DT-Web

DB00786 - Marimastat


Identification
Name Marimastat
Accession Number DB00786 (APRD00559)
Type small molecule
Description Used in the treatment of cancer, Marmiastat is an angiogenesis and metastasis inhibitor. As an angiogenesis inhibitor it limits the growth and production of blood vessels. As an antimetatstatic agent it prevents malignant cells from breaching the basement membranes.
Structure
MOL SDF PDB SMILES InChI
Categories (*)
Molecular Weight 331.4079
Groups approved
Monoisotopic Weight 331.210721053
Pharmacology
Indication For the treatment of various cancers
Mechanism of action Marimastat is a broad spectrum matrix metalloprotease inhibitor. It mimics the peptide structure of natural MMP substrates and binds to matrix metalloproteases, thereby preventing the degradation of the basement membrane by these proteases. This antiprotease action prevents the migration of endothelial cells needed to form new blood vessels. Inhibition of MMPs also prevents the entry and exit of tumor cells into existing blood cells, thereby preventing metastasis.
Absorption Not Available
Protein binding Not Available
Biotransformation Not Available
Route of elimination Not Available
Toxicity Not Available
Affected organisms
  • Humans and other mammals
Interactions
Drug Interactions Not Available
Food Interactions Not Available

Targets


Interstitial collagenase
Name Interstitial collagenase
Gene Name MMP1
Pharmacological action yes
Actions inhibitor
References
  • Heath EI, Grochow LB: Clinical potential of matrix metalloprotease inhibitors in cancer therapy. Drugs. 2000 May;59(5):1043-55. - Pubmed
  • Belotti D, Paganoni P, Giavazzi R: MMP inhibitors: experimental and clinical studies. Int J Biol Markers. 1999 Oct-Dec;14(4):232-8. - Pubmed
  • Chen X, Ji ZL, Chen YZ: TTD: Therapeutic Target Database. Nucleic Acids Res. 2002 Jan 1;30(1):412-5. - Pubmed
DTHybrid score 2.016
72 kDa type IV collagenase
Name 72 kDa type IV collagenase
Gene Name MMP2
Pharmacological action yes
Actions inhibitor
References
  • Chen X, Ji ZL, Chen YZ: TTD: Therapeutic Target Database. Nucleic Acids Res. 2002 Jan 1;30(1):412-5. - Pubmed
  • Treharne GD, Boyle JR, Goodall S, Loftus IM, Bell PR, Thompson MM: Marimastat inhibits elastin degradation and matrix metalloproteinase 2 activity in a model of aneurysm disease. Br J Surg. 1999 Aug;86(8):1053-8. - Pubmed
  • Fanchon S, Bourd K, Septier D, Everts V, Beertsen W, Menashi S, Goldberg M: Involvement of matrix metalloproteinases in the onset of dentin mineralization. Eur J Oral Sci. 2004 Apr;112(2):171-6. - Pubmed
  • Bernardo MM, Brown S, Li ZH, Fridman R, Mobashery S: Design, synthesis, and characterization of potent, slow-binding inhibitors that are selective for gelatinases. J Biol Chem. 2002 Mar 29;277(13):11201-7. Epub 2002 Jan 14. - Pubmed
  • Shinoda K, Shibuya M, Hibino S, Ono Y, Matsuda K, Takemura A, Zou D, Kokubo Y, Takechi A, Kudoh S: A novel matrix metalloproteinase inhibitor, FYK-1388 suppresses tumor growth, metastasis and angiogenesis by human fibrosarcoma cell line. Int J Oncol. 2003 Feb;22(2):281-8. - Pubmed
  • Bourd-Boittin K, Fridman R, Fanchon S, Septier D, Goldberg M, Menashi S: Matrix metalloproteinase inhibition impairs the processing, formation and mineralization of dental tissues during mouse molar development. Exp Cell Res. 2005 Apr 1;304(2):493-505. Epub 2005 Jan 11. - Pubmed
DTHybrid score 1.2967
Stromelysin-1
Name Stromelysin-1
Gene Name MMP3
Pharmacological action yes
