

    Research output: Contribution to journalDebate/Note/Editorial

  35. Galectin-inhibitory thiodigalactoside ester derivatives have antimigratory effects in cultured lung and prostate cancer cells.

    Delaine, T., Cumpstey, I., Ingrassia, L., Le Mercier, M., Okechukwu, P., Hakon Leffler, Kiss, R. & Ulf Nilsson, 2008, In : Journal of Medicinal Chemistry. 51, 24, p. 8109-8114

    Research output: Contribution to journalArticle

  36. 2007
  37. Probing Molecular Interactions within Class II MHC A(q)/Glycopeptide/T-Cell Receptor Complexes Associated with Collagen-Induced Arthritis.

    Andersson, I., Dzhambazov, B., Holmdahl, R., Linusson, A. & Kihlberg, J., 2007, In : Journal of Medicinal Chemistry. 50, 23, p. 5627-5643

    Research output: Contribution to journalArticle

  38. Quantitative Structure-Activity Relationship of Peptides Binding to the Class II Major Histocompatibility Complex Molecule A(q) Associated with Autoimmune Arthritis.

    Holm, L., Frech, K., Dzhambazov, B., Holmdahl, R., Kihlberg, J. & Linusson, A., 2007, In : Journal of Medicinal Chemistry. 50, 9, p. 2049-2059

    Research output: Contribution to journalArticle

  39. Synthesis and transfection efficiencies of new lipophilic polyamines

    Gardner, R. A., Mattias Belting, Svensson, K. & Phanstiel, O., 2007, In : Journal of Medicinal Chemistry. 50, 2, p. 308-318

    Research output: Contribution to journalArticle

  40. 2006
  41. Novel potent and efficacious nonpeptidic urotensin II receptor agonists

    Lehmann, F., Pettersen, A., Currier, E. A., Sherbukhin, V., Roger Olsson, Hacksell, U. & Luthman, K., 2006 Apr 6, In : Journal of Medicinal Chemistry. 49, 7, p. 2232-2240 9 p.

    Research output: Contribution to journalArticle

  42. 4-quinolone derivatives: High-affinity ligands at the benzodiazepine site of brain GABA(A) receptors. synthesis, pharmacology, and pharmacophore modeling

    Lager, E., Andersson, P., Nilsson, J., Pettersson, I., Nielsen, EO., Nielsen, M., Olov Sterner & Liljefors, T., 2006, In : Journal of Medicinal Chemistry. 49, 8, p. 2526-2533

    Research output: Contribution to journalArticle

  43. Ligand affinities predicted with the MM/PBSA method: Dependence on the simulation method and the force field

    Weis, A., Katebzadeh, K., Pär Söderhjelm, Nilsson, I. & Ulf Ryde, 2006, In : Journal of Medicinal Chemistry. 49, 22, p. 6596-6606

    Research output: Contribution to journalArticle

  44. Novel selective orally active CRTH2 antagonists for allergic inflammation developed from in silico derived hits

    Ulven, T., Receveur, J-M., Grimstrup, M., Rist, O., Frimurer, T. M., Gerlach, L-O., Mathiesen, J. M., Kostenis, E., Lena Uller & Hogberg, T., 2006, In : Journal of Medicinal Chemistry. 49, 23, p. 6638-6641

    Research output: Contribution to journalArticle

  45. Prediction of activation energies for hydrogen abstraction by cytochrome P450

    Olsen, L., Rydberg, P., Rod, T. H. & Ulf Ryde, 2006, In : Journal of Medicinal Chemistry. 49, 22, p. 6489-6499

    Research output: Contribution to journalArticle

  46. Selective antiproliferative activity of hydroxynaphthyl-beta-D-xylosides

    Jacobsson, M., Ulf Ellervik, Mattias Belting & Katrin Mani, 2006, In : Journal of Medicinal Chemistry. 49, 6, p. 1932-1938

    Research output: Contribution to journalArticle

  47. 2005
  48. Light-Induced Anticancer Activity of [RuCl2(DMSO)4] Complexes

    Brindell, M., Kulis, E., Sofi Elmroth, Urbanska, K. & Stochel, G., 2005, In : Journal of Medicinal Chemistry. 48, 23, p. 7298-7304

    Research output: Contribution to journalArticle

  49. 2002
  50. Discovery of the first nonpeptide agonist of the GPR14/Urotensin-II receptor: 3-(4-Chlorophenyl)-3-(2-(dimethylamino)ethyl)isochroman-1-one (AC-7954)

    Croston, G. E., Roger Olsson, Currier, E. A., Burstein, E. S., Weiner, D., Nash, N., Severance, D., Allenmark, S. G., Thunberg, L., Ma, J. N., Mohell, N., O'Dowd, B., Brann, M. R. & Hacksell, U., 2002 Oct 9, In : Journal of Medicinal Chemistry. 45, 23, p. 4950-4953

    Research output: Contribution to journalArticle

  51. Azapeptides structurally based upon inhibitory sites of cystatins as potent and selective inhibitors of cysteine proteases

    Wieczerzak, E., Drabik, P., Lankiewicz, L., Oldziej, S., Grzonka, Z., Magnus Abrahamson, Anders Grubb & Bromme, D., 2002, In : Journal of Medicinal Chemistry. 45, 19, p. 4202-4211

    Research output: Contribution to journalArticle

  52. Methanocarba modification of uracil and adenine nucleotides: High potency of northern ring conformation at P2Y(1), P2Y(2), P2Y(4), and P2Y(11) but not P2Y(6) receptors

    Kim, HS., Ravi, RG., Marquez, VE., Maddileti, S., Anna-Karin Wihlborg, David Erlinge, Malin Malmsjö, Boyer, JL., Harden, TK. & Jacobson, KA., 2002, In : Journal of Medicinal Chemistry. 45, 1, p. 208-218

    Research output: Contribution to journalArticle

  53. Refinement and evaluation of a pharmacophore model for flavone derivatives binding to the benzodiazepine site of the GABA(A) receptor

    Kahnberg, P., Lager, E., Rosenberg, C., Schougaard, J., Camet, L., Olov Sterner, Ostergaard Nielsen, E., Nielsen, M. & Liljefors, T., 2002, In : Journal of Medicinal Chemistry. 45, 19, p. 4188-4201

    Research output: Contribution to journalArticle

  54. 2000
  55. Computational predictions of binding affinities to dihydrofolate reductase: synthesis and biological evaluation of methotrexate analogues

    Graffner-Nordberg, M., Marelius, J., Ohlsson, S., Persson, A., Swedberg, G., Andersson, P., Andersson, S., Aqvist, J. & Hallberg, A., 2000, In : Journal of Medicinal Chemistry. 43, 21, p. 3852-3861

    Research output: Contribution to journalArticle