The DOI matches its Crossref record; 13 of the 13 references it cites were found in a registry or an index.
ONO-5046, a novel inhibitor of human neutrophil elastase
Abstract
ONO-5046, N-[2-[4-(2,2-Dimethylpropionyloxy)phenylsulfonylamino] aminoacetic acid, competitively inhibited human neutrophil elastase (IC50 = 0.044 microM, Ki = 0.2 microM). It also inhibited leukocyte elastase obtained from rabbit, rat, hamster and mouse. However, ONO-5046 did not inhibit trypsin, thrombin, plasmin, plasma kallikrein, pancreas kallikrein, chymotrypsin and cathepsin G even at 100 microM. In in vivo studies, ONO-5046 suppressed lung hemorrhage in hamster (ID50 = 82 micrograms/kg) by intratracheal administration and increase of skin capillary permeability in guinea pig (ID50 = 9.6 mg/kg) by intravenous administration, both of which were induced by human neutrophil elastase.
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In the citing paper
“However, PK101 and the optimal HNE peptide substrates selected from the combinatorial library contain unnatural amino acid residues [20], and the inhibitor drugs targeting HNE are small non-proteinaceous synthetic molecules [22,23].”
From Discrimination of Methionine Sulfoxide and Sulfone by Human Neutrophil Elastase (2021) · cites this paper as [22]
In the citing paper
“This notion is consistent with the observation of sulfone moieties in inhibitor drugs targeting HNE, including Sivelestat [22] and the Bayer inhibitor, BAY 85-8501 [23].”
From Discrimination of Methionine Sulfoxide and Sulfone by Human Neutrophil Elastase (2021) · cites this paper as [22]
Citations
Cites
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Campbell, E. J., Senior, R. M., McDonald, J. A., Cox, D. L., Greco, J. M., & Landis, J. A. (1982) · Journal of Clinical Investigation · doi:10.1172/jci110681 · Cited by 243
Purification and specificity of pancreatic elastase
Naughton, M. A., & Sanger, F. (1961) · Biochemical Journal · doi:10.1042/bj0780156 · Cited by 206
Physiology and Pathophysiology of Neutral Proteinases of Human Granulocytes
HAVEMANN, K., & Gramse, M. (1984) · Advances in experimental medicine and biology · doi:10.1007/978-1-4615-9355-3_1 · Cited by 132
Campbell, E. J., & Campbell, M. A. (1988) · The Journal of Cell Biology · doi:10.1083/jcb.106.3.667 · Cited by 125
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Weiss, S. J., Curnutte, J. T., & REGIANI, S. R. (1986) · The Journal of Immunology · doi:10.4049/jimmunol.136.2.636 · Cited by 112
Weissmann, G., & Korchak, H. M. (1984) · Inflammation · doi:10.1007/bf00915708 · Cited by 78
A new class of inhibitors of human leucocyte elastase
Hassall, C. H., Johnson, W. H., Kennedy, A. J., & Roberts, N. A. (1985) · FEBS Letters · doi:10.1016/0014-5793(85)80776-6 · Cited by 37
A novel method of isolation and some characteristic properties of human pancreatic elastases
Fujimoto, K.-I., Ogawa, M., Saito, N., Kōsaki, G., Minamiura, N., & Yamamoto, T. (1980) · Biochimica et Biophysica Acta (BBA) - Enzymology · doi:10.1016/0005-2744(80)90300-9 · Cited by 21
Research works printed but not linked: 7
- Carp, 1982, 79, 2041
- Jochum, 1986, Behring Inst. Mitt, 79, 121
- Krell, 1988, FASEB Journal, 2, A346
- Trainor, 1987, TIPS, 8, 303
- Levine, 1976, Am. Rev. Respir. Dis, 113, 25
- Matsuoka, 1989, Japan J. Pharmacol, 51, 455, 10.1254/jjp.51.455 · DOI
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Cited by
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Protease Inhibitors: Current Status and Future Prospects
Leung, D., Abbenante, G., & Fairlie, D. P. (2000) · Journal of Medicinal Chemistry · doi:10.1021/jm990412m · Cited by 879
Neutrophil Elastase, Proteinase 3, and Cathepsin G as Therapeutic Targets in Human Diseases
Korkmaz, B., Horwitz, M. S., Jenne, D. E., & Gauthier, F. (2010) · Pharmacological Reviews · doi:10.1124/pr.110.002733 · Cited by 898
Wang, S., Voisin, M.-B., Larbi, K. Y., Dangerfield, J. A., Scheiermann, C., Tran, M. G. B., Maxwell, P. H., Sorokin, L. M., & Nourshargh, S. (2006) · The Journal of Experimental Medicine · doi:10.1084/jem.20051210 · Cited by 374
Neutrophil elastase inhibition in acute lung injury: Results of the STRIVE study
Zeiher, B. G., Artigas, A., Vincent, J., Dmitrienko, A. A., Jackson, K. A., Thompson, B., & Bernard, G. R. (2004) · Critical Care Medicine · doi:10.1097/01.ccm.0000133332.48386.85 · Cited by 348
The role of neutrophil elastase in acute lung injury
Kawabata, K., Hagio, T., & Matsuoka, S. (2002) · European Journal of Pharmacology · doi:10.1016/s0014-2999(02)02182-9 · Cited by 338
Self-citation
Metadata
- Authors
- Kawabata, K., Suzuki, M., Sugitani, M., Imaki, K., Toda, M., & Miyamoto, T.
- Affiliations
- Ono Pharmaceutical (Japan) (JP)
- ORCID
- Suzuki, Mayumi
- Venue
- Biochemical and Biophysical Research Communications
- Publisher
- Elsevier BV
- Published
- 1991-06
- Volume
- 177
- Issue
- 2
- Pages
- 814-820
- ISSN
- 0006-291X (ISSN-L)
- OpenAlex
- W2039697569
- Cited by
- 359
- References
- 13
- Citations by year
- 2026: 8 · 2025: 6 · 2024: 11 · 2023: 10 · 2022: 10 · 2021: 9 · 2020: 7 · 2019: 9 · 2018: 7 · 2017: 8 · 2016: 8 · 2015: 18 · 2014: 8 · 2013: 11 · 2012: 12
- FWCI
- 2.09
- Type
- journal article
- Language
- en
- Open access
- closed
- Locations
- Biochemical and Biophysical Research Communications (publishedVersion)
- PubMed (publishedVersion)
- Topics
- Life Sciences › Biochemistry, Genetics and Molecular Biology › Cancer Research › Protease and Inhibitor Mechanisms
- Life Sciences › Immunology and Microbiology › Immunology › Neutrophil, Myeloperoxidase and Oxidative Mechanisms
- Health Sciences › Medicine › Hematology › Coagulation, Bradykinin, Polyphosphates, and Angioedema
- Keywords
- ONO-5046, human neutrophil elastase, leukocyte elastase, elastase inhibitors, competitive inhibition, serine protease inhibition, pulmonary hemorrhage
- MeSH terms
- Animals, Binding, Competitive, Capillary Permeability, Glycine, Guinea Pigs, Cricetinae, Hemorrhage, Humans, Lung Diseases, Male, Mesocricetus, Neutrophils, Pancreatic Elastase, Rabbits, Skin Diseases, Sulfonamides, Mice, Rats
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