833
Views
72
CrossRef citations to date
0
Altmetric
Reviews

Neutrophil elastase inhibitors

, &
Pages 339-354 | Published online: 16 Jan 2011

Bibliography

  • Calverley PM, Walker P. Chronic obstructive pulmonary disease. Lancet 2003;362:1053-61
  • Punturieria A, Croxton TL, Weinmann G, Kiley JP. The changing face of COPD. Am Fam Physician 2007;75:315-6
  • Stockley RA, Mannino D, Barnes PJ. Burden and pathogenesis of chronic obstructive pulmonary disease. Proc Am Thorac Soc 2009;6:524-6
  • Punturieria A, Croxton TL, Weinmann G, Kiley JP. Chronic obstructive pulmonary disease. Am J Respir Crit Care Med 2008;178:441-3
  • Seifert S, Vogelmeier C. Emerging drugs in chronic obstructive pulmonary disease. Expert Opin Emerg Drugs 2009;14:181-94
  • Barnes PJ. New therapies for chronic obstructive pulmonary disease. Med Princ Pract 2010;19:330-8
  • Ohbayashi H. Neutrophil elastase inhibitors as treatment for COPD. Expert Opin Investig Drugs 2002;11:965-80
  • Malhotra S, Paul Man SF, Sin DD. Emerging drugs for the treatment of chronic obstructive pulmonary disease. Expert Opin Emerg Drugs 2006;11:275-91
  • Kelly E, Greene CM, McElvaney NG. Targeting neutrophil elastase in cystic fibrosis. Expert Opin Ther Targets 2008;12:145-57
  • Sussan TE, Rangasamy T, Blake DJ, Targeting Nrf2 with the triterpenoid CDDO-imidazolide attenuates cigarette smoke-induced emphysema and cardiac dysfunction in mice. Proc Natl Acad Sci USA 2009;106:250-5
  • Brinkmann V, Reichard U, Goosmann C, Neutrophil extracellular traps kill bacteria. Science 2004;303:1532-5
  • Reeves AP, Lu H, Jacobs HL, Killing activity of neutrophils is mediated through the activation of proteases by K+ flux. Nature 2002;416:291-6
  • Ganz T. Defensins: antimicrobial peptides of innate immunity. Nat Rev Immunol 2003;3:710-20
  • Hager M, Cowland JB, Borregaard N. Neutrophil granules in health and disease. J Intern Med 2010;268:25-34
  • Malech HL, Gallin JI. Neutrophils in human diseases. N Engl J Med 1987;320:365-76
  • Quinn DJ, Weldon S, Taggart CC. Antiproteases as therapeutics to target inflammation in cystic fibrosis. Open Respir Med J 2010;30:20-31
  • Voynow JA, Fischer BM, Zheng S. Proteases and cystic fibrosis. Int J Biochem Cell Biol 2008;40:1238-45
  • Moraes TJ, Zurawska JH, Downey GP. Neutrophil granule contents in the pathogenesis of lung injury. Curr Opin Hematol 2006;13:21-7
  • Houghton AM, Rzymkiewicz DM, Ji H, Neutrophil elastase-mediated degration of IRS-1- accelerates lung tumor growth. Nat Med 2010;16:219-23
  • Kim S, Nadel JA. Role of neutrophils in mucous hypersecretion in COPD and implications for therapy. Trends Respir Med 2004;3:147-59
  • Witko-Sarsat V, Halbwachs-Mecarelli L, Schuster A, Proteinase 3, a potent secretagogue in airways, is present in cystic fibrosis sputum. Am J Respir Cell Mol Biol 1999;20:729-36
  • Abrahamson DR, Irbin MH, Blackburn WD, Heck LW. Degradation of basement laminin by human neutrophil elastase. Am J Pathol 1990;136:1267-74
  • Kafienah W, Buttle D, Burnett D, Hollander AP. Cleavage of native type I collagen by human neutrophil elastase. Biochem J 1998;330:897-902
  • Janucz MJ, Doherty NS. Degradation of matrix proteoglycan by human neutrophils involves both elastase and cathepsin G. J Immunol 1991;146:3922-8
  • Rubio F, Accurso FJ, Remold-O'Donnell E. Linkage of neutrophil serine proteases and decreased surfactant protein-A (SP-A) levels in inflammatory lung disease. Thorax 2004;59:318-23
  • Shapiro SD. The macrophage in chronic obstructive pulmonary disease. Am J Respir Crit Care Med 1999;160:S29-32
  • Palmgren MS, de Shazo RD, Carter RM, Mechanisms of neutrophil damage to human alveolar extracellular matrix: the role of serine and metalloproteases. J Allergy Clin Immunol 1992;89:905-15
