Therapeutic Targets Database
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TTD Target ID: TTDC00105

Target Information
NameStromelysin-1    
Type of targetDiscontinued target    
SynonymsMMP-3    
Matrix metalloproteinase 3    
Matrix metalloproteinase-3    
SL-1    
Transin-1    
DiseaseBrain Cancer
[ICD9: 191   ICD10: C71]
[1][2][3]
Cancer, unspecific
[ICD9: 140-229   ICD10: C00-C96]
[4][5][6][7]
Lung Cancer
[ICD9: 162   ICD10: C33-C34]
[8][9][10]
Myocardial infarction (MI)
[ICD9: 410   ICD10: I21, I22]
[11]
Osteoarthritis
[ICD9: 715   ICD10: M15-M19, M47]
[11]
Osteoarthritis
[ICD9: 715   ICD10: M15-M19, M47]
[12][13][14]
Ovarian cancer
[ICD9: 183   ICD10: C56]
[12][13][14]
Pancreatic Cancer
[ICD9: 157   ICD10: C25]
[8][9][10]
Prostate cancer
[ICD9: 185   ICD10: C61]
[1][2][3]
Drug(s)GalardinDiscontinued in Phase IICorneal ulcers[15][16]
PG-116800Suspended in Phase IIAcute and chronic heart failure[17]
PG-530742Suspended in Phase IIOsteoarthritis, Myocardial infarction[11][18]
BioChemical ClassHydrolases acting on peptide bonds (Peptidases)    
EC NumberEC 3.4.24.17
UniProt IDP08254
PDB Structure1B3D; 1B8Y; 1BIW; 1BM6; 1BQO; 1C3I; 1C8T; 1CAQ; 1CIZ; 1CQR; 1D5J; 1D7X; 1D8F; 1D8M; 1G05; 1G49; 1G4K; 1HFS; 1HY7; 1M1W; 1OO9; 1QIA; 1QIC; 1SLM; 1SLN; 1UEA; 1UMS; 1UMT; 1USN; 2D1O; 2JNP; 2JT5; 2JT6; 2SRT; 2USN; 3OHL; 3OHO; 3USN; 4DPE; 4G9L; 4JA1.    
FunctionCan degrade fibronectin, laminin, gelatins of type i, iii, iv, and v; collagens iii, iv, x, and ix, and cartilage proteoglycans. Activates procollagenase.    
SequenceMKSLPILLLLCVAVCSAYPLDGAARGEDTSMNLVQKYLENYYDLKKDVKQFVRRKDSGPV VKKIREMQKFLGLEVTGKLDSDTLEVMRKPRCGVPDVGHFRTFPGIPKWRKTHLTYRIVN YTPDLPKDAVDSAVEKALKVWEEVTPLTFSRLYEGEADIMISFAVREHGDFYPFDGPGNV LAHAYAPGPGINGDAHFDDDEQWTKDTTGTNLFLVAAHEIGHSLGLFHSANTEALMYPLY HSLTDLTRFRLSQDDINGIQSLYGPPPDSPETPLVPTEPVPPEPGTPANCDPALSFDAVS TLRGEILIFKDRHFWRKSLRKLEPELHLISSFWPSLPSGVDAAYEVTSKDLVFIFKGNQF WAIRGNEVRAGYPRGIHTLGFPPTVRKIDAAISDKEKNKTYFFVEDKYWRFDEKRNSMEP GFPKQIAEDFPGIDSKIDAVFEEFGFFYFFTGSSQLEFDPNAKKVTHTLKSNSWLNC
Related US Patent6,265,432
6,297,247
6,307,089
6,350,885
6,350,907
6,399,612
6,420,408
6,492,422
6,624,196
Target ValidationClick to Find Target Validation Information.    
QSAR ModelClick to Find Target QSAR Model.    
Inhibitor1-Methyloxy-4-Sulfone-Benzene[19]
3-Methylpyridine[19]
5-Biphenyl-4-yl-5-ethyl-pyrimidine-2,4,6-trione[20]
8-chloro-quinoline-3-carbonitrile[21]
AM-2S[22]
BAY-12-9566[23]
BB-1101[24]
CGS-27023A[25]
CIPEMASTAT[26]
FUTOENONE[27]
Galardin[15][16]
Hydroxyaminovaline[19]
IK-682[28]
ILOMASTAT[29]
L-696418[30]
MMI270[7]
PD-169469[31]
PD-169469[31]
PG-116800[17]
PG-530742[11][18]
PKF-242-484,   TNF-484[26]
PNU-107859[32]
PNU-142372[33]
PNU-142372[32]
RO-319790[34]
RS-130830[35]
RS-39066[36]
Ro-32-3555[37]
Ro-37-9790[37]
SC-44463[38]
UK-356618[39]
MultitargetPG-116800[17]
Cross References 3D Structure
Related Literature
On-Line Medical Dictionary
Ref 1Inhibition 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 2Delayed 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 3Pharmacoproteomics 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 4Curr Pharm Des. 2005;11(3):295-322.Recent developments in the design of specific Matrix Metalloproteinase inhibitors aided by structural and computational studies. To Reference
Ref 5Metalloproteinase inhibition augments antitumor efficacy of the anti-CD30 immunotoxin Ki-3(scFv)-ETA' against human lymphomas in vivo. Int J Cancer. 2004 Sep 10;111(4):568-74. To Reference
Ref 6A 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 7Strategies for MMP inhibition in cancer: innovations for the post-trial era. Nat Rev Cancer. 2002 Sep;2(9):657-72. To Reference
Ref 8Novel investigational drugs for gastric cancer. Expert Opin Investig Drugs. 2009 Jul;18(7):945-55. To Reference
Ref 9Matrix metalloproteinase-2 involvement in breast cancer progression: a mini-review. Med Sci Monit. 2009 Feb;15(2):RA32-40. To Reference
Ref 10Matrix 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 11Am J Physiol Heart Circ Physiol. 2006 Jun;290(6):H2522-7. Epub 2006 Jan 20.Selective matrix metalloproteinase inhibition attenuates progression of left ventricular dysfunction and remodeling in dogs with chronic heart failure. To Reference
