Therapeutic Targets Database
BIDD Pharmainformatics Databases
 
   
   

 

TTD Target ID: TTDR00886

Target Information
NameCathepsin B    
Type of targetResearch target    
SynonymsAPP secretase    
APPS    
Cathepsin B1    
Cathepsin-B    
Cathepsins B    
Ctsb    
DiseaseAcute otitis media
[ICD9: 381.0, 381.1, 381.2, 381.3, 381.4   ICD10: H65, H66, H67]
[1]
Arthritis
[ICD9: 710-719   ICD10: M00-M25]
[2]
Ischemia
[ICD9: 459.89   ICD10: I99.8]
[3]
Tumor angiogenesis
[ICD9: 140-199, 210-229   ICD10: C00-C75, C7A, C7B, D10-D36, D3A]
[2]
BioChemical ClassHydrolases acting on peptide bonds (Peptidases)    
EC NumberEC 3.4.22.1
PathwayAntigen processing and presentation
Lysosome
UniProt IDP07858
PDB Structure1CSB; 1GMY; 1HUC; 1PBH; 2IPP; 2PBH; 3AI8; 3CBJ; 3CBK; 3K9M; 3PBH.    
FunctionThiol protease which is believed to participate in intracellular degradation and turnover of proteins. Has also been implicated in tumor invasion and metastasis.    
SequenceMWQLWASLCCLLVLANARSRPSFHPLSDELVNYVNKRNTTWQAGHNFYNVDMSYLKRLCG TFLGGPKPPQRVMFTEDLKLPASFDAREQWPQCPTIKEIRDQGSCGSCWAFGAVEAISDR ICIHTNAHVSVEVSAEDLLTCCGSMCGDGCNGGYPAEAWNFWTRKGLVSGGLYESHVGCR PYSIPPCEHHVNGSRPPCTGEGDTPKCSKICEPGYSPTYKQDKHYGYNSYSVSNSEKDIM AEIYKNGPVEGAFSVYSDFLLYKSGVYQHVTGEMMGGHAIRILGWGVENGTPYWLVANSW NTDWGDNGFFKILRGQDHCGIESEVVAGIPRTDQYWEKI
Related US Patent6,313,119
6,420,364
6,436,925
6,455,502
6,476,026
6,492,362
6,525,036
6,525,052
6,576,630
6,593,327
6,608,057
6,635,621
6,649,642
Target ValidationClick to Find Target Validation Information.    
Inhibitor (S)-1-benzylcyclopentyl 1-oxohexan-2-ylcarbamate[4]
1- (phenyl[5]
2-Aminoethanimidic Acid[6]
2-Pyridinethiol[7]
3-Amino-4-Oxybenzyl-2-Butanone[6]
3-Methylphenylalanine[6]
Ac-hPhe-Leu-Ala-LeuVSMe[8]
Ac-hPhe-Leu-Phe-LeuVSMe[8]
Bis (3-bromophenyl)[9]
Cbz-Ile-Leu-Ala-LeuVSMe[8]
Cbz-Ile-t-ButylhomoGlu-Ala-LeuVSMe[8]
Diphenylacetic Acid[6]
GNF-PF-5434[10]
Gold trichloride,   sodium chloride[11]
L-006235-1[12]
L-873724[13]
MDL-2170,   MDL-28170[14]
PEPSTATIN A[14]
Z-Ala-Leu-His-Agly-Ile-Val-OMe[15]
Z-Ala-Leu-Nal-Agly-Ile-Val-OMe[15]
Z-Ala-Leu-Phe-Agly-Ile-Val-OMe[15]
Z-Ala-Leu-Tyr (Me)-Agly-Ile-Val-OMe[15]
Z-Ala-Leu-lle-Agly-Ile-Val-NHBzl[15]
Z-Ala-Leu-lle-Agly-Ile-Val-OMe[15]
Z-Arg-Leu-Val-Agly-Ala-Gly-NH2[15]
Z-Arg-Leu-Val-Agly-Ile-Val-Trp-NH2[15]
Z-Arg-Leu-Val-Agly-Ileu-Val-OMe[15]
Z-Arg-Leu-Val-Agly-Trp-Val-Ala-NH2[15]
Z-Arg-Leu-Val-Agly-Val-Ala-NH2[15]
Z-leu-Val-Agly-Val-OBzl[15]
[ (3-Bromophenyl)-p-tolyl-ketone]thiosemicarbazone[16]
pTosyl-Glu (OtBu)-Ala-LeuVSMe[8]
Cross References 3D Structure
Related Literature
On-Line Medical Dictionary
Ref 1Cathepsin gene expression profile in rat acute pneumococcal otitis media. Laryngoscope. 2004 Jun;114(6):1032-6. To Reference
