Therapeutic Targets Database
BIDD Pharmainformatics Databases
 
   
   

 

TTD Target ID: TTDR01266

Target Information
NameNeutrophil collagenase    
Type of targetSuccessful target    
SynonymsMMP-8    
Matrix metalloproteinase-8    
PMNL collagenase    
PMNL-CL    
DiseaseInflammatory diseases[1]
Osteoarthritis
[ICD9: 715   ICD10: M15-M19, M47]
[1]
Osteoporosis, unspecified
[ICD9: 733.0   ICD10: M80-M81]
[1]
Rheumatoid arthritis, unspecified
[ICD9: 710-719, 714   ICD10: M00-M25, M05-M06]
[1]
Tumors
[ICD9: 140-199, 210-229   ICD10: C00-C75, C7A, C7B, D10-D36, D3A]
[1]
Drug(s)DoxycyclineApprovedAdvanced gum disease, chronic periodontitis[2][3][4]
BioChemical ClassHydrolases acting on peptide bonds (Peptidases)    
EC NumberEC 3.4.24.34
UniProt IDP22894
PDB Structure1A85; 1A86; 1BZS; 1I73; 1I76; 1JAN; 1JAO; 1JAP; 1JAQ; 1JH1; 1JJ9; 1KBC; 1MMB; 1MNC; 1ZP5; 1ZS0; 1ZVX; 2OY2; 2OY4; 3DNG; 3DPE; 3DPF; 3TT4.    
FunctionCan degrade fibrillar type i, ii, and iii collagens.    
SequenceMFSLKTLPFLLLLHVQISKAFPVSSKEKNTKTVQDYLEKFYQLPSNQYQSTRKNGTNVIV EKLKEMQRFFGLNVTGKPNEETLDMMKKPRCGVPDSGGFMLTPGNPKWERTNLTYRIRNY TPQLSEAEVERAIKDAFELWSVASPLIFTRISQGEADINIAFYQRDHGDNSPFDGPNGIL AHAFQPGQGIGGDAHFDAEETWTNTSANYNLFLVAAHEFGHSLGLAHSSDPGALMYPNYA FRETSNYSLPQDDIDGIQAIYGLSSNPIQPTGPSTPKPCDPSLTFDAITTLRGEILFFKD RYFWRRHPQLQRVEMNFISLFWPSLPTGIQAAYEDFDRDLIFLFKGNQYWALSGYDILQG YPKDISNYGFPSSVQAIDAAVFYRSKTYFFVNDQFWRYDNQRQFMEPGYPKSISGAFPGI ESKVDAVFQQEHFFHVFSGPRYYAFDLIAQRVTRVARGNKWLNCRYG
Related US Patent6,310,084
Target ValidationClick to Find Target Validation Information.    
QSAR ModelClick to Find Target QSAR Model.    
Inhibitor1-Hydroxyamine-2-Isobutylmalonic Acid[5]
2- (Biphenyl-4-ylsulfonyl)N-hydroxybenzamide[6]
2- (biphenyl-4-ylsulfonamido)pentanedioic acid[7]
2-HYDROXYCARBAMOYL-4-METHYL-PENTANOIC ACID[8]
2-Thiomethyl-3-Phenylpropanoic Acid[5]
3- (4-Methoxy-benzenesulfonyl)-cyclohexanethiol[9]
3- (4-Methoxy-benzenesulfonyl)-propane-1-thiol[9]
3- (4-Phenoxy-benzenesulfonyl)-cyclohexanethiol[9]
3- (4-Phenoxy-benzenesulfonyl)-propane-1-thiol[9]
3-AMINO-AZACYCLOTRIDECAN-2-ONE[8]
4-amino-3- (4-[7]
BB-1101[10]
Batimastat[5]
CGS-27023A[11]
CIPEMASTAT[12]
Doxycycline[2][3][4]
Glycinamid[5]
IK-682[13]
ILOMASTAT[14]
METHYLAMINO-PHENYLALANYL-LEUCYL-HYDROXAMIC ACID[8]
N-Hydroxy-2- (4-phenoxy-benzenesulfonyl)benzamide[6]
Ro-32-3555[15]
Ro-37-9790[15]
SC-44463[16]
[2- (Biphenyl-4-sulfonyl)phenyl]acetic Acid[6]
Cross References 3D Structure
Related Literature
On-Line Medical Dictionary
Ref 1Drugs, their targets and the nature and number of drug targets. Nat Rev Drug Discov. 2006 Oct;5(10):821-34. To Reference
Ref 216498445 To Reference
Ref 317199549 To Reference
Ref 420370419 To Reference
Ref 5Overington JP, Al-Lazikani B, Hopkins AL: How many drug targets are there? Nat Rev Drug Discov. 2006 Dec;5(12):993-6. To Reference
Ref 6J Med Chem. 2009 Oct 22;52(20):6347-61.Design, synthesis, biological evaluation, and NMR studies of a new series of arylsulfones as selective and potent matrix metalloproteinase-12 inhibitors. To Reference
Ref 7Bioorg Med Chem. 2009 Feb 1;17(3):1101-8. Epub 2008 Mar 8.Ranking the selectivity of PubChem screening hits by activity-based protein profiling: MMP13 as a case study. To Reference
Ref 8Berman HM, Westbrook J, Feng Z, Gilliland G, Bhat TN, Weissig H, Shindyalov IN, Bourne PE: The Protein Data Bank. Nucleic Acids Res. 2000 Jan 1;28(1):235-42. To Reference
Ref 9Bioorg Med Chem Lett. 1999 Jul 5;9(13):1757-60.Synthesis and identification of conformationally constrained selective MMP inhibitors. To Reference
Ref 10J Med Chem. 1999 Nov 18;42(23):4890-908.New alpha-substituted succinate-based hydroxamic acids as TNFalpha convertase inhibitors. To Reference
Ref 11J Med Chem. 1999 Nov 4;42(22):4547-62.Design, synthesis, and biological evaluation of potent thiazine- and thiazepine-based matrix metalloproteinase inhibitors. To Reference
Ref 12J Med Chem. 2000 Feb 10;43(3):305-41.Protease inhibitors: current status and future prospects. To Reference
Ref 13J Med Chem. 2002 Nov 7;45(23):4954-7.Discovery of gamma-lactam hydroxamic acids as selective inhibitors of tumor necrosis factor alpha converting enzyme: design, synthesis, and structure-activity relationships. To Reference
Ref 14Bioorg. Med. Chem. Lett. 5(4):349-352 (1995) To Reference
Ref 15Bioorg. Med. Chem. Lett. 7(17):2299-2302 (1997) To Reference
Ref 16J 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. To Reference



 

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