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MMP3

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Immunopharmacology Ligand target has curated data in GtoImmuPdb

Target id: 1630

Nomenclature: MMP3

Family: M10: Matrix metallopeptidase

Contents:

Gene and Protein Information Click here for help
Species TM AA Chromosomal Location Gene Symbol Gene Name Reference
Human - 477 11q22.2 MMP3 matrix metallopeptidase 3
Mouse - 477 9 2.46 cM Mmp3 matrix metallopeptidase 3
Rat - 475 8q11 Mmp3 matrix metallopeptidase 3
Previous and Unofficial Names Click here for help
transin-1 | PTR1 protein | SL-1 | progelatinase | SLN1 | Str1 | STMY1 | matrix metallopeptidase 3 (stromelysin 1, progelatinase)
Database Links Click here for help
Specialist databases
MEROPS M10.005 (Hs)
Other databases
Alphafold P08254 (Hs), P28862 (Mm), P03957 (Rn)
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)
Pharos P08254 (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 Click here for help
EC Number: 3.4.24.17

Download all structure-activity data for this target as a CSV file go icon to follow link

Inhibitors
Key to terms and symbols View all chemical structures Click column headers to sort
Ligand Sp. Action Value Parameter Reference
batimastat Small molecule or natural product Click here for species-specific activity table Ligand has a PDB structure Hs Inhibition 9.2 pIC50 12
⤷ pIC50 9.2 (IC50 6.5x10-10 M) [12]
UK-356618 Small molecule or natural product Hs Inhibition 8.2 pIC50 2
⤷ pIC50 8.2 (IC50 5.9x10-9 M) [2]
CM-352 Small molecule or natural product Primary target of this compound Click here for species-specific activity table Hs Inhibition 7.9 pIC50 6
⤷ pIC50 7.9 (IC50 1.2x10-8 M) [6]
CGS-27023A Small molecule or natural product Click here for species-specific activity table Ligand has a PDB structure Hs Inhibition 7.8 pIC50 5
⤷ pIC50 7.8 (IC50 1.6x10-8 M) [5]
ilomastat Small molecule or natural product Click here for species-specific activity table Ligand has a PDB structure Hs Inhibition 7.5 pIC50 10
⤷ pIC50 7.5 (IC50 3.2x10-8 M) [10]
marimastat Small molecule or natural product Click here for species-specific activity table Ligand has a PDB structure Hs Inhibition 6.6 pIC50 9
⤷ pIC50 6.6 (IC50 2.3x10-7 M) [9]
Immunopharmacology Comments
MMP3 is included in GtoImmuPdb based on its reported involvement in inflammatory diseases.
Immuno Process Associations
Immuno Process:  Cytokine production & signalling
Immuno Process:  Immune regulation
Immuno Process:  Inflammation
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:  11
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 Click here for help
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. Rasmussen HS, McCann PP. (1997) Matrix metalloproteinase inhibition as a novel anticancer strategy: a review with special focus on batimastat and marimastat. Pharmacol Ther, 75 (1): 69-75. [PMID:9364582]

10. 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]

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

12. Yamamoto M, Tsujishita H, Hori N, Ohishi Y, Inoue S, Ikeda S, Okada Y. (1998) Inhibition of membrane-type 1 matrix metalloproteinase by hydroxamate inhibitors: an examination of the subsite pocket. J Med Chem, 41 (8): 1209-17. [PMID:9548812]

How to cite this page

M10: Matrix metallopeptidase: MMP3. Last modified on 12/07/2022. Accessed on 07/12/2024. IUPHAR/BPS Guide to PHARMACOLOGY, https://www.guidetopharmacology.org/GRAC/ObjectDisplayForward?objectId=1630.