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| 1 | Gelatin degradation assay reveals MMP-9 inhibitors and function of O-glycosylated domain显示文摘AIM: To establish a novel, sensitive and high-throughput gelatinolytic assay to define new inhibitors and compare domain deletion mutants of gelatinase B/matrix metalloproteinase (MMP)-9. METHODS: Fluorogenic Dye-quenched (DQ)TM-gelatin was used as a substrate and biochemical parameters (substrate and enzyme concentrations, DMSO solvent concentrations) were optimized to establish a highthroughput assay system. Various small-sized libraries (ChemDiv, InterBioScreen and ChemBridge) of hetero-cyclic, drug-like substances were tested and compared with prototypic inhibitors. RESULTS: First, we designed a test system with gelatin as a natural substrate. Second, the assay was validated by selecting a novel pyrimidine-2,4,6-trione (barbitu- rate) inhibitor. Third, and in line with present structural data on collagenolysis, it was found that deletion of the O-glycosylated region significantly decreased gelatinolytic activity (kcat/kM ± 40% less than full-length MMP-9). CONCLUSION: The DQTM-gelatin assay is useful in high-throughput drug screening and exosite targeting. We demonstrate that flexibility between the catalytic and hemopexin domain is functionally critical for gelatinolysis. | Jennifer Vandooren Nathalie Geurts Erik Martens Philippe E Van den Steen Steven De Jonghe Piet Herdewijn Ghislain Opdenakker | 2011 | World Journal of Biological Chemistry2011，2，1： | 3 |
| 2 | Far-field acoustic investigation into chevron nozzle mechanisms and trends显示文摘 | Callender B Gutmark E Martens S | 2005 | AIAA Journal2005，43，1： | 1 |
| 3 | Thermal denaturation of proteins in post rigor muscle tissue as studied by DSC显示文摘 | Stabursvik E Martens H | 1980 | Journal of the Science of Food and Agriculture1980，31，10： | 1 |
| 4 | Isomerization and hydrocracking of heptane over bimetallic bifunctional Pt- Pd/H - Beta and PtPd/USY zeolite catalysts 显示文摘 | Blomsma E Martens J A Jacobs P A | 1997 | J Catal1997，165，： | 1 |
| 5 | Arthroscopic findings in the knee of pre-adolescent children:report of 23 cases显示文摘 | Faraj AA Schilders E Martens M | 2000 | Arthroscopy2000，16，8： | 1 |
| 6 | Polymorphism and absence of Leu-enkephalin sequences in proenkephahn genes in Xenopus laevis 显示文摘 | MARTENS G J HERBERT E | 1984 | Nature1984，310，5974： | 1 |
| 7 | Reaction mechanisms of isomerization and cracking of heptane on Pd/H - Beta zeolite显示文摘 | Blomsma E Martens J A Jacobs P A | 1995 | J Catal1995，155，： | 1 |
| 8 | Do the stories they tell get them the money they need? the role of entrepreneurial narratives in resource acquisition 显示文摘 | Martens M L Jennings J E Jennings P D | 2007 | Academy of Management Journal2007，50，5： | 1 |
| 9 | Deficiency of gelati-nase B/MMP-9 aggravates lpr-induced lymphoprolifera-tion and lupus-like systemic autoimmune disease显示文摘 | Cauwe B Martens E Sagaert X | 2011 | JAutoimmun2011，36，34： | 1 |
| 10 | Cell cy-cle analysis of primary sponge cell cultures 显示文摘 | Schippers K J Martens D E Pomponi S A | | In0，，： | 1 |
| 11 | N2O production by heterotrophic N transformations in a semiarid soil显示文摘 | MCLAIN J E T MARTENS D A | 2006 | Appl Soil Ecol2006，32，2： | 1 |
| 12 | Texture and color changes in meat during cooking related to thermal denaturation of muscle proteins显示文摘 | MARTENS H STABUSSVIK E MARTENS M | 1982 | Journal of Texture Studies1982，13，： | 1 |
| 13 | Reactivity of recently deposited organic matter: Degradation of lipid compounds near the sediment-water interface 显示文摘 | CANUEL E A MARTENS C S | 1996 | Geochimica et Cosmochimica Acta1996，60，10： | 1 |
| 14 | Seasonal variations in ^7Be activity in the sediments of Cape Lookout Bight, North Carolina 显示文摘 | Canuel E A Martens C S Benninger L K | 1990 | Geochim Cosmochim Acta1990，54，1： | 1 |
| 15 | Effect of light intensity, pH, and temperature on triacylglycerol (TAG) accumulation induced by nitrogen starvation in Scenedesmus obliquus 显示文摘 | Breuer G Lamers P P Martens D E | 2013 | Bioresource Technology2013，143，： | 1 |
| 16 | Assessing Risk Indicators for Dental Caries in the Primary Dentition显示文摘 | Vampbbergen J Martens L Lesafre E | 2001 | Com munity Dent Oral Epidemiol2001，29，6： | 1 |
| 17 | An inactive protein phosphatase 2A population is associated with methylesterase and can be re-activated by the phosphotyrosyl phosphatase activator显示文摘 | Longin S Jordens J Martens E etal | 2004 | Biochem J2004，380，1： | 1 |
| 18 | Critical Commentary:Government Accounting and the Politics of Fear显示文摘 | Martens S Murphy E A | | 0，，03： | 1 |
| 19 | Hydrothermal CrystaUiz- tion of Zeolite Beta显示文摘 | Pereze P J Martens J A Rosinski E J | 1987 | Appl CataL1987，31，7： | 1 |
| 20 | Depression predicts elevated endothelin-1 in patients with coronary artery disease 显示文摘 | BURG M M MARTENS E J COLLINS D | 2011 | Psychosom Med2011，73，1： | 1 |
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