Therapeutic Targets Database
BIDD Pharmainformatics Databases
 
   
   

 

TTD Target ID: TTDR00029

Target Information
NameMatrilysin    
Type of targetDiscontinued target    
SynonymsMMP-7    
Matrin    
Matrix metalloproteinase-7    
Pump-1 protease    
Uterine metalloproteinase    
DiseaseCancer, unspecific
[ICD9: 140-229   ICD10: C00-C96]
[1]
Inflammation[1]
Drug(s)BB-3644Discontinued in Phase ICancer/Tumors[2][3]
BMS 275291Discontinued in Phase IIINon-small Cell Lung Cancer, Hormone-refractory Prostate Cancer, Kaposi's Sarcoma[4][5][6][2]
BatimastatDiscontinued in Phase ICancers[2]
MarimastatDiscontinued in Phase IIIPancreatic Cancer, Lung Cancer[7][8][9][2]
PrinomastatDiscontinued in Phase IIIBrain Cancer[10][11][12][13][2]
PrinomastatTrial haltedLung Cancer, Prostate Cancer[10][11][12][13][2]
BioChemical ClassHydrolases acting on peptide bonds (Peptidases)    
EC NumberEC 3.4.24.23
PathwayWnt signaling pathway
UniProt IDP09237
PDB Structure1MMP; 1MMQ; 1MMR; 2DDY.    
FunctionDegrades casein, gelatins of types i, iii, iv, and v, and fibronectin. Activates procollagenase.    
SequenceMRLTVLCAVCLLPGSLALPLPQEAGGMSELQWEQAQDYLKRFYLYDSETKNANSLEAKLK EMQKFFGLPITGMLNSRVIEIMQKPRCGVPDVAEYSLFPNSPKWTSKVVTYRIVSYTRDL PHITVDRLVSKALNMWGKEIPLHFRKVVWGTADIMIGFARGAHGDSYPFDGPGNTLAHAF APGTGLGGDAHFDEDERWTDGSSLGINFLYAATHELGHSLGMGHSSDPNAVMYPTYGNGD PQNFKLSQDDIKGIQKLYGKRSNSRKK
Related US Patent6,310,084
Target ValidationClick to Find Target Validation Information.    
Inhibitor3-Benzenesulfonyl-heptanoic acid hydroxyamide[14]
3-Cyclohexanesulfonyl-heptanoic acid hydroxyamide[14]
BB-3644[2][3]
BMS 275291[4][5][6][2]
Batimastat[2]
CGS-27023A[15]
IK-682[16]
Marimastat[7][8][9][2]
N-hydroxy-2,3-bis (phenylsulfonamido)propanamide[17]
Prinomastat[10][11][12][13][2]
RS-39066[18]
SC-44463[19]
SR-973[20]
folate gamma-L-phenylalaninehydroxamic acid[15]
folate gamma-L-proline-hydroxamic acid[15]
folate gamma-hydroxamic acid[15]
MultitargetBB-3644[2][3]
BMS 275291[4][5][6][2]
Batimastat[2]
Marimastat[7][8][9][2]
Prinomastat[10][11][12][13][2]
Cross References 3D Structure
Related Literature
On-Line Medical Dictionary
Ref 1Matrilysin (matrix metalloproteinase-7): a new promising drug target in cancer and inflammation? Cytokine Growth Factor Rev. 2004 Apr-Jun;15(2-3):111-5. To Reference
Ref 216498445 To Reference
Ref 3A phase I and pharmacological study of the matrix metalloproteinase inhibitor BB-3644 in patients with solid tumours. Br J Cancer. 2004 Feb 23;90(4):800-4. To Reference
Ref 4Phase 1/2 trial of BMS-275291 in patients with human immunodeficiency virus-related Kaposi sarcoma: a multicenter trial of the AIDS Malignancy Consortium. Cancer. 2008 Mar 1;112(5):1083-8. To Reference
Ref 5Randomized phase II feasibility study of combining the matrix metalloproteinase inhibitor BMS-275291 with paclitaxel plus carboplatin in advanced non-small cell lung cancer. Lung Cancer. 2004 Dec;46(3):361-8. To Reference
