دورية أكاديمية
Purification of active matrix metalloproteinase catalytic domains and its use for screening of specific stromelysin-3 inhibitors.
| العنوان: | Purification of active matrix metalloproteinase catalytic domains and its use for screening of specific stromelysin-3 inhibitors. |
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| المؤلفون: | Kannan, R., Ruff, M., Kochins, J. G., Manly, S. P., Stoll, I., El Fahime, E. M., Noël, Agnès, Foidart, Jean-Michel, Dive, v, Basset, P. |
| المصدر: | Protein Expression and Purification, 16, 76-83 (1999) |
| بيانات النشر: | Academic Press, 1999. |
| سنة النشر: | 1999 |
| مصطلحات موضوعية: | α-1 proteinase inhibitor, cephalosporin, matrix metalloproteinase inhibitors, stromelysin-3, Life sciences, Biochemistry, biophysics & molecular biology, Sciences du vivant, Biochimie, biophysique & biologie moléculaire |
| الوصف: | The matrix metalloproteinase (MMP) stromelysin-3 (ST3) has been shown to be involved in malignant tumor progression and therefore represents an attractive therapeutical target. In order to screen for ST3 synthetic inhibitors, we have produced and purified the catalytic domain of ST3, matrilysin, stromelysin-2, and membrane type-1 MMP from inclusion bodies in a bacterial system. Our strategy allowed the purification of MMPs directly in the active form, thereby avoidingin vitroactivation. A total of 140,000 synthetic compounds from the Bristol-Myers Pharmaceutical Research Institute chemical deck were tested, using a substrate-based colorimetric enzymatic assay, in which ST3 activity was evaluated through its ability to cleave and inactivate α-1 proteinase inhibitor. One ST3 inhibitor belonging to the cephalosporin family of antibiotics was thereby identified. |
| نوع الوثيقة: | journal article http://purl.org/coar/resource_type/c_6501 article |
| اللغة: | English |
| Relation: | urn:issn:1046-5928; urn:issn:1096-0279 |
| DOI: | 10.1006/prep.1999.1068 |
| URL الوصول: | https://orbi.uliege.be/handle/2268/39419 |
| حقوق: | open access http://purl.org/coar/access_right/c_abf2 info:eu-repo/semantics/openAccess |
| رقم الأكسشن: | edsorb.39419 |
| قاعدة البيانات: | ORBi |
| DOI: | 10.1006/prep.1999.1068 |
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