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MMP8

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Immunopharmacology Ligand target has curated data in GtoImmuPdb

Target id: 1632

Nomenclature: MMP8

Family: M10: Matrix metallopeptidase

Contents:

Gene and Protein Information Click here for help
Species TM AA Chromosomal Location Gene Symbol Gene Name Reference
Human - 467 11q22.2 MMP8 matrix metallopeptidase 8
Mouse - 465 9 A1 Mmp8 matrix metallopeptidase 8
Rat - 466 8q11 Mmp8 matrix metallopeptidase 8
Previous and Unofficial Names Click here for help
PMNL collagenase | neutrophil collagenease | Collagenase-2 | CLG1 | matrix metallopeptidase 8 (neutrophil collagenase)
Database Links Click here for help
Specialist databases
MEROPS M10.002 (Hs)
Other databases
Alphafold P22894 (Hs), O70138 (Mm), O88766 (Rn)
BRENDA 3.4.24.34
CATH/Gene3D 3.40.390.10, 2.110.10.10
ChEMBL Target CHEMBL4588 (Hs), CHEMBL2312 (Rn)
DrugBank Target P22894 (Hs)
Ensembl Gene ENSG00000118113 (Hs), ENSMUSG00000005800 (Mm), ENSRNOG00000009907 (Rn)
Entrez Gene 4317 (Hs), 17394 (Mm), 63849 (Rn)
Human Protein Atlas ENSG00000118113 (Hs)
KEGG Enzyme 3.4.24.34
KEGG Gene hsa:4317 (Hs), mmu:17394 (Mm), rno:63849 (Rn)
OMIM 120355 (Hs)
Pharos P22894 (Hs)
RefSeq Nucleotide NM_002424 (Hs), NM_008611 (Mm), NM_022221 (Rn)
RefSeq Protein NP_002415 (Hs), NP_032637 (Mm), NP_071557 (Rn)
UniProtKB P22894 (Hs), O70138 (Mm), O88766 (Rn)
Wikipedia MMP8 (Hs)
Enzyme Reaction Click here for help
EC Number: 3.4.24.34

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
SL422 Small molecule or natural product Click here for species-specific activity table Hs Inhibition 9.3 pKi 6
⤷ pKi 9.3 (Ki 5x10-10 M) [6]
ONO-4817 Small molecule or natural product Hs Inhibition 9.0 pKi 7
⤷ pKi 9.0 (Ki 1.1x10-9 M) [7]
ilomastat Small molecule or natural product Click here for species-specific activity table Ligand has a PDB structure Hs Inhibition 9.0 pIC50 5
⤷ pIC50 9.0 (IC50 1.1x10-9 M) [5]
marimastat Small molecule or natural product Click here for species-specific activity table Ligand has a PDB structure Hs Inhibition 8.9 pIC50 1
⤷ pIC50 8.9 (IC50 1.3x10-9 M) [1]
CGS-27023A Small molecule or natural product Click here for species-specific activity table Ligand has a PDB structure Hs Inhibition 8.1 pIC50 3
⤷ pIC50 8.1 (IC50 7.7x10-9 M) [3]
MMP13 tracer [18F]5j Small molecule or natural product Click here for species-specific activity table Ligand is labelled Ligand is radioactive Hs Inhibition 5.9 pIC50 1
⤷ pIC50 5.9 (IC50 1.2x10-6 M) [1]
TP0556351 Peptide Click here for species-specific activity table Hs Inhibition 5.4 pIC50 5
⤷ pIC50 5.4 (IC50 3.725x10-6 M) [5]
doxycycline Small molecule or natural product Approved drug Click here for species-specific activity table Ligand has a PDB structure Immunopharmacology Ligand Guide to Malaria Pharmacology Ligand Hs Inhibition 4.6 pIC50 4
⤷ pIC50 4.6 (IC50 2.6x10-5 M) [4]
Inhibitor Comments
SL422 is a broad-spectrum inhibitor of MMP enzymes [6].
Immunopharmacology Comments
MMP8 is included in GtoImmuPdb based on its potential protective role in asthma.
Immuno Process Associations
Immuno Process:  Inflammation
Immuno Process:  Cellular signalling
Immuno Process:  Cytokine production & signalling
Immuno Process:  Immune regulation
Immuno Disease Associations
Disease Name:  Asthma
Disease Synonyms:  no synonynms
Comment:  MMP8 plays a protective role in asthma by promoting the clearance of recruited neutrophils.
Disease X-refs:  Disease Ontology: DOID:2841
OMIM: 600807
References:  2

References

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1. Buchler A, Ismailani US, MacMullin N, Abdirahman F, Adi M, Bi C, Jany C, Keillor JW, Rotstein BH. (2023) Quinazoline-2-Carboxamides as Selective PET Radiotracers for Matrix Metalloproteinase-13 Imaging in Atherosclerosis. J Med Chem, 66 (10): 6682-6696. [PMID:37158732]

2. Gueders MM, Balbin M, Rocks N, Foidart JM, Gosset P, Louis R, Shapiro S, Lopez-Otin C, Noël A, Cataldo DD. (2005) Matrix metalloproteinase-8 deficiency promotes granulocytic allergen-induced airway inflammation. J Immunol, 175 (4): 2589-97. [PMID:16081833]

3. 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]

4. Sepper R, Konttinen YT, Ding Y, Takagi M, Sorsa T. (1995) Human neutrophil collagenase (MMP-8), identified in bronchiectasis BAL fluid, correlates with severity of disease. Chest, 107 (6): 1641-7. [PMID:7781360]

5. 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]

6. Xue CB, Voss ME, Nelson DJ, Duan JJ, Cherney RJ, Jacobson IC, He X, Roderick J, Chen L, Corbett RL et al.. (2001) Design, synthesis, and structure-activity relationships of macrocyclic hydroxamic acids that inhibit tumor necrosis factor alpha release in vitro and in vivo. J Med Chem, 44 (16): 2636-60. [PMID:11472217]

7. Yamada A, Uegaki A, Nakamura T, Ogawa K. (2000) ONO-4817, an orally active matrix metalloproteinase inhibitor, prevents lipopolysaccharide-induced proteoglycan release from the joint cartilage in guinea pigs. Inflamm Res, 49 (4): 144-6. [PMID:10858013]

How to cite this page

M10: Matrix metallopeptidase: MMP8. Last modified on 10/05/2023. Accessed on 16/04/2024. IUPHAR/BPS Guide to PHARMACOLOGY, https://www.guidetopharmacology.org/GRAC/ObjectDisplayForward?objectId=1632.