Ref 6Randomized phase III study of matrix metalloproteinase inhibitor BMS-275291 in combination with paclitaxel and carboplatin in advanced non-small-cell lung cancer: National Cancer Institute of Canada-Clinical Trials Group Study BR.18. J Clin Oncol. 2005 Apr 20;23(12):2831-9. To Reference
Ref 7Metalloelastase (MMP-12) induced inflammatory response in mice airways: effects of dexamethasone, rolipram and marimastat. Eur J Pharmacol. 2007 Mar 15;559(1):75-81. Epub 2006 Dec 12. To Reference
Ref 8Matrix metalloproteinase-2 involvement in breast cancer progression: a mini-review. Med Sci Monit. 2009 Feb;15(2):RA32-40. To Reference
Ref 9Matrix metalloproteinase inhibition as a novel anticancer strategy: a review with special focus on batimastat and marimastat. Pharmacol Ther. 1997;75(1):69-75. To Reference
Ref 10AG-3340 (Agouron Pharmaceuticals Inc). IDrugs. 2000 Mar;3(3):336-45. To Reference
Ref 11Inhibition of gelatinase activity reduces neural injury in an ex vivo model of hypoxia-ischemia. Neuroscience. 2009 Jun 2;160(4):755-66. Epub 2009 Mar 9. To Reference
Ref 12Delayed administration of a matrix metalloproteinase inhibitor limits progressive brain injury after hypoxia-ischemia in the neonatal rat. J Neuroinflammation. 2008 Aug 11;5:34. To Reference
Ref 13Pharmacoproteomics of a metalloproteinase hydroxamate inhibitor in breast cancer cells: dynamics of membrane type 1 matrix metalloproteinase-mediated membrane protein shedding. Mol Cell Biol. 2008 Aug;28(15):4896-914. Epub 2008 May 27. To Reference
Ref 14J Med Chem. 2000 Jun 15;43(12):2324-31.Hydroxamic acid derivatives as potent peptide deformylase inhibitors and antibacterial agents. To Reference
Ref 15Bioorg Med Chem. 2007 Feb 1;15(3):1266-74. Epub 2006 Nov 14.Methotrexate gamma-hydroxamate derivatives as potential dual target antitumor drugs. To Reference
Ref 16J Med Chem. 2002 Nov 7;45(23):4954-7.Discovery of gamma-lactam hydroxamic acids as selective inhibitors of tumor necrosis factor alpha converting enzyme: design, synthesis, and structure-activity relationships. To Reference
Ref 17Bioorg Med Chem Lett. 2008 Jun 1;18(11):3333-7. Epub 2008 Apr 16.Novel bis-(arylsulfonamide) hydroxamate-based selective MMP inhibitors. To Reference
Ref 18Bioorg. Med. Chem. Lett. 6(13):1601-1606 (1996) To Reference
Ref 19J Med Chem. 2003 Jul 31;46(16):3514-25.A potent, selective inhibitor of matrix metalloproteinase-3 for the topical treatment of chronic dermal ulcers. To Reference
Ref 20Bioorg Med Chem Lett. 2006 May 1;16(9):2357-63. Epub 2006 Feb 10.Synthesis and evaluation of succinoyl-caprolactam gamma-secretase inhibitors. To Reference



 

Welcome to sign our Guestbook.

If you find any error in data or bug in web service, please kindly report it to Dr. Zhu.


Dr. Chen Yuzong
Deputy Director of Center for Computational Science and Engineering
Professor in Department of Pharmacy
National University of Singapore, Singapore


All rights reserved.

   
 
 
Computer-aided Drug Design
about BIDD |  databases |  software |  teaching |  research |  links

 

Department of Computational Science | National University of Singapore | Blk S17, 3 Science Drive 2, Singapore 117543