MMP13

Target id: 1637

Nomenclature: MMP13

Family: M10: Matrix metallopeptidase

Annotation status:  image of an orange circle Annotated and awaiting review. Please contact us if you can help with reviewing.  » Email us

This target is also described as a ligand entry: matrix metalloproteinase 13

   GtoImmuPdb view: OFF :     MMP13 has curated GtoImmuPdb data

Gene and Protein Information
Species TM AA Chromosomal Location Gene Symbol Gene Name Reference
Human - 471 11q22.3 MMP13 matrix metallopeptidase 13
Mouse - 472 9 A1-A2 Mmp13 matrix metallopeptidase 13
Rat - 472 8q11 Mmp13 matrix metallopeptidase 13
Previous and Unofficial Names
UMRCASE | interstitial collagenase | Mmp1 | CLG3 | collagenase-1 | matrix metallopeptidase 13 (collagenase 3)
Database Links
Specialist databases
MEROPS M10.013 (Hs)
Other databases
BRENDA
CATH/Gene3D
ChEMBL Target
DrugBank Target
Ensembl Gene
Entrez Gene
GenitoUrinary Development Molecular Anatomy Project
Human Protein Atlas
KEGG Enzyme
KEGG Gene
OMIM
Orphanet
RefSeq Nucleotide
RefSeq Protein
SynPHARM
UniProtKB
Wikipedia
Enzyme Reaction
EC Number: 3.4.24.-

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
Ligand Sp. Action Affinity Units Reference
SL422 Hs Inhibition 9.4 pKi 9
pKi 9.4 (Ki 4.5x10-10 M) [9]
prinomastat Hs Inhibition 10.4 pIC50 1
pIC50 10.4 (IC50 3.8x10-11 M) [1]
compound 1 [PMID: 17935984] Hs Inhibition 9.2 pIC50 3
pIC50 9.2 (IC50 6x10-10 M) [3]
compound 15 [PMID: 22017539] Hs Inhibition 9.0 pIC50 6
pIC50 9.0 (IC50 1x10-9 M) [6]
PF-152 Hs Inhibition 8.8 pIC50 5
pIC50 8.8 (IC50 1.5x10-9 M) [5]
AZD6605 Hs Inhibition 8.3 pIC50 4
pIC50 8.3 (IC50 5x10-9 M) [4]
CL82198 Hs Inhibition - - 2
[2]
WAY170523 Hs Inhibition - - 2
[2]
Inhibitor Comments
SL422 is a broad-spectrum inhibitor of MMP enzymes [9].
Immunopharmacology Comments
Elevated MMP-13 expression correlates with inflammation in patients with Crohn's disease and ulcerative colitis, suggesting a role for this protease in disease pathogenesis [8].
Immuno Disease Associations
Disease Name:  Osteoarthritis
Disease Synonyms:  no synonynms
Comment:  The collagenolytic MMPs 3 and 13 are strongly implicated in cartilage destruction in OA.
Disease X-refs:  Disease Ontology: DOID:8398
References:  7
Clinically-Relevant Mutations and Pathophysiology
Disease:  Spondyloepimetaphyseal dysplasia, Missouri type
Synonyms: Metaphyseal anadysplasia [Orphanet: ORPHA1040]
Metaphyseal anadysplasia 1
Disease Ontology: DOID:0080030
OMIM: 602111
Orphanet: ORPHA93356, ORPHA1040

References

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1. Abbenante G, Fairlie DP. (2005) Protease inhibitors in the clinic. Med Chem1 (1): 71-104. [PMID:16789888]

2. Chen JM, Nelson FC, Levin JI, Mobilio D, Moy FJ, Nilakantan R, Zask A, Powers R. (2000) Structure-Based Design of a Novel, Potent, and Selective Inhibitor for MMP-13 Utilizing NMR Spectroscopy and Computer-Aided Molecular Design. Journal of the American Chemical Society122 (40): 9648-9654.

3. Freeman-Cook KD, Reiter LA, Noe MC, Antipas AS, Danley DE, Datta K, Downs JT, Eisenbeis S, Eskra JD, Garmene DJ et al.. (2007) Potent, selective spiropyrrolidine pyrimidinetrione inhibitors of MMP-13. Bioorg. Med. Chem. Lett.17 (23): 6529-34. [PMID:17935984]

4. MRC. AZD6605 Matrix metallopeptidase 13 (MMP13) inhibitor. Accessed on 28/10/2014. Modified on 28/10/2014. MRC/AstraZeneca: Mechanisms of Disease Call, http://webarchive.nationalarchives.gov.uk/20120104105854/http://www.mrc.ac.uk/consumption/groups/public/documents/content/mrc008371.pdf

5. Ruminski PG, Massa M, Strohbach J, Hanau CE, Schmidt M, Scholten JA, Fletcher TR, Hamper BC, Carroll JN, Shieh HS. (2016) Discovery of N-(4-Fluoro-3-methoxybenzyl)-6-(2-(((2S,5R)-5-(hydroxymethyl)-1,4-dioxan-2-yl)methyl)-2H-tetrazol-5-yl)-2-methylpyrimidine-4-carboxamide. A Highly Selective and Orally Bioavailable Matrix Metalloproteinase-13 Inhibitor for the Potential Treatment of Osteoarthritis. Journal of Medicinal Chemistry.59 (1): 313-327.

6. Taylor SJ, Abeywardane A, Liang S, Muegge I, Padyana AK, Xiong Z, Hill-Drzewi M, Farmer B, Li X, Collins B et al.. (2011) Fragment-based discovery of indole inhibitors of matrix metalloproteinase-13. J. Med. Chem.54 (23): 8174-87. [PMID:22017539]

7. Troeberg L, Nagase H. (2012) Proteases involved in cartilage matrix degradation in osteoarthritis. Biochim. Biophys. Acta1824 (1): 133-45. [PMID:21777704]

8. Vizoso FJ, González LO, Corte MD, Corte MG, Bongera M, Martínez A, Martín A, Andicoechea A, Gava RR. (2006) Collagenase-3 (MMP-13) expression by inflamed mucosa in inflammatory bowel disease. Scand. J. Gastroenterol.41 (9): 1050-5. [PMID:16938718]

9. Xue CB, Voss ME, Nelson DJ, Duan JJ, Cherney RJ, Jacobson IC, He X, Roderick J, Chen L, Corbett RL et al.. (2001) Design, synthesis, and structure-activity relationships of macrocyclic hydroxamic acids that inhibit tumor necrosis factor alpha release in vitro and in vivo. J. Med. Chem.44 (16): 2636-60. [PMID:11472217]

How to cite this page

M10: Matrix metallopeptidase: MMP13. Last modified on 16/03/2017. Accessed on 24/10/2017. IUPHAR/BPS Guide to PHARMACOLOGY, http://www.guidetopharmacology.org/GRAC/ObjectDisplayForward?objectId=1637.