ADAMTS5

Target id: 1678

Nomenclature: ADAMTS5

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 :     ADAMTS5 has curated GtoImmuPdb data

Gene and Protein Information
Species TM AA Chromosomal Location Gene Symbol Gene Name Reference
Human - 930 21q21.3 ADAMTS5 ADAM metallopeptidase with thrombospondin type 1 motif 5
Mouse - 930 16 C3.3 Adamts5 a disintegrin-like and metallopeptidase (reprolysin type) with thrombospondin type 1 motif, 5 (aggrecanase-2)
Rat - 928 11q11 Adamts5 ADAM metallopeptidase with thrombospondin type 1 motif, 5
Previous and Unofficial Names
ADAMTS11 | ADMP-2 | aggrecanase-2 | ADAM metallopeptidase with thrombospondin type 1 motif
Database Links
Specialist databases
MEROPS M12.225 (Hs)
Other databases
BRENDA
CATH/Gene3D
ChEMBL Target
Ensembl Gene
Entrez Gene
GenitoUrinary Development Molecular Anatomy Project
Human Protein Atlas
KEGG Enzyme
KEGG Gene
OMIM
RefSeq Nucleotide
RefSeq Protein
UniProtKB
Wikipedia
Enzyme Reaction
EC Number: 3.4.24.-

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
compound 15c [PMID: 21536437] Hs Inhibition 7.7 pIC50 1
pIC50 7.7 (IC50 2x10-8 M) [1]
Immunopharmacology Comments
ADAMTS4 and -5 diminish cartilage integrity in rheumatoid arthritis (RA) [2-3].
Immuno Disease Associations
Disease Name:  Rheumatoid arthritis
Disease Synonyms:  no synonynms
Comment:  ADAMTS5 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.
Disease X-refs:  Disease Ontology: DOID:8398
References:  4

References

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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]

How to cite this page

M12: Astacin/Adamalysin: ADAMTS5. Last modified on 16/03/2017. Accessed on 21/10/2017. IUPHAR/BPS Guide to PHARMACOLOGY, http://www.guidetopharmacology.org/GRAC/ObjectDisplayForward?objectId=1678.