MMP2

Target id: 1629

Nomenclature: MMP2

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 2matrix metalloproteinase 2matrix metalloproteinase 2

   GtoImmuPdb view: OFF :     MMP2 has curated GtoImmuPdb data

Gene and Protein Information
Species TM AA Chromosomal Location Gene Symbol Gene Name Reference
Human - 660 16q13-q21 MMP2 matrix metallopeptidase 2
Mouse - 662 8 C5 Mmp2 matrix metallopeptidase 2
Rat - 662 19p11 Mmp2 matrix metallopeptidase 2
Previous and Unofficial Names
TBE- 1 | gelatinase A | CLG4 | CLG4A | matrix metallopeptidase 2 (gelatinase A, 72kDa gelatinase, 72kDa type IV collagenase)
Database Links
Specialist databases
MEROPS M10.003 (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
UniProtKB
Wikipedia
Enzyme Reaction
EC Number: 3.4.24.24

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
tanomastat Hs Inhibition 8.0 pKi 3
pKi 8.0 (Ki 1x10-8 M) [3]
SB-3CT Hs Inhibition 7.9 pKi 1
pKi 7.9 (Ki 1.39x10-8 M) [1]
AZD6605 Hs Inhibition 8.5 pIC50 5
pIC50 8.5 (IC50 3x10-9 M) [5]
ilomastat Hs Inhibition 8.1 pIC50 4
pIC50 8.1 (IC50 7x10-9 M) [4]
CGS-27023A Hs Inhibition 7.6 pIC50 6
pIC50 7.6 (IC50 2.5x10-8 M) [6]
tiludronic acid Hs Inhibition 5.1 pIC50 7
pIC50 5.1 (IC50 7.2x10-6 M) [7]
ARP100 Hs Inhibition - - 8
[8]
Immunopharmacology Comments
MMP2 is included in GtoImmuPdb based on its potential involvement in asthma.
Immuno Process Associations
Immuno Process:  Inflammation
GO Annotations:  Associated to 1 GO processes, IEA only
click arrow to show/hide IEA associations
GO:0045089 positive regulation of innate immune response IEA
Immuno Process:  Immune regulation
GO Annotations:  Associated to 1 GO processes, IEA only
click arrow to show/hide IEA associations
GO:0045089 positive regulation of innate immune response IEA
Immuno Disease Associations
Disease Name:  Asthma
Disease Synonyms:  no synonynms
Comment:  MMP2 and MMP9 can promote the egress of inflammatory cells into airway lumen, suggesting a protective anti-inflammatory role in asthma. MMP2/MMP9 gelatinolytic activity is elevated in the sputum of asthmatic patients
Disease X-refs:  Disease Ontology: DOID:2841
OMIM: 600807
References:  2
Clinically-Relevant Mutations and Pathophysiology
Disease:  Multicentric osteolysis, nodulosis, and arthropathy
Synonyms: Nodulosis-arthropathy-osteolysis syndrome [Orphanet: ORPHA85196]
OMIM: 259600
Orphanet: ORPHA85196
Disease:  Winchester syndrome
OMIM: 277950
Orphanet: ORPHA3460

References

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1. Brown S, Bernardo MM, Li Z-H, Kotra LP, Tanaka Y, Fridman R, Mobashery S. (2000) Potent and Selective Mechanism-Based Inhibition of Gelatinases. J. Am. Chem. Soc., 122: 6799-6800.

2. Cataldo D, Munaut C, Noël A, Frankenne F, Bartsch P, Foidart JM, Louis R. (2000) MMP-2- and MMP-9-linked gelatinolytic activity in the sputum from patients with asthma and chronic obstructive pulmonary disease. Int. Arch. Allergy Immunol., 123 (3): 259-67. [PMID:11112863]

3. Fisher JF, Mobashery S. (2006) Recent advances in MMP inhibitor design. Cancer Metastasis Rev., 25 (1): 115-36. [PMID:16680577]

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. 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

6. 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]

7. Tauro M, Laghezza A, Loiodice F, Agamennone M, Campestre C, Tortorella P. (2013) Arylamino methylene bisphosphonate derivatives as bone seeking matrix metalloproteinase inhibitors. Bioorg. Med. Chem., 21 (21): 6456-65. [PMID:24071448]

8. Tuccinardi T, Martinelli A, Nuti E, Carelli P, Balzano F, Uccello-Barretta G, Murphy G, Rossello A. (2006) Amber force field implementation, molecular modelling study, synthesis and MMP-1/MMP-2 inhibition profile of (R)- and (S)-N-hydroxy-2-(N-isopropoxybiphenyl-4-ylsulfonamido)-3-methylbutanamides. Bioorg. Med. Chem., 14 (12): 4260-76. [PMID:16483784]

How to cite this page

M10: Matrix metallopeptidase: MMP2. Last modified on 19/04/2017. Accessed on 20/06/2018. IUPHAR/BPS Guide to PHARMACOLOGY, http://www.guidetopharmacology.org/GRAC/ObjectDisplayForward?objectId=1629.