Kirsten A, Watz H, Kretschmar G, Pedersen F, Bock D, Meyer-Sabellek W, Magnussen H.
Efficacy of the pan-selectin antagonist Bimosiamose on ozone-induced airway inflammation in healthy subjects - A double blind, randomized, placebo-controlled, cross-over clinical trial.
Pulm Pharmacol Ther. 2011 Apr 14. [
Aydt, E.M., Bock, D., Wolff, G.
Selectin antagonists and their potential impact for the treatment of inflammatory lung diseases
Hansel TT, Barnes PJ (eds): New Drugs and Targets for Asthma and COPD. Prog Respir Res. Basel, Karger 2010, vol 39, pp 175–184
Anaya-Prado R, Pérez-Gomez N, Toledo-Pereyra LH, Walsh J, Jordan J, Ward PA.
Small molecule selectin inhibitor in global cerebral ischemia and controlled hemorrhagic shock.
J Trauma. 2008 Sep;65(3):678-84
Mackay CR.
Moving targets: cell migration inhibitors as new anti-inflammatory therapies.
Nat Immunol. 2008 Sep;9(9):988-98
Meyer M, Beyer D, Vollhardt K, Woischwill C, Jilma B, Wolff G.
The pharmacokinetics of subcutaneously injected bimosiamose disodium in healthy male volunteers.
Biopharm Drug Dispos. 2007; 28(9):475-484
Mayr FB, Firbas C, Leitner JM, Spiel AO, Reiter RA, Beyer D, Meyer M, Wolff G, Jilma B.
Effects of the pan-selectin antagonist bimosiamose (TBC1269) in experimental human endotoxemia.
Shock. 2008 Apr;29(4):475-82
Calvey CR, Toledo-Pereyra LH.
Selectin inhibitors and their proposed role in ischemia and reperfusion.
J Invest Surg. 2007 Mar-Apr;20(2):71-85
Kranich R, Busemann AS, Bock D, Schroeter-Maas S, Beyer D, Heinemann B, Meyer M, Schierhorn K, Zahlten R, Wolff G, Aydt EM.
Rational Design of Novel, Potent Small Molecule Pan-Selectin Antagonists.
J Med Chem. 2007 Mar 22;50(6):1101-1115
Lopez-Neblina F, Toledo-Pereyra LH.
Anti-ischemic Effect of Selectin Blocker Through Modulation of Tumor Necrosis Factor-alpha and Interleukin-10.
J Surg Res. 2007 Apr;138(2):275-83
Meyer M, Beeh KM, Beier J, Beyer D, Aydt E, Zahlten R, Jilma B, Wolff G.
Tolerability and pharmacokinetics of inhaled bimosiamose disodium in healthy males.
Br J Clin Pharmacol. 2007; 63(4):451-458
Jayle C, Milinkevitch S, Favreau F, Doucet C, Richer JP, Deretz S, Mauco G, Rabb H, Hauet T.
Protective role of selectin ligand inhibition in a large animal model of kidney ischemia-reperfusion injury.
Kidney Int. 2006 May;69(10):1749-55
Bock D, Aydt EM, Kuebler, WM, Wolff G.
The Role of Selectins During Lung Inflammation and Their Potential Impact for Innovative Therapeutic Strategies
Current Respiratory Medicine Reviews 2006,2(3):339-354
Bock D, Philipp S, Wolff G.
Therapeutic potential of selectin antagonists in psoriasis.
Expert Opin Investig Drugs. 2006 Aug;15(8):963-79
Friedrich M, Bock D, Philipp S, Ludwig N, Sabat R, Wolk K, Schroeter-Maas S, Aydt E, Kang S, Dam TN, Zahlten R, Sterry W, Wolff G
Pan-selectin antagonism improves psoriasis manifestation in mice and man.
Arch Dermatol Res. 2006 Feb;297(8):345-51
Schumacher A, Liebers U, John M, Gerl V, Meyer M, Witt C, Wolff G.
P-selectin glycoprotein ligand-1 (PSGL-1) is up-regulated on leucocytes from patients with chronic obstructive pulmonary disease.
Clin Exp Immunol. 2005 Nov;142(2):370-6
Michail S, Mezoff E, Abernathy F.
Role of selectins in the intestinal epithelial migration of eosinophils.
Pediatr Res. 2005 Oct;58(4):644-7
Meyer M, Jilma B, Zahlten R, Wolff G.
Physiochemical properties, safety and pharmacokinetics of bimosiamose disodium after intravenous administration.
