ADAMTS4 | M12: Astacin/Adamalysin | IUPHAR/BPS Guide to PHARMACOLOGY

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target has curated data in GtoImmuPdb

Target id: 1677

Nomenclature: ADAMTS4

Family: M12: Astacin/Adamalysin

Annotation status:  image of a grey circle Awaiting annotation/under development. Please contact us if you can help with annotation.  » Email us

Gene and Protein Information
Species TM AA Chromosomal Location Gene Symbol Gene Name Reference
Human - 837 1q31-q32 ADAMTS4 ADAM metallopeptidase with thrombospondin type 1 motif 4
Mouse - 845 1 H3 Adamts4 a disintegrin-like and metallopeptidase (reprolysin type) with thrombospondin type 1 motif
Rat - 851 13q24 Adamts4 ADAM metallopeptidase with thrombospondin type 1 motif
Previous and Unofficial Names
ADMP-1 | aggrecanase-1 | ADAMTS-4 | ADAMTS-2 | ADAM metallopeptidase with thrombospondin type 1 motif, 4 | ADAM metallopeptidase with thrombospondin type 1 motif | a disintegrin-like and metallopeptidase (reprolysin type) with thrombospondin type 1 motif
Database Links
Specialist databases
MEROPS M12.221 (Hs)
Other databases
ChEMBL Target
Ensembl Gene
Entrez Gene
Human Protein Atlas
KEGG Enzyme
RefSeq Nucleotide
RefSeq Protein
Enzyme Reaction
EC Number:

Download all structure-activity data for this target as a CSV file

Key to terms and symbols View all chemical structures Click column headers to sort
Ligand Sp. Action Value Parameter Reference
compound 15c [PMID: 21536437] Hs Inhibition 8.9 pIC50 1
pIC50 8.9 (IC50 1.2x10-9 M) [1]
Immunopharmacology Comments
ADAMTS4 and -5 diminish cartilage integrity in rheumatoid arthritis (RA) by catalysing degradation of aggrecan [2-3].
Immuno Disease Associations
Disease Name:  Rheumatoid arthritis
Disease Synonyms:  no synonynms
Comment:  ADAMTS4 is involved in RA pathogenesis.
Disease X-refs:  Disease Ontology: DOID:7148
OMIM: 180300
References:  2-3
Disease Name:  Osteoarthritis
Disease Synonyms:  no synonynms
Comment:  ADAMTS4 and -5 are major players in development of OA. In human OA ADAMTS4 is induced by IL-1α and TNF-α, two cytokines involved in OA.
Disease X-refs:  Disease Ontology: DOID:8398
References:  4-5


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1. De Savi C, Pape A, Sawyer Y, Milne D, Davies C, Cumming JG, Ting A, Lamont S, Smith PD, Tart J et al.. (2011) Orally active achiral N-hydroxyformamide inhibitors of ADAM-TS4 (aggrecanase-1) and ADAM-TS5 (aggrecanase-2) for the treatment of osteoarthritis. Bioorg. Med. Chem. Lett., 21 (11): 3301-6. [PMID:21536437]

2. McInnes IB, Schett G. (2011) The pathogenesis of rheumatoid arthritis. N. Engl. J. Med., 365 (23): 2205-19. [PMID:22150039]

3. Porter S, Clark IM, Kevorkian L, Edwards DR. (2005) The ADAMTS metalloproteinases. Biochem. J., 386 (Pt 1): 15-27. [PMID:15554875]

4. Song RH, Tortorella MD, Malfait AM, Alston JT, Yang Z, Arner EC, Griggs DW. (2007) Aggrecan degradation in human articular cartilage explants is mediated by both ADAMTS-4 and ADAMTS-5. Arthritis Rheum., 56 (2): 575-85. [PMID:17265492]

5. Yamanishi Y, Boyle DL, Clark M, Maki RA, Tortorella MD, Arner EC, Firestein GS. (2002) Expression and regulation of aggrecanase in arthritis: the role of TGF-beta. J. Immunol., 168 (3): 1405-12. [PMID:11801682]

How to cite this page

M12: Astacin/Adamalysin: ADAMTS4. Last modified on 16/03/2017. Accessed on 27/05/2020. IUPHAR/BPS Guide to PHARMACOLOGY,