  • Chapman HA, Shi G-P. Protease injury in the development of COPD. Chest 2000;117:S295-8
  • Ohnishi K, Tagaki M, Kurokawa Y, Matrix metalloproteinase-mediated extracellular matrix protein degradation in human pulmonary emphysema. Lab Invest 1998;78:1077-87
  • Finkelstein R, Fraser RS, Ghezzo H, Cosio MG. Alveolar inflammation and its relation to emphysema in smokers. Am J Respir Crit Care Med 1998;152:1666-72
  • Saetta M, DiStephano A, Turato G, CD8+ T lymphocytes in peripheral airways of smokers with COPD. Am J Respir Crit Care Med 1998;157:822-6
  • Ito K, Ito M, Elliott WM, Decreased histone deacetylase activity in COPD. N Engl J Med 2005;352:1967-77
  • Shapiro SD. COPD unwound. N Engl J Med 2005;352:2016-19
  • Wouters EFM. Local and systemic inflammation in chronic obstructive pulmonary disease. Proc Am Thorac Soc 2005;2:26-33
  • Rennard SI. Inflammation and repair processes in COPD. Am J Respir Crit Care Med 1999;160:S12-16
  • Harada A, Sekido N, Akahoshi T, Essential involvement of IL-8 in acute inflammation. J Leuk Biol 1994;56:559-64
  • Taub DT, Anver M, Oppenheim JJ, T lymphocyte recruitment by IL-8. J Clin Invest 1996;97:1931-41
  • Richman-Eisenstadt JB, Jorens PG, Hebert CA, Interleukin 8: an important chemoattractant in sputum of patients with COPD. Am J Physiol 1993;264:L413-18
  • Yamamoto C, Yoneda T, Yoshikawa M, Airway inflammation in COPD assessed by sputum levels of IL-8. Chest 1997;112:505-10
  • Meyer-Hoffert U. Neutrophil-derived serine proteases modulate innate immune responses. Frontiers Biosci 2009;14:3409-18
  • Pryor WA, Stone K. Oxidants in cigarette smoke. Radicals, hydrogen peroxide, peroxynitrate, and peroxynitrite. Ann NY Acad Sci 1993;686:12-27
  • Rangasamy T, Misra V, Zhen L, Cigarette-smoke-induced emphysema in A/J mice is associated with pulmonary oxidative stress, apoptosis of lung cells, and global alterations in gene expression. Am J Physiol Lung Cell Mol Physiol 2009;296:L888-900
  • Abboud RT, Vimalanathan S. Pathogenesis of COPD. The role of the protease-antiprotease imbalance in emphysema. Int J Tuberc Lung Dis 2010;12:361-7
  • Owen CA. Roles of proteinases in the pathogenesis of chronic obstructive pulmonary disease. Int J COPD 2008;3:253-68
  • Pham CT. Neutrophil serine proteases fine-tune the inflammatory response. Int J Biochem Cell Biol 2008;40:1317-33
  • Boutten A, Goven D, Boczkowski J, Bonay M. Oxidative stress targets in pulmonary emphysema: focus on the Nrf2 pathway. Expert Opin Ther Targets 2010;14:329-46
  • MacNee W. Pulmonary and systemic oxidant/antioxidant imbalance in chronic obstructive pulmonary disease. Proc Am Thorac Soc 2005;2:50-60
  • Luppi F, Hiemstra PS. Epithelial responses to oxidative stress in chronic obstructive pulmonary disease. Am J Respir Crit Care Med 2007;175:527-31
  • Tuder RM, Petrache I, Elias JA, Apoptosis and emphysema: the missing link. Am J Respir Cell Mol Biol 2003;28:551-4
  • Morissette MC, Parent J, Milot J. Alveolar epithelial and endothelial cell apoptosis in emphysema: what we know and what we need to know. Int J COPD 2009;4:19-31
  • Giordano RJ, Lahdenranta J, Zhen L, Targeted induction of lung endothelial cell apoptosis causes emphysema-like changes in the mouse. J Biol Chem 2008;283:29447-60
  • Gorska K, Maskey-Warzechowska M, Krenke R. Airway inflammation in chonic obstructive pulmonary disease. Curr Opin Pulm Med 2010;16:89-96
  • Yoshida T, Tuder RM. Pathobiology of cigarette smoke-induced chronic obstructive pulmonary disease. Physiol Rev 2007;87:1047-82
  • MacNee W, Tuder RM. New paradigms in the pathogenesis of chronic obstructive pulmonary disease I. Proc Am Thorac Soc 2009;6:527-31
  • Wright TL, Churg A. Current concepts in mechanisms of emphysema. Toxicol Pathol 2007;35:111-15
