Target Information
Target General Infomation | |||||
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Target ID |
T65019
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Former ID |
TTDC00042
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Target Name |
Matrix metalloproteinase-14
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Gene Name |
MMP14
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Synonyms |
MMP-14; MMP-X1; MT-MMP 1; MT1-MMP; MT1MMP; MTMMP1; Membrane-type matrix metalloproteinase 1; Membrane-type-1 matrix metalloproteinase; MMP14
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Target Type |
Research
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Disease | Solid tumours [ICD9: 140-199, 210-229; ICD10: C00-D48] | ||||
Function |
Seems to specifically activate progelatinase A. May thus trigger invasion by tumor cells by activating progelatinase A on the tumor cell surface. May be involved in actin cytoskeleton reorganization bycleaving PTK7. Acts as a positive regulator of cell growth and migration via activation of MMP15. Involved in the formation of the fibrovascular tissues in association with pro- MMP2.
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BioChemical Class |
Peptidase
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Target Validation |
T65019
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UniProt ID | |||||
EC Number |
EC 3.4.24.80
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Sequence |
MSPAPRPPRCLLLPLLTLGTALASLGSAQSSSFSPEAWLQQYGYLPPGDLRTHTQRSPQS
LSAAIAAMQKFYGLQVTGKADADTMKAMRRPRCGVPDKFGAEIKANVRRKRYAIQGLKWQ HNEITFCIQNYTPKVGEYATYEAIRKAFRVWESATPLRFREVPYAYIREGHEKQADIMIF FAEGFHGDSTPFDGEGGFLAHAYFPGPNIGGDTHFDSAEPWTVRNEDLNGNDIFLVAVHE LGHALGLEHSSDPSAIMAPFYQWMDTENFVLPDDDRRGIQQLYGGESGFPTKMPPQPRTT SRPSVPDKPKNPTYGPNICDGNFDTVAMLRGEMFVFKERWFWRVRNNQVMDGYPMPIGQF WRGLPASINTAYERKDGKFVFFKGDKHWVFDEASLEPGYPKHIKELGRGLPTDKIDAALF WMPNGKTYFFRGNKYYRFNEELRAVDSEYPKNIKVWEGIPESPRGSFMGSDEVFTYFYKG NKYWKFNNQKLKVEPGYPKSALRDWMGCPSGGRPDEGTEEETEVIIIEVDEEGGGAVSAA AVVLPVLLLLLVLAVGLAVFFFRRHGTPRRLLYCQRSLLDKV |
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Drugs and Mode of Action | |||||
Inhibitor | 2-(4-bromophenylsulfonamido)-N-hydroxyacetamide | Drug Info | [530746] | ||
2-(biphenyl-4-ylsulfonamido)-N-hydroxyacetamide | Drug Info | [530746] | |||
2-(Biphenyl-4-ylsulfonyl)N-hydroxybenzamide | Drug Info | [530402] | |||
compound 29e | Drug Info | [532333] | |||
DX-2400 | Drug Info | [543455] | |||
EPIGALOCATECHIN GALLATE | Drug Info | [530210] | |||
IK-682 | Drug Info | [526446] | |||
ILOMASTAT | Drug Info | [529683] | |||
MMI270 | Drug Info | [528548] | |||
N-hydroxy-2-(4-methoxyphenylsulfonamido)acetamide | Drug Info | [530746] | |||
N-Hydroxy-2-(4-phenoxy-benzenesulfonyl)benzamide | Drug Info | [530402] | |||
SR-973 | Drug Info | [528025] | |||
UK-356618 | Drug Info | [526680] | |||
[2-(Biphenyl-4-sulfonyl)phenyl]acetic Acid | Drug Info | [530402] | |||
Target Expression Profile (TEP) and Drug Resistance Mutation (DRM) | |||||
TEP | EXP Info | ||||
Pathways | |||||
KEGG Pathway | TNF signaling pathway | ||||
GnRH signaling pathway | |||||
PANTHER Pathway | Alzheimer disease-presenilin pathway | ||||
Pathway Interaction Database | HIF-2-alpha transcription factor network | ||||
Signaling events mediated by focal adhesion kinase | |||||
Reactome | Collagen degradation | ||||
Degradation of the extracellular matrix | |||||
Activation of Matrix Metalloproteinases | |||||
WikiPathways | Senescence and Autophagy in Cancer | ||||
Activation of Matrix Metalloproteinases | |||||
Degradation of collagen | |||||
AGE/RAGE pathway | |||||
Matrix Metalloproteinases | |||||
References | |||||
Ref 526446 | J 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. | ||||
Ref 526680 | J 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. | ||||
Ref 528025 | Bioorg Med Chem Lett. 2006 May 1;16(9):2357-63. Epub 2006 Feb 10.Synthesis and evaluation of succinoyl-caprolactam gamma-secretase inhibitors. | ||||
Ref 528548 | Bioorg Med Chem. 2007 Feb 1;15(3):1266-74. Epub 2006 Nov 14.Methotrexate gamma-hydroxamate derivatives as potential dual target antitumor drugs. | ||||
Ref 529683 | Bioorg 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. | ||||
Ref 530210 | Bioorg Med Chem Lett. 2009 Aug 1;19(15):4171-4. Epub 2009 Jun 2.Regioselective synthesis of methylated epigallocatechin gallate via nitrobenzenesulfonyl (Ns) protecting group. | ||||
Ref 530402 | J Med Chem. 2009 Oct 22;52(20):6347-61.Design, synthesis, biological evaluation, and NMR studies of a new series of arylsulfones as selective and potent matrix metalloproteinase-12 inhibitors. | ||||
Ref 530746 | J Med Chem. 2010 Mar 25;53(6):2622-35.Potent arylsulfonamide inhibitors of tumor necrosis factor-alpha converting enzyme able to reduce activated leukocyte cell adhesion molecule shedding in cancer cell models. | ||||
Ref 532333 | Matrix metalloproteinase inhibitors based on the 3-mercaptopyrrolidine core. J Med Chem. 2013 Jun 13;56(11):4357-73. |
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