MMP3 | M10: Matrix metallopeptidase | IUPHAR/BPS Guide to PHARMACOLOGY

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MMP3

target has curated data in GtoImmuPdb

Target id: 1630

Nomenclature: MMP3

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

Contents:

Gene and Protein Information
Species TM AA Chromosomal Location Gene Symbol Gene Name Reference
Human - 477 11q22.3 MMP3 matrix metallopeptidase 3
Mouse - 479 9 A1 Mmp3 matrix metallopeptidase 3
Rat - 475 8q11 Mmp3 matrix metallopeptidase 3
Previous and Unofficial Names
transin-1 | PTR1 protein | SL-1 | progelatinase | SLN1 | Str1 | STMY1 | matrix metallopeptidase 3 (stromelysin 1, progelatinase)
Database Links
Specialist databases
MEROPS M10.005 (Hs)
Other databases
BRENDA 3.4.24.17
CATH/Gene3D 2.110.10.10, 3.40.390.10
ChEMBL Target CHEMBL283 (Hs)
DrugBank Target P08254 (Hs)
Ensembl Gene ENSG00000149968 (Hs), ENSMUSG00000043613 (Mm), ENSRNOG00000032626 (Rn)
Entrez Gene 4314 (Hs), 17392 (Mm), 171045 (Rn)
Human Protein Atlas ENSG00000149968 (Hs)
KEGG Enzyme 3.4.24.17
KEGG Gene hsa:4314 (Hs), mmu:17392 (Mm), rno:171045 (Rn)
OMIM 185250 (Hs)
RefSeq Nucleotide NM_002422 (Hs), NM_010809 (Mm), NM_133523 (Rn)
RefSeq Protein NP_002413 (Hs), NP_034939 (Mm), NP_598207 (Rn)
UniProtKB P08254 (Hs), P28862 (Mm), P03957 (Rn)
Wikipedia MMP3 (Hs)
Enzyme Reaction
EC Number: 3.4.24.17

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 Value Parameter Reference
UK-356618 Hs Inhibition 8.2 pIC50 2
⤷ pIC50 8.2 (IC50 5.9x10-9 M) [2]
CM-352 Hs Inhibition 7.9 pIC50 6
⤷ pIC50 7.9 (IC50 1.2x10-8 M) [6]
CGS-27023A Hs Inhibition 7.8 pIC50 5
⤷ pIC50 7.8 (IC50 1.6x10-8 M) [5]
Immunopharmacology Comments
MMP3 is included in GtoImmuPdb based on its reported involvement in inflammatory diseases.
Immuno Process Associations
Immuno Process:  Cytokine production & signalling
GO Annotations:  Associated to 1 GO processes
GO:0019221 cytokine-mediated signaling pathway TAS
Immuno Process:  Immune regulation
GO Annotations:  Associated to 1 GO processes
GO:0150077 regulation of neuroinflammatory response TAS
Immuno Process:  Inflammation
GO Annotations:  Associated to 1 GO processes
GO:0150077 regulation of neuroinflammatory response TAS
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:  9
Disease Name:  Rheumatoid arthritis
Disease Synonyms:  no synonynms
Comment:  Serum level of MMP3 correlates with disease activity in RA, and is used as a biomarker for predicting bone and cartilage damage and evaluating therapeutic efficacy.
Disease X-refs:  Disease Ontology: DOID:7148
OMIM: 180300
References:  1,3
Disease Name:  Irritable bowel syndrome
Disease Synonyms:  no synonynms
Comment:  MMP3 has been shown to be causative in the tissue injury in IBD. Several functional polymorphisms in the promoter region of the MMP3 gene are associated with increased susceptibility to IBD.
Disease X-refs:  Disease Ontology: DOID:9778
References:  4,7-8
Clinically-Relevant Mutations and Pathophysiology
Disease:  Coronary heart disease, susceptibility to, 6
Synonyms: Coronary heart disease [Disease Ontology: DOID:3393]
Disease Ontology: DOID:3393
OMIM: 614466

References

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1. Fiedorczyk M, Klimiuk PA, Sierakowski S, Gindzienska-Sieskiewicz E, Chwiecko J. (2006) Serum matrix metalloproteinases and tissue inhibitors of metalloproteinases in patients with early rheumatoid arthritis. J. Rheumatol., 33 (8): 1523-9. [PMID:16881109]

2. Fray MJ, Dickinson RP. (2001) Discovery of potent and selective succinyl hydroxamate inhibitors of matrix metalloprotease-3 (stromelysin-1). Bioorg. Med. Chem. Lett., 11 (4): 571-4. [PMID:11229774]

3. Green MJ, Gough AK, Devlin J, Smith J, Astin P, Taylor D, Emery P. (2003) Serum MMP-3 and MMP-1 and progression of joint damage in early rheumatoid arthritis. Rheumatology (Oxford), 42 (1): 83-8. [PMID:12509618]

4. Juran BD, Atkinson EJ, Schlicht EM, Larson JJ, Ellinghaus D, Franke A, Lazaridis KN. (2011) Genetic polymorphisms of matrix metalloproteinase 3 in primary sclerosing cholangitis. Liver Int., 31 (6): 785-91. [PMID:21134112]

5. 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]

6. Orbe J, Rodríguez JA, Sánchez-Arias JA, Salicio A, Belzunce M, Ugarte A, Chang HC, Rabal O, Oyarzabal J, Páramo JA. (2015) Discovery and safety profiling of a potent preclinical candidate, (4-[4-[[(3R)-3-(hydroxycarbamoyl)-8-azaspiro[4.5]decan-3-yl]sulfonyl]phenoxy]-N-methylbenzamide) (CM-352), for the prevention and treatment of hemorrhage. J. Med. Chem., 58 (7): 2941-57. [PMID:25686022]

7. Pender SL, Croucher PJ, Mascheretti S, Prothero JD, Fisher SA, MacDonald TT, Schreiber S, Ye S. (2004) Transmission disequilibrium test of stromelysin-1 gene variation in relation to Crohn's disease. J. Med. Genet., 41 (9): e112. [PMID:15342709]

8. Pender SL, Tickle SP, Docherty AJ, Howie D, Wathen NC, MacDonald TT. (1997) A major role for matrix metalloproteinases in T cell injury in the gut. J. Immunol., 158 (4): 1582-90. [PMID:9029093]

9. Troeberg L, Nagase H. (2012) Proteases involved in cartilage matrix degradation in osteoarthritis. Biochim. Biophys. Acta, 1824 (1): 133-45. [PMID:21777704]

How to cite this page

M10: Matrix metallopeptidase: MMP3. Last modified on 19/04/2017. Accessed on 25/06/2019. IUPHAR/BPS Guide to PHARMACOLOGY, http://www.guidetopharmacology.org/GRAC/ObjectDisplayForward?objectId=1630.