Target Information

Target General Infomation
Target ID
T65019
Former ID
TTDC00042
Target Name
Matrix metalloproteinase-14
Gene Name
MMP14
Synonyms
MMP-14; MMP-X1; MT-MMP 1; MT1-MMP; MT1MMP; MTMMP1; Membrane-type matrix metalloproteinase 1; Membrane-type-1 matrix metalloproteinase; MMP14
Target Type
Research
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.
BioChemical Class
Peptidase
Target Validation
T65019
UniProt ID
P50281
EC Number
EC 3.4.24.80
Sequence
MSPAPRPPRCLLLPLLTLGTALASLGSAQSSSFSPEAWLQQYGYLPPGDLRTHTQRSPQS
LSAAIAAMQKFYGLQVTGKADADTMKAMRRPRCGVPDKFGAEIKANVRRKRYAIQGLKWQ
HNEITFCIQNYTPKVGEYATYEAIRKAFRVWESATPLRFREVPYAYIREGHEKQADIMIF
FAEGFHGDSTPFDGEGGFLAHAYFPGPNIGGDTHFDSAEPWTVRNEDLNGNDIFLVAVHE
LGHALGLEHSSDPSAIMAPFYQWMDTENFVLPDDDRRGIQQLYGGESGFPTKMPPQPRTT
SRPSVPDKPKNPTYGPNICDGNFDTVAMLRGEMFVFKERWFWRVRNNQVMDGYPMPIGQF
WRGLPASINTAYERKDGKFVFFKGDKHWVFDEASLEPGYPKHIKELGRGLPTDKIDAALF
WMPNGKTYFFRGNKYYRFNEELRAVDSEYPKNIKVWEGIPESPRGSFMGSDEVFTYFYKG
NKYWKFNNQKLKVEPGYPKSALRDWMGCPSGGRPDEGTEEETEVIIIEVDEEGGGAVSAA
AVVLPVLLLLLVLAVGLAVFFFRRHGTPRRLLYCQRSLLDKV
Drugs and Mode of Action
Drug(s) ILOMASTAT Drug Info Preclinical Discovery agent [542432], [544872]
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 542432(http://www.guidetopharmacology.org/) Nucleic Acids Res. 2015 Oct 12. pii: gkv1037. The IUPHAR/BPS Guide to PHARMACOLOGY in 2016: towards curated quantitative interactions between 1300 protein targets and 6000 ligands. (Ligand id: 7409).
Ref 544872Trusted, scientifically sound profiles of drug programs, clinical trials, safety reports, and company deals, written by scientists. Springer. 2015. Adis Insight (drug id 800001387)
Ref 526446J 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 526680J 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 528025Bioorg Med Chem Lett. 2006 May 1;16(9):2357-63. Epub 2006 Feb 10.Synthesis and evaluation of succinoyl-caprolactam gamma-secretase inhibitors.
Ref 528548Bioorg Med Chem. 2007 Feb 1;15(3):1266-74. Epub 2006 Nov 14.Methotrexate gamma-hydroxamate derivatives as potential dual target antitumor drugs.
Ref 529683Bioorg 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 530210Bioorg 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 530402J 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 530746J 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 532333Matrix metalloproteinase inhibitors based on the 3-mercaptopyrrolidine core. J Med Chem. 2013 Jun 13;56(11):4357-73.
Ref 543455(http://www.guidetopharmacology.org/) Nucleic Acids Res. 2015 Oct 12. pii: gkv1037. The IUPHAR/BPS Guide to PHARMACOLOGY in 2016: towards curated quantitative interactions between 1300 protein targets and 6000 ligands. (Target id: 1638).
Ref 1587926URL: https://www.ebi.ac.uk/chembl/ The ChEMBL database in 2017

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