  • Churg A, Cosio M, Wright JL. Mechanisms of cigarette smoke-induced COPD: insights from animal models. Am J Physiol Lung Cell Mol Physiol 2008;294:L612-31
  • Taraseviciene-Stewart L, Voelkel NF. Molecular pathogenesis of emphysema. J Clin Invest 2008;118:394-402
  • Bode W, Meyer EF, Powers JC. Human leukocyte elastase and porcine pancreatic elastase: X-ray crystal structures, mechanism, substrate specificity, and mechanism-based inhibitors. Biochemistry 1989;28:1951-63
  • Stein RL, Strimpler AM, Ho H, Powers JC. Catalysis by human leukocyte elastase. Mechanistic insights into specificity requirements. Biochemistry 1987;26:1301-5
  • Bachovchin WW. 15N NMR spectroscopy of hydrogen-bonding interactions in the active site of serine proteases:evidence for a moving histidine mechanism. Biochemistry 1986;25:7751-9
  • Ekeowa U, Gooptu B, Belorgey D, Alpha-1-Antitrypsin deficiency, chronic obstructive pulmonary disease and the serpinopathies. Clin Sci (Lond) 2009;116:837-50
  • Silverman GA, Bird PI, Carrell W, The serpins are an expanding superfamily of structurally similar but functionally diverse proteins. Evolution, mechanism of inhibition, novel functions, and a revised nomenclature. J Biol Chem 2001;276:33293-6
  • Brew K, Nagase H. The tissue inhibitors of metalloproteinases (TIMPs): an ancient family with structural and functional diversity. Biochim Biophys Acta 2010;1803:55-71
  • Turk V, Stoka V, Turk D. Cystatins: biochemical and structural properties, and medical relevance. Front Biosci 2008;13:5406-20
  • Carrell RW, Jeppsson J-O, Laurell CB, Structure and variation of human alpha-1-antitrypsin. Nature 1982;298:329-34
  • Cooley J, Takayama TK, Shapiro SD, The serpin MN/EI inhibits elastase-like and chymotrypsin-like serine proteases through efficient reactions at two active sites. Biochemistry 2001;40:15762-70
  • Thomson RC, Ohlsson K. Isolation, properties, and complete amino acid sequence of human secretory leukocyte protease inhibitor: a potent inhibitor of leukocyte elastase. Proc Natl Acad Sci USA 1986;83:6692-6
  • Wiedow O, Schroder J-M, Gregory H, Elafin: an elastase-specific inhibitor of human skin. J Biol Chem 1990;265:14791-5
  • Wiedow O, Lidemann J, Utecht B. Elafin is a potent inhibitor of proteinase 3. Biochem Biophys Res Commun 1991;174:6-10
  • Boudier C, Bieth J. Mucous proteinase inhibitor: a fast acting inhibitor of leukocyte elastase. Biochem Biophys Acta 1989;995:36-41
  • Churg A, Wang RD, Xie C, Wright JL. alpha-1-Antitrypsin ameliorates cigarette smoke-induced emphysema in the mouse. Am J Respir Crit Care Med 2003;168:199-207
  • Taggart C, Cervantes-Laurean D, Kim G, Oxidation of either methionine 351 or methionine 358 in alpha-1-antitrypsin causes loss of anti-neutrophil elastase activity. J Biol Chem 2000;275:27258-65
  • Beatty K, Matheson N, Travis J. Kinetics and chemical evidence for the inability of oxidized alpha-1-proteinase inhibitor to protect lung elastin from elastolytic degradation. Hoppe Seylers Z Physiol Chem 1984;365:731-6
  • Li Z, Alam S, Wang J, Oxidized alpha-1-antitrypsin stimulates the release of monocyte chemotactic protein-1 from lung epithelial cells: potential role in emphysema. Am J Physiol Lung Cell Mol Physiol 2009;297:L358-400
  • Zhong J, Groutas WC. Recent developments in the design of mechanism-based and alternate substrate inhibitors of serine proteases. Curr Top Med Chem 2004;4:1203-16
  • Maryanoff BE, Constanzo MJ. Inhibitors of proteases and amide hydrolases that employ alpha-ketoheterocycles as a key enabling functionality. Bioorg Med Chem 2008;16:1562-95
  • Guarnieri F, Spencer JL, Lucey EC, A human surfactant peptide-elastase inhibitor construct as a treatment for emphysema. Proc Natl Acad Sci USA 2010;107:10661-6
