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Gene and Protein Information | ||||||
Species | TM | AA | Chromosomal Location | Gene Symbol | Gene Name | Reference |
Human | 1 | 582 | 14q11.2 | MMP14 | matrix metallopeptidase 14 | |
Mouse | 1 | 582 | 14 27.79 cM | Mmp14 | matrix metallopeptidase 14 (membrane-inserted) | |
Rat | 1 | 582 | 15p13 | Mmp14 | matrix metallopeptidase 14 |
Database Links | |
Specialist databases | |
MEROPS | M10.014 (Hs) |
Other databases | |
Alphafold | P50281 (Hs), P53690 (Mm), Q10739 (Rn) |
BRENDA | 3.4.24.80 |
CATH/Gene3D | 3.40.390.10, 2.110.10.10 |
ChEMBL Target | CHEMBL3869 (Hs), CHEMBL4295783 (Mm) |
DrugBank Target | P50281 (Hs) |
Ensembl Gene | ENSG00000157227 (Hs), ENSMUSG00000000957 (Mm), ENSRNOG00000010947 (Rn) |
Entrez Gene | 4323 (Hs), 17387 (Mm), 81707 (Rn) |
Human Protein Atlas | ENSG00000157227 (Hs) |
KEGG Enzyme | 3.4.24.80 |
KEGG Gene | hsa:4323 (Hs), mmu:17387 (Mm), rno:81707 (Rn) |
OMIM | 600754 (Hs) |
Orphanet | ORPHA314731 (Hs) |
Pharos | P50281 (Hs) |
RefSeq Nucleotide | NM_004995 (Hs), NM_008608 (Mm), NM_031056 (Rn) |
RefSeq Protein | NP_004986 (Hs), NP_032634 (Mm), NP_112318 (Rn) |
UniProtKB | P50281 (Hs), P53690 (Mm), Q10739 (Rn) |
Wikipedia | MMP14 (Hs) |
Enzyme Reaction | ||||
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Download all structure-activity data for this target as a CSV file
Inhibitors | |||||||||||||||||||||||||||||||||||||||||||||||||||||||||||||||||||||||||||||||||||||||||||||||||||||||||||||||||||||||||||||||||||||||||||||||||||||||||||||||||||||||||||||||||||
Key to terms and symbols | View all chemical structures | Click column headers to sort | |||||||||||||||||||||||||||||||||||||||||||||||||||||||||||||||||||||||||||||||||||||||||||||||||||||||||||||||||||||||||||||||||||||||||||||||||||||||||||||||||||||||||||||||||
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Immunopharmacology Comments |
MMP14 is included in GtoImmuPdb based on its contribution to degradation of collagenous cartilage matrix in rheumatoid arthritis. An anti-MMP14 antibody, DX-2400 [1], has shown preclinical efficacy in the mouse collagen-induced arthritis (CIA) model of RA [3]. DX-2400 inhibits MMP14 activity with a Ki of 0.8 nM [1]. |
Immuno Process Associations | ||
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Immuno Disease Associations | ||||||||||
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Clinically-Relevant Mutations and Pathophysiology | ||||||||||||
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1. Devy L, Huang L, Naa L, Yanamandra N, Pieters H, Frans N, Chang E, Tao Q, Vanhove M, Lejeune A et al.. (2009) Selective inhibition of matrix metalloproteinase-14 blocks tumor growth, invasion, and angiogenesis. Cancer Res, 69 (4): 1517-26. [PMID:19208838]
2. Jin Y, Roycik MD, Bosco DB, Cao Q, Constantino MH, Schwartz MA, Sang QX. (2013) Matrix metalloproteinase inhibitors based on the 3-mercaptopyrrolidine core. J Med Chem, 56 (11): 4357-73. [PMID:23631440]
3. Kaneko K, Williams RO, Dransfield DT, Nixon AE, Sandison A, Itoh Y. (2016) Selective Inhibition of Membrane Type 1 Matrix Metalloproteinase Abrogates Progression of Experimental Inflammatory Arthritis: Synergy With Tumor Necrosis Factor Blockade. Arthritis Rheumatol, 68 (2): 521-31. [PMID:26315469]
4. Ma D, Wu W, Yang G, Li J, Li J, Ye Q. (2004) Tetrahydroisoquinoline based sulfonamide hydroxamates as potent matrix metalloproteinase inhibitors. Bioorg Med Chem Lett, 14 (1): 47-50. [PMID:14684295]
5. Nguyen TT, Ding D, Wolter WR, Pérez RL, Champion MM, Mahasenan KV, Hesek D, Lee M, Schroeder VA, Jones JI et al.. (2018) Validation of Matrix Metalloproteinase-9 (MMP-9) as a Novel Target for Treatment of Diabetic Foot Ulcers in Humans and Discovery of a Potent and Selective Small-Molecule MMP-9 Inhibitor That Accelerates Healing. J Med Chem, 61 (19): 8825-8837. [PMID:30212201]
6. Nuti E, Casalini F, Santamaria S, Gabelloni P, Bendinelli S, Da Pozzo E, Costa B, Marinelli L, La Pietra V, Novellino E et al.. (2011) Synthesis and biological evaluation in U87MG glioma cells of (ethynylthiophene)sulfonamido-based hydroxamates as matrix metalloproteinase inhibitors. Eur J Med Chem, 46 (7): 2617-29. [PMID:21514700]
7. Pap T, Shigeyama Y, Kuchen S, Fernihough JK, Simmen B, Gay RE, Billingham M, Gay S. (2000) Differential expression pattern of membrane-type matrix metalloproteinases in rheumatoid arthritis. Arthritis Rheum, 43 (6): 1226-32. [PMID:10857781]
8. Sabeh F, Fox D, Weiss SJ. (2010) Membrane-type I matrix metalloproteinase-dependent regulation of rheumatoid arthritis synoviocyte function. J Immunol, 184 (11): 6396-406. [PMID:20483788]
9. Takeuchi T, Hayashi M, Tamita T, Nomura Y, Kojima N, Mitani A, Takeda T, Hitaka K, Kato Y, Kamitani M et al.. (2022) Discovery of Aryloxyphenyl-Heptapeptide Hybrids as Potent and Selective Matrix Metalloproteinase-2 Inhibitors for the Treatment of Idiopathic Pulmonary Fibrosis. J Med Chem, 65 (12): 8493-8510. [PMID:35687819]
M10: Matrix metallopeptidase: MMP14. Last modified on 12/07/2022. Accessed on 10/12/2024. IUPHAR/BPS Guide to PHARMACOLOGY, https://www.guidetoimmunopharmacology.org/GRAC/ObjectDisplayForward?objectId=1638.