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

   GtoImmuPdb view: OFF :     ADAMTS4 has curated GtoImmuPdb data

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
Database Links
Specialist databases
MEROPS M12.221 (Hs)
Other databases
ChEMBL Target
Ensembl Gene
Entrez Gene
GenitoUrinary Development Molecular Anatomy Project
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 Affinity Units 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 18/01/2018. IUPHAR/BPS Guide to PHARMACOLOGY,