Actions antagonist
References
  • Chen X, Ji ZL, Chen YZ: TTD: Therapeutic Target Database. Nucleic Acids Res. 2002 Jan 1;30(1):412-5. - Pubmed
DTHybrid score 2.4966
Matrilysin
Name Matrilysin
Gene Name MMP7
Pharmacological action yes
Actions antagonist
References
  • Heath EI, Grochow LB: Clinical potential of matrix metalloprotease inhibitors in cancer therapy. Drugs. 2000 May;59(5):1043-55. - Pubmed
  • Belotti D, Paganoni P, Giavazzi R: MMP inhibitors: experimental and clinical studies. Int J Biol Markers. 1999 Oct-Dec;14(4):232-8. - Pubmed
DTHybrid score 2.0251
Neutrophil collagenase
Name Neutrophil collagenase
Gene Name MMP8
Pharmacological action yes
Actions inhibitor
References
  • Heath EI, Grochow LB: Clinical potential of matrix metalloprotease inhibitors in cancer therapy. Drugs. 2000 May;59(5):1043-55. - Pubmed
  • Belotti D, Paganoni P, Giavazzi R: MMP inhibitors: experimental and clinical studies. Int J Biol Markers. 1999 Oct-Dec;14(4):232-8. - Pubmed
DTHybrid score 2.3248
Matrix metalloproteinase-9
Name Matrix metalloproteinase-9
Gene Name Not Available
Pharmacological action yes
Actions inhibitor
References
  • Underwood CK, Min D, Lyons JG, Hambley TW: The interaction of metal ions and Marimastat with matrix metalloproteinase 9. J Inorg Biochem. 2003 Jun 1;95(2-3):165-70. - Pubmed
  • Nenan S, Lagente V, Planquois JM, Hitier S, Berna P, Bertrand CP, Boichot E: Metalloelastase (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. - Pubmed
  • Chen X, Ji ZL, Chen YZ: TTD: Therapeutic Target Database. Nucleic Acids Res. 2002 Jan 1;30(1):412-5. - Pubmed
DTHybrid score 1.4848
Stromelysin-2
Name Stromelysin-2
Gene Name MMP10
Pharmacological action yes
Actions antagonist
References
  • Heath EI, Grochow LB: Clinical potential of matrix metalloprotease inhibitors in cancer therapy. Drugs. 2000 May;59(5):1043-55. - Pubmed
  • Belotti D, Paganoni P, Giavazzi R: MMP inhibitors: experimental and clinical studies. Int J Biol Markers. 1999 Oct-Dec;14(4):232-8. - Pubmed
DTHybrid score 1.2382
Stromelysin-3
Name Stromelysin-3
Gene Name MMP11
Pharmacological action yes
Actions antagonist
References
  • Heath EI, Grochow LB: Clinical potential of matrix metalloprotease inhibitors in cancer therapy. Drugs. 2000 May;59(5):1043-55. - Pubmed
  • Belotti D, Paganoni P, Giavazzi R: MMP inhibitors: experimental and clinical studies. Int J Biol Markers. 1999 Oct-Dec;14(4):232-8. - Pubmed
DTHybrid score 1.6571
Macrophage metalloelastase
Name Macrophage metalloelastase
Gene Name MMP12
Pharmacological action yes
Actions inhibitor
References
  • Heath EI, Grochow LB: Clinical potential of matrix metalloprotease inhibitors in cancer therapy. Drugs. 2000 May;59(5):1043-55. - Pubmed
  • Belotti D, Paganoni P, Giavazzi R: MMP inhibitors: experimental and clinical studies. Int J Biol Markers. 1999 Oct-Dec;14(4):232-8. - Pubmed
DTHybrid score 2.3327
Collagenase 3
Name Collagenase 3
Gene Name MMP13
Pharmacological action yes
Actions inhibitor
References
  • Heath EI, Grochow LB: Clinical potential of matrix metalloprotease inhibitors in cancer therapy. Drugs. 2000 May;59(5):1043-55. - Pubmed
  • Belotti D, Paganoni P, Giavazzi R: MMP inhibitors: experimental and clinical studies. Int J Biol Markers. 1999 Oct-Dec;14(4):232-8. - Pubmed
DTHybrid score 2.1458
Matrix metalloproteinase-14
Name Matrix metalloproteinase-14
Gene Name MMP14
Pharmacological action yes
Actions inhibitor
References
