MMP1

Target id: 1628

Nomenclature: MMP1

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 1

   GtoImmuPdb view: OFF :     MMP1 has curated GtoImmuPdb data

Gene and Protein Information
Species TM AA Chromosomal Location Gene Symbol Gene Name Reference
Human - 469 11q21-q22 MMP1 matrix metallopeptidase 1
Mouse - 464 9 A1-A2 Mmp1a matrix metallopeptidase 1a (interstitial collagenase)
Rat - 464 8q11 Mmp1 matrix metallopeptidase 1
Previous and Unofficial Names
Collagenase-1 | fibroblast collagenase | matrix metallopeptidase 1a | Mcol-A | CLG | matrix metallopeptidase 1 (interstitial collagenase)
Database Links
Specialist databases
MEROPS M10.001 (Hs)
Other databases
BRENDA
CATH/Gene3D
ChEMBL Target
DrugBank Target
Ensembl Gene
Entrez Gene
Human Protein Atlas
KEGG Enzyme
KEGG Gene
OMIM
Orphanet
RefSeq Nucleotide
RefSeq Protein
SynPHARM
UniProtKB
Wikipedia
Enzyme Reaction
EC Number: 3.4.24.7

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
cipemastat Hs Inhibition 8.5 pKi 1
pKi 8.5 (Ki 3x10-9 M) [1]
ilomastat Hs Inhibition 8.2 pIC50 4
pIC50 8.2 (IC50 6x10-9 M) [4]
apratastat Hs Inhibition 7.5 pIC50 3
pIC50 7.5 (IC50 3.3x10-8 M) [3]
CGS-27023A Hs Inhibition 7.3 pIC50 5
pIC50 7.3 (IC50 5.6x10-8 M) [5]
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 [6].
Immuno Process Associations
Immuno Process:  Inflammation
GO Annotations:  Associated to 1 GO processes
GO:0050900 leukocyte migration TAS
Immuno Process:  Chemotaxis & migration
GO Annotations:  Associated to 1 GO processes
GO:0050900 leukocyte migration TAS
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:  2
Clinically-Relevant Mutations and Pathophysiology
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. Close DR. (2001) Matrix metalloproteinase inhibitors in rheumatic diseases. Ann. Rheum. Dis., 60 Suppl 3: iii62-7. [PMID:11890658]

2. 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]

3. 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]

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. 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. 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 21/03/2018. Accessed on 16/07/2018. IUPHAR/BPS Guide to PHARMACOLOGY, http://www.guidetopharmacology.org/GRAC/ObjectDisplayForward?objectId=1628.