  • Inoue Y, Omodani T, Shiratake R, Development of a highly water-soluble peptide-based human neutrophil elastase inhibitor: AE-3763 for treatment of acute organ injury. Bioorg Med Chem 2009;17:7477-86
  • Krantz A, Spencer RW, Tam TF, Design and synthesis of 4H-3,1-benzoxazin-4-ones as potent alternate substrate inhibitors of human leukocyte elastase. J Med Chem 1990;33:464-79
  • Neumann U, Schechter NM, Gutschow M. Inhibition of human chymase by 2-amino-3,1-benzoxazin-4-ones. Bioorg Med Chem 2001;9:947-54
  • Gutschow M, Kuerschner L, Neumann U, 2-(Diethylamino)thieno[1,3]oxazin-4-ones as stable inhibitors of human leukocyte elastase. J Med Chem 1999;42:5437-47
  • Neumann U, Gutschow M. 3,1-benzothiazin-4-ones and 3,1-benzoxazin-4-ones: highly different activities in chymotrypsin inactivation. Bioorg Med Chem 1995;23:72-88
  • Mistuhashi H, Nonaka T, Hamamura I, Pharmacological activities of TEI-8362, a novel inhibitor of human neutrophil elastase. Br J Pharmacol 2009;126:1147-52
  • Hsieh P-W, Yu H-P, Chang Y-J, Hwang TL. Synthesis and evaluation of benzoxazinone derivatives on activity of human neutrophil elastase and on hemorrhagic shock-induced lung injury in rats. Eur J Med Chem 2010;45:3111-15
  • Shreder KR, Cajica J, Du L, Synthesis and optimization of 2-pyridyl-3-yl-benzo[d][1,3]oxazin-4-one based inhibitors of human neutrophil elastase. Bioorg Med Chem Lett 2009;19:4743-6
  • Mulchande J, Oliveira R, Carrasco M, 4-Oxo-beta-lactams (Azetidine-2, 4-diones) are potent and selective inhibitors of human leukocyte elastase. J Med Chem 2010;53:241-53
  • Mulchande J, Simoes SI, Gaspar MM, Synthesis, stability, biochemical and pharmacokinetic properties of a new potent and selective 4-oxo-beta-lactam inhibitor of human leukocyte elastase. J Enz Inh Med Chem 2010: posted online on June 14, 2010, doi:10.3109/14756366.2010.486794
  • Schepetkin IA, Khlebnikov AI, Quinn MT. N-Benzoyl pyrazoles are novel small-molecule inhibitors of human neutrophil elastase. J Med Chem 2007;50:4928-38
  • Nakayama Y, Odagaki Y, Fujita S, Clarification of the mechanism of human sputum elastase inhibition by a new inhibitor, ONO-5046, using electron-spray ionization mass spectrometry. Bioorg Med Chem Lett 2002;12:2349-53
  • Hayakawa M, Ketabami K, Wada T, Silevestat (selective neutrophil elastase inhibitor) improves the mortality rate of sepsis associated with both acute respiratory distress syndrome and disseminated intravascular coagulation patients. Shock 2010;33:14-8
  • Sakashita A, Nishimura Y, Nishiuma T, Neutrophil elastase inhibitor (sivelestat) attenuates subsequent ventilator-induced lung injury in mice. Eur J Pharmacol 2007;571:62-71
  • Yoshikawa S, Tsushima K, Koizumi T, Kubo K. Effects of a synthetic protease inhibitor (gabexate mesylate) and a neutrophil elastase inhibitor (sivelestat sodium) on acid-induced lung injury in rats. Eur J Pharmacol 2010;641:220-5
  • Yang Q, Dou D, Gan X, Inhibition of serine proteases by a new class of cyclosulfamide-based carbamylating agents. Arch Biochem Biophys 2008;475:115-20
  • Li Y, Dou D, He G, Mechanism-based inhibitors of serine proteases with high selectivity through optimization of S' subsite binding. Bioorg Med Chem 2009;17:3536-42
  • He G, Dou D, Wei L, Inhibitors of human neutrophil elastase based on a highly functionalized N-amino-4-imidazolidinone scaffold. Eur J Med Chem 2010;45:4280-7
  • Von Nussbaum F, Karthaus D, Klein M, Preparation of 1,4-diarylpyrimidopyridazinyldiones as neutrophil elastase inhibitors. WO135599A120091112; 2009
  • Von Nussbaum F, Karthaus D, Anlauf S, 4-(4-Cyano-2-thioaryl)-dihydropyrimidones as neutrophil elastase inhibitors and their preparation and use in the treatment of diseases of the lung and cardiovascular system. WO080199A120090702; 2009