  • Heath EI, Grochow LB: Clinical potential of matrix metalloprotease inhibitors in cancer therapy. Drugs. 2000 May;59(5):1043-55. - Pubmed
  • Belotti D, Paganoni P, Giavazzi R: MMP inhibitors: experimental and clinical studies. Int J Biol Markers. 1999 Oct-Dec;14(4):232-8. - Pubmed
DTHybrid score 1.0605
Matrix metalloproteinase-15
Name Matrix metalloproteinase-15
Gene Name MMP15
Pharmacological action yes
Actions inhibitor
References
  • Heath EI, Grochow LB: Clinical potential of matrix metalloprotease inhibitors in cancer therapy. Drugs. 2000 May;59(5):1043-55. - Pubmed
  • Belotti D, Paganoni P, Giavazzi R: MMP inhibitors: experimental and clinical studies. Int J Biol Markers. 1999 Oct-Dec;14(4):232-8. - Pubmed
DTHybrid score 1.0606
Matrix metalloproteinase-16
Name Matrix metalloproteinase-16
Gene Name MMP16
Pharmacological action yes
Actions inhibitor
References
  • Heath EI, Grochow LB: Clinical potential of matrix metalloprotease inhibitors in cancer therapy. Drugs. 2000 May;59(5):1043-55. - Pubmed
  • Belotti D, Paganoni P, Giavazzi R: MMP inhibitors: experimental and clinical studies. Int J Biol Markers. 1999 Oct-Dec;14(4):232-8. - Pubmed
DTHybrid score 1.0922
Matrix metalloproteinase-17
Name Matrix metalloproteinase-17
Gene Name MMP17
Pharmacological action yes
Actions inhibitor
References
  • Heath EI, Grochow LB: Clinical potential of matrix metalloprotease inhibitors in cancer therapy. Drugs. 2000 May;59(5):1043-55. - Pubmed
  • Belotti D, Paganoni P, Giavazzi R: MMP inhibitors: experimental and clinical studies. Int J Biol Markers. 1999 Oct-Dec;14(4):232-8. - Pubmed
DTHybrid score 1.0581
Matrix metalloproteinase-19
Name Matrix metalloproteinase-19
Gene Name MMP19
Pharmacological action yes
Actions inhibitor
References
  • Heath EI, Grochow LB: Clinical potential of matrix metalloprotease inhibitors in cancer therapy. Drugs. 2000 May;59(5):1043-55. - Pubmed
  • Belotti D, Paganoni P, Giavazzi R: MMP inhibitors: experimental and clinical studies. Int J Biol Markers. 1999 Oct-Dec;14(4):232-8. - Pubmed
DTHybrid score 1.0575
Matrix metalloproteinase-20
Name Matrix metalloproteinase-20
Gene Name MMP20
Pharmacological action yes
Actions inhibitor
References
  • Heath EI, Grochow LB: Clinical potential of matrix metalloprotease inhibitors in cancer therapy. Drugs. 2000 May;59(5):1043-55. - Pubmed
  • Belotti D, Paganoni P, Giavazzi R: MMP inhibitors: experimental and clinical studies. Int J Biol Markers. 1999 Oct-Dec;14(4):232-8. - Pubmed
DTHybrid score 1.2356
Matrix metalloproteinase-21
Name Matrix metalloproteinase-21
Gene Name MMP21
Pharmacological action yes
Actions inhibitor
References
  • Heath EI, Grochow LB: Clinical potential of matrix metalloprotease inhibitors in cancer therapy. Drugs. 2000 May;59(5):1043-55. - Pubmed
  • Belotti D, Paganoni P, Giavazzi R: MMP inhibitors: experimental and clinical studies. Int J Biol Markers. 1999 Oct-Dec;14(4):232-8. - Pubmed
DTHybrid score 1.0573
Matrix metalloproteinase-23
Name Matrix metalloproteinase-23
Gene Name MMP23A
Pharmacological action yes
Actions inhibitor
References
  • Heath EI, Grochow LB: Clinical potential of matrix metalloprotease inhibitors in cancer therapy. Drugs. 2000 May;59(5):1043-55. - Pubmed
  • Belotti D, Paganoni P, Giavazzi R: MMP inhibitors: experimental and clinical studies. Int J Biol Markers. 1999 Oct-Dec;14(4):232-8. - Pubmed
DTHybrid score 1.0581
Matrix metalloproteinase-24
Name Matrix metalloproteinase-24
Gene Name MMP24
Pharmacological action yes
Actions inhibitor
References
