Target Information
| Target General Infomation | |||||
|---|---|---|---|---|---|
| Target ID |
T79570
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| Former ID |
TTDR00696
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| Target Name |
ADAMTS-4
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| Gene Name |
ADAMTS4
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| Synonyms |
A disintegrin and metalloproteinase with thrombospondin motifs 4; ADAM-TS 4; ADAM-TS4; ADMP-1; Aggrecanase 1; ADAMTS4
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| Target Type |
Discontinued
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| Function |
Cleaves aggrecan, a cartilage proteoglycan, and may be involved in its turnover. May play an important role in the destruction of aggrecan in arthritic diseases. Could also be a critical factor in the exacerbation of neurodegeneration in Alzheimer disease. Cleaves aggrecan at the '392-Glu-|-Ala-393' site.
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| BioChemical Class |
Peptidase
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| Target Validation |
T79570
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| UniProt ID | |||||
| EC Number |
EC 3.4.24.82
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| Sequence |
MSQTGSHPGRGLAGRWLWGAQPCLLLPIVPLSWLVWLLLLLLASLLPSARLASPLPREEE
IVFPEKLNGSVLPGSGAPARLLCRLQAFGETLLLELEQDSGVQVEGLTVQYLGQAPELLG GAEPGTYLTGTINGDPESVASLHWDGGALLGVLQYRGAELHLQPLEGGTPNSAGGPGAHI LRRKSPASGQGPMCNVKAPLGSPSPRPRRAKRFASLSRFVETLVVADDKMAAFHGAGLKR YLLTVMAAAAKAFKHPSIRNPVSLVVTRLVILGSGEEGPQVGPSAAQTLRSFCAWQRGLN TPEDSDPDHFDTAILFTRQDLCGVSTCDTLGMADVGTVCDPARSCAIVEDDGLQSAFTAA HELGHVFNMLHDNSKPCISLNGPLSTSRHVMAPVMAHVDPEEPWSPCSARFITDFLDNGY GHCLLDKPEAPLHLPVTFPGKDYDADRQCQLTFGPDSRHCPQLPPPCAALWCSGHLNGHA MCQTKHSPWADGTPCGPAQACMGGRCLHMDQLQDFNIPQAGGWGPWGPWGDCSRTCGGGV QFSSRDCTRPVPRNGGKYCEGRRTRFRSCNTEDCPTGSALTFREEQCAAYNHRTDLFKSF PGPMDWVPRYTGVAPQDQCKLTCQAQALGYYYVLEPRVVDGTPCSPDSSSVCVQGRCIHA GCDRIIGSKKKFDKCMVCGGDGSGCSKQSGSFRKFRYGYNNVVTIPAGATHILVRQQGNP GHRSIYLALKLPDGSYALNGEYTLMPSPTDVVLPGAVSLRYSGATAASETLSGHGPLAQP LTLQVLVAGNPQDTRLRYSFFVPRPTPSTPRPTPQDWLHRRAQILEILRRRPWAGRK |
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| Drugs and Mode of Action | |||||
| Drug(s) | SC-44463 | Drug Info | Terminated | Discovery agent | [1] |
| Inhibitor | (R)-2-(biphenyl-4-sulfonylamino)-propionic acid | Drug Info | [2] | ||
| MMI270 | Drug Info | [2] | |||
| SC-44463 | Drug Info | [3] | |||
| Pathways | |||||
| Reactome | Degradation of the extracellular matrix | ||||
| O-glycosylation of TSR domain-containing proteins | |||||
| WikiPathways | Endochondral Ossification | ||||
| References | |||||
| REF 1 | Trusted, scientifically sound profiles of drug programs, clinical trials, safety reports, and company deals, written by scientists. Springer. 2015. Adis Insight (drug id 800007717) | ||||
| REF 2 | Bioorg Med Chem Lett. 2006 Jan 15;16(2):311-6. Epub 2005 Nov 3.Synthesis and biological evaluation of biphenylsulfonamide carboxylate aggrecanase-1 inhibitors. | ||||
| REF 3 | J Med Chem. 2001 Oct 11;44(21):3347-50.Design and synthesis of a series of (2R)-N(4)-hydroxy-2-(3-hydroxybenzyl)-N(1)- [(1S,2R)-2-hydroxy-2,3-dihydro-1H-inden-1-yl]butanediamide derivatives as potent, selective, and orally bioavailable aggrecanase inhibitors. | ||||
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