  • Ainge D, Chapman D, Lindsjoe M, Preparation of 2-pyrazinone derivatives as inhibitors of neutrophil elastase. WO061271A120090514; 2009
  • Finch H, Ray NC, Edwards C. Preparation of 3,4,6,7-tetrahydro-1H-pyrrolo[3,4-d]pyrimidine-2,5-diones having dual neutrophil elastase inhibiting and muscarinic M3 antagonist activity. WO060203A120090514; 2009
  • Ray NC, Finch H, Edwards C, Preparation of 4-(4-cyanophenyl)-1-(3-trifluoromethylphenyl)-3,4,6,7-tetrahydro-1H-pyrrolo[3,4-d]pyrimidine-2,5-diones as human neutrophil elastase inhibitors. WO060158A120090514; 2009
  • Burkamp F, Hansen P, Hossain N, Preparation of 2-pyrazinone derivatives and their use as inhibitors of neutrophil elastase. WO058076A120090507; 2009
  • Bergstroem L, Lundvkist M, Loenn H, Sjoe P. Preparation of 1-phenyl-6-methyl-2-pyridinone derivatives as neutrophil elastase inhibitors. WO030158A120080313; 2008
  • Hansen P, Lawitz K, Lepistoe M, Ray A. Preparation of 2-pyridone derivatives as neutrophil elastase inhibitors. WO129962A120071115; 2007
  • Brimert T, Lawitz K, Loenn H, Preparation of 2-pyridone derivatives as neutrophil elastase inhibitors and their use for treating inflammatory diseases and conditions. WO098684A120080921; 2006
  • Von Nussbaum F, Karthaus D, Anlauf S, Preparation of tetrazolopyrimidines as human neutrophil elastase inhibitors in treatment of pulmonary and cardiovascular diseases. WO078953A12010715; 2010
  • Klingstedt T, Lepistoe M, Lundkvist M, Loenn H. Preparation of dihydropyridones as human neutrophil elastase inhibitors. WO104752A120080904; 2008
  • Finch H, Edwards C, Ray NC, Fitzgerald MF. Preparation of dihydropyrimidone multimers as human neutrophil elastase inhibitors. WO136857A120061228; 2006
  • Thongyoo P, Bonomelli C, Leatherbarrow RJ, Tate EW. Potent inhibitors of beta-tryptase and human leukocyte elastase based on the MCoTI-II scaffold. J Med Chem 2009;52:6197-200
  • Sisay MT, Hautmann S, Mehner C, Inhibition of human leukocyte elastase by brunsvicamides A-C: cyanobacterial cyclic peptides. ChemMedChem 2009;4:1425-9
  • Craik DJ, Cemazar M, Daly NL. The cyclotides and related macrocyclic peptides as scaffolds in drug design. Curr Opin Drug Discov Dev 2006;9:251-60
  • Schmidtko A, Lotsch S, Freynhagen R, Geisslinger G. Zicotonide for treatment of severe chronic pain. Lancet 2010;375(9725):1569-77
  • Sin DD, Vestbo J. Biomarkers in chronic obstructive pulmonary disease. Proc Am Thorac Soc 2009;6:543-5
  • Gross NJ, Giembycz MA, Rennard SI. Treatment of chronic obstructive pulmonary disease with roflumilast, a new phosphodiesterase 4 inhibitor. J Chron Obstr Pulm Dis 2010;7:141-53
  • Le Quement C, Guenon I, Gillon JY, The selective MMP-12 inhibitor, AS111793 reduces airway inflammation in mice exposed to cigarette smoke. Br J Pharmacol 2008;154:1206-15
  • Banner KH, Press NJ. Dual PDE3/4 inhibitors as therapeutic agents for chronic obstructive pulmonary disease. Br J Pharmacol 2009;157:892-906
  • Morjaria JB, Malerba M, Polosa R. Biologic and pharmacologic therapies in clinical development for the inflammatory response in COPD. Drug Discov Today 2010;15:396-405

Reprints and Corporate Permissions

Please note: Selecting permissions does not provide access to the full text of the article, please see our help page How do I view content?

To request a reprint or corporate permissions for this article, please click on the relevant link below:

Academic Permissions

Please note: Selecting permissions does not provide access to the full text of the article, please see our help page How do I view content?

Obtain permissions instantly via Rightslink by clicking on the button below:

If you are unable to obtain permissions via Rightslink, please complete and submit this Permissions form. For more information, please visit our Permissions help page.