Therapeutic Targets Database
BIDD Pharmainformatics Databases
 
   
   

 

TTD Target ID: TTDR01031

Target Information
NameCathepsin L    
Type of targetResearch target    
SynonymsMEP    
Major excreted protein    
DiseaseAutoimmune diseases
[ICD9: 279.4   ICD10: D84.9, M35.9]
[1]
Melanoma
[ICD9: 172   ICD10: C43]
[1]
BioChemical ClassHydrolases acting on peptide bonds (Peptidases)    
EC NumberEC 3.4.22.15
PathwayAntigen processing and presentation
Lysosome
UniProt IDP07711
PDB Structure1CJL; 1CS8; 1ICF; 1MHW; 2NQD; 2VHS; 2XU1; 2XU3; 2XU4; 2XU5; 2YJ2; 2YJ8; 2YJ9; 2YJB; 2YJC; 3BC3; 3H89; 3H8B; 3H8C; 3HHA; 3HWN; 3IV2; 3K24; 3KSE; 3OF8; 3OF9; 4AXL; 4AXM.    
FunctionImportant for the overall degradation of proteins in lysosomes.    
SequenceMNPTLILAAFCLGIASATLTFDHSLEAQWTKWKAMHNRLYGMNEEGWRRAVWEKNMKMIE LHNQEYREGKHSFTMAMNAFGDMTSEEFRQVMNGFQNRKPRKGKVFQEPLFYEAPRSVDW REKGYVTPVKNQGQCGSCWAFSATGALEGQMFRKTGRLISLSEQNLVDCSGPQGNEGCNG GLMDYAFQYVQDNGGLDSEESYPYEATEESCKYNPKYSVANDTGFVDIPKQEKALMKAVA TVGPISVAIDAGHESFLFYKEGIYFEPDCSSEDMDHGVLVVGYGFESTESDNNKYWLVKN SWGEEWGMGGYVKMAKDRRNHCGIASAASYPTV
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 (3-Bromobenzoylpyridine)thiosemicarbazone[2]
(S)-1-benzylcyclopentyl 1-oxohexan-2-ylcarbamate[3]
(S)-tert-butyl 1-oxohexan-2-ylcarbamate[3]
1- (1,3-diphenylpropylidene)thiosemicarbazide[4]
1- (phenyl[4]
6- (benzylamino)-9-butyl-9H-purine-2-carbonitrile[5]
9-benzyl-6- (benzylamino)-9H-purine-2-carbonitrile[5]
BIPHENYL-4-YL-ACETALDEHYDE[6]
BOCEPREVIR[7]
Bis (3-Fluorophenyl)-ketone]thiosemicarbazone[8]
Bis (3-bromophenyl)[2]
Bis (3-bromophenyl)[2]
Cysteinesulfonic Acid[9]
L-006235-1[10]
L-873724[11]
MDL-2170,   MDL-28170[12]
N- (4-phenylbenzoyl)-phenylalanyl-glycine-nitrile[13]
N- (benzyloxycarbonyl)-leucyl-glycine-nitrile[13]
N- (tert-butoxycarbonyl)-isoleucyl-glycine-nitrile[13]
N- (tert-butoxycarbonyl)-leucyl-glycine-nitrile[13]
N- (tert-butoxycarbonyl)-methionyl-glycine-nitrile[13]
N- (tert-butoxycarbonyl)-norleucyl-glycine-nitrile[13]
N- (tert-butoxycarbonyl)-tyrosyl-glycine-nitrile[13]
N- (tert-butoxycarbonyl)-valyl-glycine-nitrile[13]
N-acetyl-phenylalanyl-glycine-nitrile[13]
N-benzoyl-phenylalanyl-glycine-nitrile[13]
PEPSTATIN A[12]
[ (3-Bromophenyl)-m-tolyl-ketone]thiosemicarbazone[8]
[ (3-Bromophenyl)-p-tolyl-ketone]thiosemicarbazone[8]
[2-Phenylacetophenone]thiosemicarbazone[2]
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 2Bioorg 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 3Bioorg 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 4Bioorg 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 5J Med Chem. 2008 Feb 14;51(3):545-52. Epub 2008 Jan 4.Development of potent purine-derived nitrile inhibitors of the trypanosomal protease TbcatB. To Reference
Ref 6Berman 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 7Antimicrob Agents Chemother. 2010 Jan;54(1):305-11. Epub 2009 Oct 19.MK-7009, a potent and selective inhibitor of hepatitis C virus NS3/4A protease. To Reference
Ref 8Bioorg 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
Ref 9Overington 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 10J 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 11Bioorg 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 12J 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 13J Med Chem. 2005 Dec 1;48(24):7688-707.Interaction of papain-like cysteine proteases with dipeptide-derived nitriles. To Reference



 

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