Int J Clin Pharmacol Ther. 2005 Oct;43(10):463-71
Ulbrich H, Prech P, Luxenburger A, Dannhardt G.
Characterization of a computerized assay for rapid and easy determination of leukocyte adhesion to endothelial cells.
Biol Pharm Bull. 2005 Apr;28(4):718-24
Beeh KM, Beier J, Meyer M, Buhl R, Zahlten R, Wolff G.
Bimosiamose, an inhaled small-molecule pan-selectin antagonist, attenuates late asthmatic reactions following allergen challenge in mild asthmatics: A randomized, double-blind, placebo-controlled clinical cross-over-trial.
Pulm Pharmacol Ther 2006; 19(4):233-41
Beauharnois ME, Lindquist KC, Marathe D, Vanderslice P, Xia J, Matta KL, Neelamegham S.
Affinity and kinetics of sialyl Lewis-X and core-2 based oligosaccharides binding to L- and P-selectin.
Biochemistry. 2005 Jul 12;44(27):9507-19
Hicks AE, Abbitt KB, Dodd P, Ridger VC, Hellewell PG, Norman KE.
The anti-inflammatory effects of a selectin ligand mimetic, TBC-1269, are not a result of competitive inhibition of leukocyte rolling in vivo.
J Leukoc Biol. 2005 Jan;77(1):59-66
Toledo-Pereyra LH, Lopez-Neblina F, Reuben JS, Toledo AH, Ward PA.
Selectin inhibition modulates Akt/MAPK signaling and chemokine expression after liver ischemia-reperfusion.
J Invest Surg. 2004 Nov-Dec;17(6):303-13
Langer R, Wang M, Stepkowski SM, Hancock WW, Han R, Li P, Feng L, Kirken RA, Berens KL, Dupre B, Podder H, Dixon RA, Kahan BD.
Selectin inhibitor bimosiamose prolongs survival of kidney allografts by reduction in intragraft production of cytokines and chemokines.
J Am Soc Nephrol. 2004 Nov;15(11):2893-901
Green CE, Pearson DN, Camphausen RT, Staunton DE, Simon SI.
Shear-dependent capping of L-selectin and P-selectin glycoprotein ligand 1 by E-selectin signals activation of high-avidity beta2-integrin on neutrophils.
J Immunol. 2004 Jun 15;172(12):7780-90
Avila PC, Boushey HA, Wong H, Grundland H, Liu J, Fahy JV
Effect of a single dose of the selectin inhibitor TBC1269 on early and late asthmatic responses.
Clin Exp Allergy. 2004 Jan;34(1):77-84
Vanderslice P, Biediger RJ, Woodside DG, Berens KL, Holland GW, Dixon RA.
Development of cell adhesion molecule antagonists as therapeutics for asthma and COPD.
Pulm Pharmacol Ther. 2004;17(1):1-10. Review
Onai Y, Suzuki J, Nishiwaki Y, Gotoh R, Berens K, Dixon R, Yoshida M, Ito H, Isobe M. Blockade of cell adhesion by a small molecule selectin antagonist attenuates myocardial ischemia/reperfusion injury.
Eur J Pharmacol. 2003 Nov 28;481(2-3):217-25
Donnelly LE, Rogers DF.
Therapy for chronic obstructive pulmonary disease in the 21st century.
Drugs. 2003;63(19):1973-98. Review.
Bayes M, Rabasseda X, Prous JR.
Gateways to clinical trials.
Methods Find Exp Clin Pharmacol. 2003 Jun;25(5):387-408.
Aydt E, Wolff G.
Development of synthetic pan-selectin antagonists: a new treatment strategy for chronic inflammation in asthma.
Pathobiology. 2002-2003;70(5):297-301. Review.
Malhotra R, Ward M, Bright H, Priest R, Foster MR, Hurle M, Blair E, Bird M
Isolation and characterisation of potential respiratory syncytial virus receptor(s) on epithelial cells.
Microbes Infect. 2003 Feb;5(2):123-33.
Radi ZA, Brogden KA, Dixon RA, Gallup JM, Ackermann MR.
A selectin inhibitor decreases neutrophil infiltration during acute Mannheimia haemolytica pneumonia.
Vet Pathol. 2002 Nov;39(6):697-705.
Anaya-Prado R, Ramos-Kelly JR, Toledo-Pereyra LH, Walsh J, Ward PA.
Multiple selectin blockade with a small-molecule selectin inhibitor does not affect survival after a second inflammatory challenge with nonlethal LPS.