Ref 12Radiation therapy and biological compounds for consolidation therapy in advanced ovarian cancer. Int J Gynecol Cancer. 2008 Mar-Apr;18 Suppl 1:44-6. To Reference
Ref 13Conflicting results from clinical observations and murine models: what is the role of plasminogen activators in tumor growth? J Natl Cancer Inst. 2006 Jun 7;98(11):726-7. To Reference
Ref 14A phase III randomized trial of BAY 12-9566 (tanomastat) as maintenance therapy in patients with advanced ovarian cancer responsive to primary surgery and paclitaxel/platinum containing chemotherapy: a National Cancer Institute of Canada Clinical Trials Group Study. Gynecol Oncol. 2006 Aug;102(2):300-8. Epub 2006 Jan 25. To Reference
Ref 1517060126 To Reference
Ref 1618172013 To Reference
Ref 17Emerging drugs for acute and chronic heart failure: current and future developments. Expert Opin Emerg Drugs. 2007 Mar;12(1):75-95. To Reference
Ref 1816498445 To Reference
Ref 19Overington JP, Al-Lazikani B, Hopkins AL: How many drug targets are there? Nat Rev Drug Discov. 2006 Dec;5(12):993-6. To Reference
Ref 20Bioorg Med Chem Lett. 2001 Apr 23;11(8):969-72.Novel 5,5-disubstitutedpyrimidine-2,4,6-triones as selective MMP inhibitors. To Reference
Ref 21J Biol Chem. 2007 Nov 16;282(46):33295-304. Epub 2007 Sep 11.Pharmacologic inhibition of tpl2 blocks inflammatory responses in primary human monocytes, synoviocytes, and blood. To Reference
Ref 22Bioorg Med Chem Lett. 2009 Apr 1;19(7):1970-6. Epub 2009 Feb 14.Synthesis of hydroxypyrone- and hydroxythiopyrone-based matrix metalloproteinase inhibitors: developing a structure-activity relationship. To Reference
Ref 23Suppression of adjuvant arthritis of rats by a novel matrix metalloproteinase-inhibitor. Br J Pharmacol. 2000 Dec;131(8):1513-20. To Reference
Ref 24Bioorg Med Chem Lett. 1998 Jun 16;8(12):1443-8.Broad spectrum matrix metalloproteinase inhibitors: an examination of succinamide hydroxamate inhibitors with P1 C alpha gem-disubstitution. To Reference
Ref 25Bioorg Med Chem Lett. 2005 Mar 1;15(5):1321-6.N-i-Propoxy-N-biphenylsulfonylaminobutylhydroxamic acids as potent and selective inhibitors of MMP-2 and MT1-MMP. To Reference
Ref 26Bioorg Med Chem Lett. 2006 May 15;16(10):2632-6. Epub 2006 Mar 3.A cassette-dosing approach for improvement of oral bioavailability of dual TACE/MMP inhibitors. To Reference
Ref 27Bioorg. Med. Chem. Lett. 5(15):1637-1642 (1995) To Reference
Ref 28J 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 29Bioorg Med Chem. 2008 Sep 15;16(18):8745-59. Epub 2008 Jul 20.Introduction of the 4-(4-bromophenyl)benzenesulfonyl group to hydrazide analogs of Ilomastat leads to potent gelatinase B (MMP-9) inhibitors with improved selectivity. To Reference
Ref 30Bioorg. Med. Chem. Lett. 5(6):539-542 (1995) To Reference
Ref 31J Med Chem. 2006 Feb 9;49(3):923-31.Structural insight into the stereoselective inhibition of MMP-8 by enantiomeric sulfonamide phosphonates. To Reference
Ref 32J Med Chem. 2004 Jun 3;47(12):3065-74.A molecular basis for the selectivity of thiadiazole urea inhibitors with stromelysin-1 and gelatinase-A from generalized born molecular dynamics simulations. To Reference
Ref 33Bioorg Med Chem Lett. 2002 Oct 7;12(19):2667-72.Protease inhibitors: synthesis of matrix metalloproteinase and bacterial collagenase inhibitors incorporating 5-amino-2-mercapto-1,3,4-thiadiazole zinc binding functions. To Reference
Ref 34Bioorg Med Chem Lett. 1998 May 19;8(10):1163-8.The asymmetric synthesis and in vitro characterization of succinyl mercaptoalcohol and mercaptoketone inhibitors of matrix metalloproteinases. To Reference
Ref 35Bioorg Med Chem Lett. 2005 Feb 15;15(4):1101-6.Structure-based design of potent and selective inhibitors of collagenase-3 (MMP-13). To Reference
Ref 36Bioorg. Med. Chem. Lett. 6(13):1601-1606 (1996) To Reference
Ref 37Bioorg. Med. Chem. Lett. 7(17):2299-2302 (1997) To Reference
Ref 38Bioorg. Med. Chem. Lett. 7(18):2331-2336 (1997) To Reference
Ref 39J 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



 

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