Ref 2Molecular regulation of human cathepsin B: implication in pathologies. Biol Chem. 2003 Jun;384(6):845-54. To Reference
Ref 3Evidence that inhibition of cathepsin-B contributes to the neuroprotective properties of caspase inhibitor Tyr-Val-Ala-Asp-chloromethyl ketone. J Biol Chem. 2001 Aug 31;276(35):32750-5. Epub 2001 Jun 26. To Reference
Ref 4Bioorg Med Chem Lett. 2006 Feb 15;16(4):978-83. Epub 2005 Nov 15.Semicarbazone-based inhibitors of cathepsin K, are they prodrugs for aldehyde inhibitors? To Reference
Ref 5Bioorg Med Chem Lett. 2008 May 1;18(9):2883-5. Epub 2008 Apr 8.Discovery of trypanocidal thiosemicarbazone inhibitors of rhodesain and TbcatB. To Reference
Ref 6Overington 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 7Nucleic Acids Res. 2011 January; 39(Database issue): D1035¨CD1041. DrugBank 3.0: a comprehensive resource for ¡®Omics¡¯ research on drugs To Reference
Ref 8J Med Chem. 2006 May 18;49(10):2953-68.Optimization of subsite binding to the beta5 subunit of the human 20S proteasome using vinyl sulfones and 2-keto-1,3,4-oxadiazoles: syntheses and cellular properties of potent, selective proteasome inhibitors. To Reference
Ref 9Bioorg Med Chem Lett. 2010 Nov 15;20(22):6610-5. Epub 2010 Sep 15.Functionalized benzophenone, thiophene, pyridine, and fluorene thiosemicarbazone derivatives as inhibitors of cathepsin L. To Reference
Ref 10Bioorg Med Chem. 2009 Feb 1;17(3):1064-70. Epub 2008 Feb 7.Substrate optimization for monitoring cathepsin C activity in live cells. To Reference
Ref 11Bioorg Med Chem Lett. 2004 Oct 18;14(20):5113-6.Inhibition of lysosomal cysteine proteases by chrysotherapeutic compounds: a possible mechanism for the antiarthritic activity of Au(I). To Reference
Ref 12J Med Chem. 2005 Dec 1;48(24):7535-43.Lysosomotropism of basic cathepsin K inhibitors contributes to increased cellular potencies against off-target cathepsins and reduced functional selectivity. To Reference
Ref 13Bioorg Med Chem Lett. 2007 Sep 1;17(17):4929-33. Epub 2007 Jun 10.The identification of potent, selective, and bioavailable cathepsin S inhibitors. To Reference
Ref 14J Med Chem. 2009 May 14;52(9):3093-7.Identification of 3-acetyl-2-aminoquinolin-4-one as a novel, nonpeptidic scaffold for specific calpain inhibitory activity. To Reference
Ref 15J Med Chem. 2002 Sep 12;45(19):4202-11.Azapeptides structurally based upon inhibitory sites of cystatins as potent and selective inhibitors of cysteine proteases. To Reference
Ref 16Bioorg Med Chem Lett. 2010 Feb 15;20(4):1415-9. Epub 2010 Jan 6.Design, synthesis, and biological evaluation of potent thiosemicarbazone based cathepsin L inhibitors. To Reference



 

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