J Invest Surg. 2002 May-Jun;15(3):171-80.
Romano SJ, Slee DH.
Targeting selectins for the treatment of respiratory diseases.
Curr Opin Investig Drugs. 2001 Jul;2(7):907-13.
Nemoto T, Burne MJ, Daniels F, O'Donnell MP, Crosson J, Berens K, Issekutz A, Kasiske BL, Keane WF, Rabb H.
Small molecule selectin ligand inhibition improves outcome in ischemic
Sauer HH, Allen SJ, Cox Jr CS Jr, Laine GA.
Effect of sialyl Lewis(x) selectin blockade on myocardial protection during cardioplegic arrest and reperfusion.
Heart Surg Forum. 2001;4(3):216-22.
Caverly JM, Radi ZA, Andreasen CB, Dixon RA, Brogden KA, Ackermann MR.
Comparison of bronchoalveolar lavage fluid obtained from Mannheimia haemolytica-inoculated calves with and without prior treatment with the selectin inhibitor TBC1269.
m J Vet Res. 2001 May;62(5):665-72.
Radi ZA, Caverly JM, Dixon RA, Brogden KA, Ackermann MR.
Effects of the synthetic selectin inhibitor TBC1269 on tissue damage during acute Mannheimia haemolytica-induced pneumonia in neonatal calves.
Am J Vet Res. 2001 Jan;62(1):17-22.
Ramos-Kelly JR, Toledo-Pereyra LH, Jordan J, Rivera-Chavez F, Rohs T, Holevar M, Dixon RA, Yun E, Ward PA.
Multiple selectin blockade with a small molecule inhibitor downregulates liver chemokine expression and neutrophil infiltration after hemorrhagic shock
J Trauma. 2000 Jul;49(1):92-100.
Ramirez-Romero R, Brogden KA, Gallup JM, Dixon RA, Ackermann MR.
Reduction of pulmonary mast cells in areas of acute inflammation in calves with Mannheimia (Pasteurella) haemolytica pneumonia.
J Comp Pathol. 2000 Jul;123(1):29-35.
Cox CS Jr, Allen SJ, Sauer H, Frederick J.
Effects of selectin-sialyl Lewis blockade on mesenteric microvascular permeability associated with cardiopulmonary bypass.
J Thorac Cardiovasc Surg. 2000 Jun;119(6):1255-61.
Davenpeck KL, Berens KL, Dixon RA, Dupre B, Bochner BS.
Inhibition of adhesion of human neutrophils and eosinophils to P-selectin by the sialyl Lewis antagonist TBC1269: preferential activity against neutrophil adhesion in vitro.
J Allergy Clin Immunol. 2000 Apr;105(4):769-75.
Ramos-Kelly JR, Toledo-Pereyra LH, Jordan JA, Rivera-Chavez FA, Dixon RA, Ward PA. Upregulation of lung chemokines associated with hemorrhage is reversed with a small molecule multiple selectin inhibitor.
J Am Coll Surg. 1999 Dec;189(6):546-53.
Abraham WM, Ahmed A, Sabater JR, Lauredo IT, Botvinnikova Y, Bjercke RJ, Hu X, Revelle BM, Kogan TP, Scott IL, Dixon RA, Yeh ET, Beck PJ
Selectin blockade prevents antigen-induced late bronchial responses and airway hyperresponsiveness in allergic sheep.
Am J Respir Crit Care Med. 1999 Apr;159(4 Pt 1):1205-14.
Kogan TP, Dupre B, Bui H, McAbee KL, Kassir JM, Scott IL, Hu X, Vanderslice P, Beck PJ, Dixon RA.
Novel synthetic inhibitors of selectin-mediated cell adhesion: synthesis of 1,6-bis[3-(3-carboxymethylphenyl)-4-(2-alpha-D-mannopyranosyloxy)phenyl]hexane (TBC1269).
J Med Chem. 1998 Mar 26;41(7):1099-111.
Keller VA, Pigott JD, Flint LM, Hart KK, Lefer DJ, Ferrara JJ.
Age-related differences in response to neutrophil-mediated reperfusion injury in the neonatal piglet heart.
Surgery. 1998 Mar;123(3):294-304.
Palma-Vargas JM, Toledo-Pereyra L, Dean RE, Harkema JM, Dixon RA, Kogan TP.
Small-molecule selectin inhibitor protects against liver inflammatory response after ischemia and reperfusion.
J Am Coll Surg. 1997 Oct;185(4):365-72