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MMP1

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Target id: 1628

Nomenclature: MMP1

Family: M10: Matrix metallopeptidase

This target is also described as a ligand entry: matrix metalloproteinase 1

Contents:

Gene and Protein Information Click here for help
Species TM AA Chromosomal Location Gene Symbol Gene Name Reference
Human - 469 11q22.2 MMP1 matrix metallopeptidase 1
Mouse - 464 9 A1 Mmp1a matrix metallopeptidase 1a (interstitial collagenase)
Rat - 464 8q11 Mmp1 matrix metallopeptidase 1
Previous and Unofficial Names Click here for help
Collagenase-1 | fibroblast collagenase | matrix metallopeptidase 1a | Mcol-A | CLG | matrix metallopeptidase 1 (interstitial collagenase)
Database Links Click here for help
Specialist databases
MEROPS M10.001 (Hs)
Other databases
Alphafold P03956 (Hs), Q9EPL5 (Mm), P81563 (Rn)
BRENDA 3.4.24.7
CATH/Gene3D 2.110.10.10, 3.40.390.10
ChEMBL Target CHEMBL332 (Hs)
DrugBank Target P03956 (Hs)
Ensembl Gene ENSG00000196611 (Hs), ENSMUSG00000043089 (Mm), ENSRNOG00000032353 (Rn)
Entrez Gene 4312 (Hs), 83995 (Mm), 300339 (Rn)
Human Protein Atlas ENSG00000196611 (Hs)
KEGG Enzyme 3.4.24.7
KEGG Gene hsa:4312 (Hs), mmu:83995 (Mm), rno:300339 (Rn)
OMIM 120353 (Hs)
Orphanet ORPHA306110 (Hs)
Pharos P03956 (Hs)
RefSeq Nucleotide NM_002421 (Hs), NM_032006 (Mm), NM_001134530 (Rn)
RefSeq Protein NP_002412 (Hs), NP_114395 (Mm), NP_001128002 (Rn)
SynPHARM 82905 (in complex with CGS-27023A)
UniProtKB P03956 (Hs), Q9EPL5 (Mm), P81563 (Rn)
Wikipedia MMP1 (Hs)
Enzyme Reaction Click here for help
EC Number: 3.4.24.7

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 9.3 pKi 1
⤷ pKi 9.3 (Ki 5x10-10 M) [1]
cipemastat Small molecule or natural product Immunopharmacology Ligand Hs Inhibition 8.5 pKi 2
⤷ pKi 8.5 (Ki 3x10-9 M) [2]
batimastat Small molecule or natural product Click here for species-specific activity table Ligand has a PDB structure Hs Inhibition 9.0 pIC50 3
⤷ pIC50 9.0 (IC50 9.9x10-10 M) [3]
ilomastat Small molecule or natural product Click here for species-specific activity table Ligand has a PDB structure Hs Inhibition 8.2 – 9.3 pIC50 6,9
⤷ pIC50 9.3 (IC50 5.6x10-10 M) [9]
pIC50 8.2 (IC50 6x10-9 M) [6]
marimastat Small molecule or natural product Click here for species-specific activity table Ligand has a PDB structure Hs Inhibition 8.3 pIC50 8
⤷ pIC50 8.3 (IC50 5x10-9 M) [8]
apratastat Small molecule or natural product Click here for species-specific activity table Immunopharmacology Ligand Hs Inhibition 7.5 pIC50 5
⤷ pIC50 7.5 (IC50 3.3x10-8 M) [5]
CGS-27023A Small molecule or natural product Click here for species-specific activity table Ligand has a PDB structure Hs Inhibition 7.3 pIC50 7
⤷ pIC50 7.3 (IC50 5.6x10-8 M) [7]
Immunopharmacology Comments
Overexpression of MMP-1 degrades extracellular matrix causing damage to the colon mucosa in patients with ulcerative colitis. The MMP-1 promotes secretion of TNFα causing futher damage. Levels of MMP-1 and TNFα correlate with disease severity [10].
Immuno Process Associations
Immuno Process:  Inflammation
Immuno Process:  Cytokine production & signalling
Immuno Process:  Chemotaxis & migration
Immuno Disease Associations
Disease Name:  Rheumatoid arthritis
Disease Synonyms:  no synonynms
Comment:  Serum level of MMP1 correlates with disease activity in RA.
Disease X-refs:  Disease Ontology: DOID:7148
OMIM: 180300
References:  4
Clinically-Relevant Mutations and Pathophysiology Click here for help
Disease:  Epidermolysis bullosa dystrophica, autosomal recessive
Synonyms: Epidermolysis bullosa dystrophica [Disease Ontology: DOID:4959]
Severe generalized recessive dystrophic epidermolysis bullosa [Orphanet: ORPHA79408]
Disease Ontology: DOID:4959
OMIM: 226600
Orphanet: ORPHA79408

References

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1. Castelhano AL, Billedeau R, Dewdney N, Donnelly S, Horne S, Kurz LJ, Liak T, Martin R, Uppington R, Zhengyu Yuan et al.. (1995) Novel indolactam-based inhibitors of matrix metalloproteinases. Bioorg Med Chem Lett, 5: 1415-1420. DOI: 10.1016/0960-894X(95)00233-J

2. Close DR. (2001) Matrix metalloproteinase inhibitors in rheumatic diseases. Ann Rheum Dis, 60 Suppl 3: iii62-7. [PMID:11890658]

3. Fray MJ, Dickinson RP, Huggins JP, Occleston NL. (2003) A potent, selective inhibitor of matrix metalloproteinase-3 for the topical treatment of chronic dermal ulcers. J Med Chem, 46 (16): 3514-25. [PMID:12877590]

4. 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]

5. Levin JI, Chen JM, Laakso LM, Du M, Schmid J, Xu W, Cummons T, Xu J, Jin G, Barone D et al.. (2006) Acetylenic TACE inhibitors. Part 3: Thiomorpholine sulfonamide hydroxamates. Bioorg Med Chem Lett, 16 (6): 1605-9. [PMID:16426848]

6. 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]

7. 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]

8. 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]

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]

10. Wang YD, Mao JW. (2007) Expression of matrix metalloproteinase-1 and tumor necrosis factor-alpha in ulcerative colitis. World J Gastroenterol, 13 (44): 5926-32. [PMID:17990358]

How to cite this page

M10: Matrix metallopeptidase: MMP1. Last modified on 12/07/2022. Accessed on 15/10/2024. IUPHAR/BPS Guide to PHARMACOLOGY, https://www.guidetomalariapharmacology.org/GRAC/ObjectDisplayForward?objectId=1628.