MMP2 | M10: Matrix metallopeptidase | IUPHAR Guide to IMMUNOPHARMACOLOGY

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MMP2

  Target has curated data in GtoImmuPdb

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 2; matrix metalloproteinase 2; matrix metalloproteinase 2

Contents:

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 | CLG4A | CLG4 | matrix metallopeptidase 2 (gelatinase A, 72kDa gelatinase, 72kDa type IV collagenase)
Database Links
Specialist databases
MEROPS M10.003 (Hs)
Other databases
BRENDA 3.4.24.24
CATH/Gene3D 3.40.390.10, 2.10.10.10, 2.110.10.10, 1.10.101.10
ChEMBL Target CHEMBL333 (Hs), CHEMBL3095 (Mm), CHEMBL1075175 (Rn)
DrugBank Target P08253 (Hs)
Ensembl Gene ENSG00000087245 (Hs), ENSMUSG00000031740 (Mm), ENSRNOG00000016695 (Rn)
Entrez Gene 4313 (Hs), 17390 (Mm), 81686 (Rn)
Human Protein Atlas ENSG00000087245 (Hs)
KEGG Enzyme 3.4.24.24
KEGG Gene hsa:4313 (Hs), mmu:17390 (Mm), rno:81686 (Rn)
OMIM 120360 (Hs)
Orphanet ORPHA123439 (Hs)
Pharos P08253 (Hs)
RefSeq Nucleotide NM_001127891 (Hs), NM_004530 (Hs), NM_008610 (Mm), NM_031054 (Rn)
RefSeq Protein NP_004521 (Hs), NP_001121363 (Hs), NP_032636 (Mm), NP_112316 (Rn)
UniProtKB P08253 (Hs), P33434 (Mm), P33436 (Rn)
Wikipedia MMP2 (Hs)
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 Value Parameter 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]
(R)-ND-336 Hs Inhibition 6.9 pKi 6
⤷ pKi 6.9 (Ki 1.27x10-7 M) [6]
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 7
⤷ pIC50 7.6 (IC50 2.5x10-8 M) [7]
tiludronic acid Hs Inhibition 5.1 pIC50 8
⤷ pIC50 5.1 (IC50 7.2x10-6 M) [8]
ARP100 Hs Inhibition - - 9
⤷ [9]
Immunopharmacology Comments
MMP2 is included in GtoImmuPdb based on its potential involvement in asthma.
Immuno Process Associations
Immuno Process:  Cytokine production & signalling
GO Annotations:  Associated to 4 GO processes
GO:0019221 cytokine-mediated signaling pathway TAS
GO:0034097 response to cytokine IEP
GO:0071345 cellular response to cytokine stimulus IEP
GO:0071347 cellular response to interleukin-1 IEP
Immuno Process:  Immune regulation
GO Annotations:  Associated to 1 GO processes
GO:0045089 positive regulation of innate immune response IDA
Immuno Process:  Inflammation
GO Annotations:  Associated to 1 GO processes
GO:0045089 positive regulation of innate immune response IDA
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. Nguyen TT, Ding D, Wolter WR, Pérez RL, Champion MM, Mahasenan KV, Hesek D, Lee M, Schroeder VA, Jones JI et al.. (2018) Validation of Matrix Metalloproteinase-9 (MMP-9) as a Novel Target for Treatment of Diabetic Foot Ulcers in Humans and Discovery of a Potent and Selective Small-Molecule MMP-9 Inhibitor That Accelerates Healing. J. Med. Chem., 61 (19): 8825-8837. [PMID:30212201]

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. 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]

9. 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 22/05/2020. Accessed on 13/07/2020. IUPHAR/BPS Guide to PHARMACOLOGY, http://www.guidetoimmunopharmacology.org/GRAC/ObjectDisplayForward?objectId=1629.