Therapeutic Targets Database
BIDD Pharmainformatics Databases
 
   
   

 

TTD Target ID: TTDR00982

Target Information
NameCruzipain    
Type of targetResearch target    
SynonymsCongopain    
Cruzaine    
Cysteine proteinase cruzipain    
Major cysteine proteinase    
DiseaseChagas' disease
[ICD9: 086   ICD10: B57]
[1]
Trypanolytic infections
[ICD9: 001-139   ICD10: A00-B99]
[2]
BioChemical ClassHydrolases acting on peptide bonds (Peptidases)    
EC NumberEC 3.4.22.51
UniProt IDP25779
PDB Structure1AIM; 1EWL; 1EWM; 1EWO; 1EWP; 1F29; 1F2A; 1F2B; 1F2C; 1ME3; 1ME4; 1U9Q; 2AIM; 2OZ2; 3HD3; 3I06; 3IUT; 3KKU; 3LXS.    
SequenceMSGWARALLLAAVLVVMACLVPAATASLHAEETLTSQFAEFKQKHGRVYESAAEEAFRLS VFRENLFLARLHAAANPHATFGVTPFSDLTREEFRSRYHNGAAHFAAAQERARVPVKVEV VGAPAAVDWRARGAVTAVKDQGQCGSCWAFSAIGNVECQWFLAGHPLTNLSEQMLVSCDK TDSGCSGGLMNNAFEWIVQENNGAVYTEDSYPYASGEGISPPCTTSGHTVGATITGHVEL PQDEAQIAAWLAVNGPVAVAVDASSWMTYTGGVMTSCVSEQLDHGVLLVGYNDSAAVPYW IIKNSWTTQWGEEGYIRIAKGSNQCLVKEEASSAVVGGPGPTPEPTTTTTTSAPGPSPSY FVQMSCTDAACIVGCENVTLPTGQCLLTTSGVSAIVTCGAETLTEEVFLTSTHCSGPSVR SSVPLNKCNRLLRGSVEFFCGSSSSGRLADVDRQRRHQPYHSRHRRL
Target ValidationClick to Find Target Validation Information.    
Inhibitor (3Z)-1H-indole-2,3-dione 3-thiosemicarbazone[3]
1- (1-[4]
1- (3,4-dihydronaphthalen-1-yl)ethanone[4]
1- (3-Methoxy-benzyl)-5-methyl-1H-indole-2,3-dione[3]
1- (bis[4]
2- (cycloheptylamino)-2-oxoethyl 2-aminonicotinate[5]
2- (trifluoromethyl)benzaldehyde thiosemicarbazone[6]
2-methoxy-1-naphthaldehyde thiosemicarbazone[6]
3',4'-dichloroacetophenonethiosemicarbazone[7]
3'-bromopropiophenonethiosemicarbazone[7]
3,4-dichlorobenzaldehyde thiosemicarbazone[6]
3,5-dichlorobenzaldehyde thiosemicarbazone[6]
3- (trifluoromethyl)benzaldehyde thiosemicarbazone[6]
3-amino-5- (furan-2-yl)biphenyl-2,4-dicarbonitrile[8]
3-chloro-N- (4-[8]
5- (3,4-dichlorophenyl)-1H-pyrazol-3-ol[8]
5- (4-bromophenyl)-2-furaldehyde thiosemicarbazone[6]
5-Chloro-1- (4-chloro-benzyl)-1H-indole-2,3-dione[3]
Benzoyl-Arginine-Alanine-Methyl Ketone[9]
GNF-PF-4478[10]
K-777[11]
L-755507[8]
MANIDIPINE[12]
N1,N4-bis (5-chloro-2-methylphenyl)succinamide[8]
TRICLABENDAZOLE[12]
VITAMIN K2[12]
WRR-112[9]
WRR-204[9]
WRR-99[9]
BinderVinylsulphones[13]
Cross References 3D Structure
Related Literature
On-Line Medical Dictionary
Ref 1Proteinases of Trypanosoma cruzi: patential targets for the chemotherapy of Changas desease. Curr Top Med Chem. 2002 Nov;2(11):1261-71. To Reference
Ref 2Congopain from Trypanosoma congolense: drug target and vaccine candidate. Biol Chem. 2002 May;383(5):739-49. To Reference
Ref 3Bioorg Med Chem Lett. 2003 Oct 20;13(20):3527-30.Synthesis and evaluation of isatins and thiosemicarbazone derivatives against cruzain, falcipain-2 and rhodesain. To Reference
Ref 4Bioorg Med Chem Lett. 2006 Aug 15;16(16):4405-9. Epub 2006 Jun 15.Design, synthesis, and biochemical evaluation of novel cruzain inhibitors with potential application in the treatment of Chagas' disease. To Reference
Ref 5J Med Chem. 2009 Aug 27;52(16):5005-8.Divergent modes of enzyme inhibition in a homologous structure-activity series. To Reference
Ref 6J Med Chem. 2002 Jun 20;45(13):2695-707.Synthesis and structure-activity relationship study of potent trypanocidal thio semicarbazone inhibitors of the trypanosomal cysteine protease cruzain. To Reference
Ref 7Bioorg Med Chem. 2010 Nov 15;18(22):7826-35. Epub 2010 Sep 29.Studies toward the structural optimization of novel thiazolylhydrazone-based potent antitrypanosomal agents. To Reference
Ref 8J Med Chem. 2010 Jan 14;53(1):37-51.Quantitative analyses of aggregation, autofluorescence, and reactivity artifacts in a screen for inhibitors of a thiol protease. 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. 2010 Jul 8;53(13):4891-905.Complementarity between a docking and a high-throughput screen in discovering new cruzain inhibitors. To Reference
Ref 11Bioorg Med Chem Lett. 2009 Nov 1;19(21):6218-21. Epub 2009 Sep 3.Novel non-peptidic vinylsulfones targeting the S2 and S3 subsites of parasite cysteine proteases. To Reference
Ref 12J Med Chem. 2010 May 27;53(10):4259-65.Colloid formation by drugs in simulated intestinal fluid. To Reference
Ref 13Opportunities and challenges in antiparasitic drug discovery. Nat Rev Drug Discov. 2005 Sep;4(9):727-40. To Reference



 

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