  • Heath EI, Grochow LB: Clinical potential of matrix metalloprotease inhibitors in cancer therapy. Drugs. 2000 May;59(5):1043-55. - Pubmed
  • Belotti D, Paganoni P, Giavazzi R: MMP inhibitors: experimental and clinical studies. Int J Biol Markers. 1999 Oct-Dec;14(4):232-8. - Pubmed
DTHybrid score 1.0619
Matrix metalloproteinase-25
Name Matrix metalloproteinase-25
Gene Name MMP25
Pharmacological action yes
Actions inhibitor
References
  • Heath EI, Grochow LB: Clinical potential of matrix metalloprotease inhibitors in cancer therapy. Drugs. 2000 May;59(5):1043-55. - Pubmed
  • Belotti D, Paganoni P, Giavazzi R: MMP inhibitors: experimental and clinical studies. Int J Biol Markers. 1999 Oct-Dec;14(4):232-8. - Pubmed
DTHybrid score 1.0587
Matrix metalloproteinase-26
Name Matrix metalloproteinase-26
Gene Name MMP26
Pharmacological action yes
Actions inhibitor
References
  • Heath EI, Grochow LB: Clinical potential of matrix metalloprotease inhibitors in cancer therapy. Drugs. 2000 May;59(5):1043-55. - Pubmed
  • Belotti D, Paganoni P, Giavazzi R: MMP inhibitors: experimental and clinical studies. Int J Biol Markers. 1999 Oct-Dec;14(4):232-8. - Pubmed
DTHybrid score 1.0589
Matrix metalloproteinase-27
Name Matrix metalloproteinase-27
Gene Name MMP27
Pharmacological action yes
Actions inhibitor
References
  • Heath EI, Grochow LB: Clinical potential of matrix metalloprotease inhibitors in cancer therapy. Drugs. 2000 May;59(5):1043-55. - Pubmed
  • Belotti D, Paganoni P, Giavazzi R: MMP inhibitors: experimental and clinical studies. Int J Biol Markers. 1999 Oct-Dec;14(4):232-8. - Pubmed
DTHybrid score 1.0589
Matrix metalloproteinase-28
Name Matrix metalloproteinase-28
Gene Name MMP28
Pharmacological action yes
Actions inhibitor
References
  • Heath EI, Grochow LB: Clinical potential of matrix metalloprotease inhibitors in cancer therapy. Drugs. 2000 May;59(5):1043-55. - Pubmed
  • Belotti D, Paganoni P, Giavazzi R: MMP inhibitors: experimental and clinical studies. Int J Biol Markers. 1999 Oct-Dec;14(4):232-8. - Pubmed
DTHybrid score 1.0575

Predictions


Id Partner name Gene Name Score
6230 A disintegrin and metalloproteinase with thrombospondin motifs 5 ADAMTS5 0.1935
6374 Disintegrin and metalloproteinase domain-containing protein 28 ADAM28 0.1648
370 Urease alpha subunit ureC 0.0676
244 Angiotensin-converting enzyme ACE 0.0477
1539 Oligopeptide transporter, small intestine isoform SLC15A1 0.037
1729 Solute carrier family 22 member 6 SLC22A6 0.0365
587 Serum albumin ALB 0.0302
3090 Chitosanase csn 0.0267
4149 Nuclear factor NF-kappa-B p100 subunit NFKB2 0.0267
1588 Multidrug resistance protein 1 ABCB1 0.0255
4119 Cytochrome P450 2D6 CYP2D6 0.025
1253 Interferon gamma IFNG 0.023
777 Tumor necrosis factor TNF 0.0203
1654 Interleukin-1 beta IL1B 0.0149
494 Caspase-1 CASP1 0.0135
1507 Cytochrome c CYCS 0.0127
183 Vascular endothelial growth factor A VEGFA 0.012
2077 Caspase-3 CASP3 0.0116
6013 Cytochrome P450 2E1 CYP2E1 0.0104
22 30S ribosomal protein S4 rpsD 0.0103
6714 30S ribosomal protein S4 rpsD 0.0103
140 30S ribosomal protein S9 rpsI 0.0097
6719 30S ribosomal protein S9 rpsI 0.0097
6725 30S ribosomal protein S9 rpsI 0.0097
6016 Cytochrome P450 2C19 CYP2C19 0.0092
275 Arachidonate 5-lipoxygenase ALOX5 0.0089
1024 Solute carrier family 22 member 11 SLC22A11 0.0072
6143 Solute carrier family 22 member 7 SLC22A7 0.007
6142 Solute carrier family 22 member 8 SLC22A8 0.0063
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