Therapeutic Targets Database
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TTD Target ID: TTDR00847

Target Information
NameADAM 17    
Type of targetResearch target    
SynonymsA disintegrin and metalloproteinase domain 17    
CD156b antigen    
Snake venom-like protease    
TACE    
TNF alpha converting enzyme    
TNF-alpha convertase    
TNF-alpha converting enzyme    
DiseaseInflammatory bowel disease
[ICD9: 555, 556   ICD10: K50, K51]
[1]
Inflammatory diseases[2]
Neuroimmunological diseases[2]
Drug(s)DPC-333DiscontinuedInflammatory bowel disease, rheumatoid arthritis[3]
GW-3333PreclinicalChronic obstructive pulmonary disease[3]
BioChemical ClassHydrolases acting on peptide bonds (Peptidases)    
EC NumberEC 3.4.24.86
PathwayAlzheimer's disease
Epithelial cell signaling in Helicobacter pylori
Notch signaling pathway
UniProt IDP78536
PDB Structure1BKC; 1ZXC; 2A8H; 2DDF; 2FV5; 2FV9; 2I47; 2M2F; 2OI0; 3B92; 3CKI; 3E8R; 3EDZ; 3EWJ; 3G42; 3KMC; 3KME; 3L0T; 3L0V; 3LE9; 3LEA; 3LGP; 3O64.    
FunctionCleaves the membrane-bound precursor of tnf-alpha to its mature soluble form. Responsible for the proteolytic release of several other cell-surface proteins, including p75 tnf-receptor, interleukin 1 receptor type II and p55 tnf-receptor.    
SequenceMRQSLLFLTSVVPFVLAPRPPDDPGFGPHQRLEKLDSLLSDYDILSLSNIQQHSVRKRDL QTSTHVETLLTFSALKRHFKLYLTSSTERFSQNFKVVVVDGKNESEYTVKWQDFFTGHVV GEPDSRVLAHIRDDDVIIRINTDGAEYNIEPLWRFVNDTKDKRMLVYKSEDIKNVSRLQS PKVCGYLKVDNEELLPKGLVDREPPEELVHRVKRRADPDPMKNTCKLLVVADHRFYRYMG RGEESTTTNYLIELIDRVDDIYRNTSWDNAGFKGYGIQIEQIRILKSPQEVKPGEKHYNM AKSYPNEEKDAWDVKMLLEQFSFDIAEEASKVCLAHLFTYQDFDMGTLGLAYVGSPRANS HGGVCPKAYYSPVGKKNIYLNSGLTSTKNYGKTILTKEADLVTTHELGHNFGAEHDPDGL AECAPNEDQGGKYVMYPIAVSGDHENNKMFSNCSKQSIYKTIESKAQECFQERSNKVCGN SRVDEGEECDPGIMYLNNDTCCNSDCTLKEGVQCSDRNSPCCKNCQFETAQKKCQEAINA TCKGVSYCTGNSSECPPPGNAEDDTVCLDLGKCKDGKCIPFCEREQQLESCACNETDNSC KVCCRDLSGRCVPYVDAEQKNLFLRKGKPCTVGFCDMNGKCEKRVQDVIERFWDFIDQLS INTFGKFLADNIVGSVLVFSLIFWIPFSILVHCVDKKLDKQYESLSLFHPSNVEMLSSMD SASVRIIKPFPAPQTPGRLQPAPVIPSAPAAPKLDHQRMDTIQEDPSTDSHMDEDGFEKD PFPNSSTAAKSFEDLTDHPVTRSEKAASFKLQRQNRVDSKETEC
Related US Patent6,200,996
6,225,311
6,277,885
6,288,086
6,313,128
6,326,516
6,331,563
6,340,694
6,342,508
6,358,980
6,387,901
6,441,023
6,444,704
6,462,073
6,498,167
6,534,491
6,548,524
6,716,833
Target ValidationClick to Find Target Validation Information.    
QSAR ModelClick to Find Target QSAR Model.    
Inhibitor2- (4-bromophenylsulfonamido)-N-hydroxyacetamide[4]
2- (biphenyl-4-ylsulfonamido)-N-hydroxyacetamide[4]
Batimistat[5]
CGS-27023A[4]
CH4474[1]
CIPEMASTAT[6]
DPC-333[3]
GW-3333[3]
IK-682[7]
IK-682[8]
IM-491[9]
IM-491[7]
N-hydroxy-2- (4-methoxyphenylsulfonamido)acetamide[4]
N-hydroxy-3- (2-oxo-2H-chromen-3-yl)propanamide[10]
N-hydroxy-3- (6-methoxy-2-oxo-2H-chromen-3-yl)[10]
PKF-241-466[11]
PKF-242-484,   TNF-484[11]
SR-973[12]
TMI-05[13]
Cross References 3D Structure
Related Literature
On-Line Medical Dictionary
Ref 1Tumour necrosis factor-alpha converting enzyme (TACE) activity in human colonic epithelial cells. Clin Exp Immunol. 2004 Jan;135(1):146-53. To Reference
Ref 2Structural features and biochemical properties of TNF-alpha converting enzyme (TACE). J Neuroimmunol. 1997 Feb;72(2):127-9. To Reference
Ref 3Emerging drugs for the treatment of chronic obstructive pulmonary disease. Expert Opin Emerg Drugs. 2006 May;11(2):275-91. To Reference
Ref 4J Med Chem. 2010 Mar 25;53(6):2622-35.Potent arylsulfonamide inhibitors of tumor necrosis factor-alpha converting enzyme able to reduce activated leukocyte cell adhesion molecule shedding in cancer cell models. To Reference
Ref 5The secretases that cleave angiotensin converting enzyme and the amyloid precursor protein are distinct from tumour necrosis factor-alpha convertase. FEBS Lett. 1998 Jul 10;431(1):63-5. To Reference
Ref 6Bioorg Med Chem Lett. 2006 May 15;16(10):2632-6. Epub 2006 Mar 3.A cassette-dosing approach for improvement of oral bioavailability of dual TACE/MMP inhibitors. To Reference
Ref 7Bioorg Med Chem. 2008 Oct 1;16(19):8781-94. Epub 2008 Aug 29.Specific targeting of metzincin family members with small-molecule inhibitors: progress toward a multifarious challenge. To Reference
Ref 8Bioorg Med Chem Lett. 2007 Mar 1;17(5):1408-12. Epub 2006 Dec 3.A molecular modeling analysis of novel non-hydroxamate inhibitors of TACE. To Reference
Ref 9Bioorg Med Chem Lett. 2008 Jan 1;18(1):241-6. Epub 2007 Oct 30.Discovery of beta-benzamido hydroxamic acids as potent, selective, and orally bioavailable TACE inhibitors. To Reference
Ref 10Bioorg Med Chem. 2008 Jan 1;16(1):530-5. Epub 2007 Sep 14.Chromen-based TNF-alpha converting enzyme (TACE) inhibitors: design, synthesis, and biological evaluation. To Reference
Ref 11Bioorg Med Chem. 2009 Jan 15;17(2):444-59. Epub 2008 Dec 3.Current perspective of TACE inhibitors: a review. To Reference
Ref 12Bioorg Med Chem Lett. 2006 May 1;16(9):2357-63. Epub 2006 Feb 10.Synthesis and evaluation of succinoyl-caprolactam gamma-secretase inhibitors. To Reference
Ref 13Bioorg Med Chem Lett. 2006 Mar 15;16(6):1605-9. Epub 2006 Jan 19.Acetylenic TACE inhibitors. Part 3: Thiomorpholine sulfonamide hydroxamates. To Reference



 

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