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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 | Changes in the epidemiolngic profile of sudden infant death syndrome as rates decline among California infants:1990-1995显示文摘 | Adams E J Chavez G F Steen D | 1998 | Pediatrics1998，102，6： | 1 |
| 3 | Insight into the pathophysiology of unstable coronary artery disease显示文摘 | Steen D K Ravn H B Falk E | 1997 | J Am Cardiol1997，80，5： | 1 |
| 4 | Biochemistry and molecular biology of gelatinase B or matrix metalloproteinase-9 (MMP-9) 显示文摘 | VAN DEN STEEN P E DUBOIS B NELISSEN I | 2002 | Crit Rev Biochem Mol Biol2002，37，6： | 1 |
| 5 | Distinguish source rock facies显示文摘 | Schulz L K Wilhelms A Rein E Steen A S | 2001 | Org Geochem2001，32，3： | 1 |
| 6 | Tackling matrix effects during development of a liquidchromatographic-electrospray ionisation tandem massspectrometric analysis of nine basic pharmaceuticals inaqueous environmental samples 显示文摘 | Van De Steene J C Mortier K A Lambert W E | 2006 | Journal ofChromatography A2006，1123，2： | 1 |
| 7 | Positive psychology in clinical practice显示文摘 | Lee D A Steen T A Seligman M E | 2005 | Annu Rev Clin Psychol2005，1，： | 1 |
| 8 | Soluble TWEAK is markedly upregulated in patients with ST elevation myocardial infarction and relatde to an adverse short term outcome显示文摘 | Chorianopoulos E Jarr K Steen H | 2010 | Ath erose[erosis2010，21，1： | 1 |
| 9 | New aspects for heterogeneous cobalt-catalyzed hydroamination of ethanol 显示文摘 | Rausch A K Steen E van Roessner F | 2008 | Journal of Catalysis2008，253，1： | 1 |
| 10 | Ge-latinase B functions as regulator and effectorin leukocyte biology显示文摘 | Ghislain Opdenakker Philippe E Van den Steen | | 0，，06： | 1 |
| 11 | Luminescence properties of red-emitting M2Si5N8:Eu2+ (M=Ca,Sr,Ba) LED conversion phosphors显示文摘 | Li Y Q van Steen J E J van Krevel J W H | 2006 | J Alloys Compd2006，417，： | 1 |
| 12 | Impaired insulin and insulin-like growth factor expression and signaling mechanisms in Alzheimer's disease-is this type 3 diabetes?显示文摘 | Steen E Terry BM Rivera EJ | 2005 | J Alzheimers Dis2005，7，1： | 1 |
| 13 | Impaired insulin and insulin-likegrowth factor expression and signaling mechanisms in Alzheimer’s dis-ease-is this type 3 diabetes?显示文摘 | Steen E Terry BM Rivera EJ | 2005 | J Alzheimers Dis2005，7，1： | 1 |
| 14 | Organizational beliefs and managerial vi- sion 显示文摘 | Van den Steen E | 2005 | Journal of Law Economics and Organization2005，21，1： | 1 |
| 15 | Insight into the pathophysiology of unstable coronary artery disease显示文摘 | Steen DK Ravn HB Falk E | 1997 | Am J Cardiol1997，80，5： | 1 |
| 16 | Root and rhizome dynamics in a perennial grass crop during an animal growth cycle显示文摘 | Steen E | 1985 | Journal of Agricultural Research1985，15，： | 1 |
| 17 | Positive psychology progress : Empirical validation of interventions 显示文摘 | Seligrnan M E Steen T A Park N | 2005 | Am Psychol2005，60，5： | 1 |
| 18 | TPRstudyon the preparation of impregnated Co/SiO2 catalysts显示文摘 | Van STEEN E SEWELL G S MAKHOTHE R A MIKELETHWAITE C MANSTEIN H de LANGE M OCONNOR C T | | 0，，02： | 1 |
| 19 | Temperature guided radiofrequency catheter ablation of myocardium:comparision of catheter tip and tissue temperature in vitro显示文摘 | Kongsgaard E Steen T Jense O | 1997 | Pacing Clin Electrophysiol1997，20，5： | 1 |
| 20 | Matrix metalloproteinase (MMP) expression in experimental choroidal neovascularization 显示文摘 | Kvanta A Shen WY Sarman S Seregard S Steen B Rakoczy E | 2000 | Curr Eye Res2000，21，： | 1 |
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