Target Information
Target General Infomation | |||||
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Target ID |
T30372
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Former ID |
TTDR00982
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Target Name |
Cruzipain
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Synonyms |
Congopain; Cruzaine; Cysteine proteinase cruzipain; Major cysteine proteinase
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Target Type |
Successful
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Disease | Helminth infection [ICD9: 001-139; ICD10: A00-B99] | ||||
Infection of P. falciparum [ICD9: 84; ICD10: B50-B54] | |||||
Function |
The cysteine protease may play an important role in the development and differentiation of the parasites at several stages of their life cycle.
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BioChemical Class |
Peptidase
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Target Validation |
T30372
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UniProt ID | |||||
EC Number |
EC 3.4.22.51
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Sequence |
MSGWARALLLAAVLVVMACLVPAATASLHAEETLTSQFAEFKQKHGRVYESAAEEAFRLS
VFRENLFLARLHAAANPHATFGVTPFSDLTREEFRSRYHNGAAHFAAAQERARVPVKVEV VGAPAAVDWRARGAVTAVKDQGQCGSCWAFSAIGNVECQWFLAGHPLTNLSEQMLVSCDK TDSGCSGGLMNNAFEWIVQENNGAVYTEDSYPYASGEGISPPCTTSGHTVGATITGHVEL PQDEAQIAAWLAVNGPVAVAVDASSWMTYTGGVMTSCVSEQLDHGVLLVGYNDSAAVPYW IIKNSWTTQWGEEGYIRIAKGSNQCLVKEEASSAVVGGPGPTPEPTTTTTTSAPGPSPSY FVQMSCTDAACIVGCENVTLPTGQCLLTTSGVSAIVTCGAETLTEEVFLTSTHCSGPSVR SSVPLNKCNRLLRGSVEFFCGSSSSGRLADVDRQRRHQPYHSRHRRL |
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Drugs and Mode of Action | |||||
Inhibitor | (3Z)-1H-indole-2,3-dione 3-thiosemicarbazone | Drug Info | [526832] | ||
1-(1-(3-nitrophenyl)propylidene)thiosemicarbazide | Drug Info | [528258] | |||
1-(3,4-dihydronaphthalen-1-yl)ethanone | Drug Info | [528258] | |||
1-(3-Methoxy-benzyl)-5-methyl-1H-indole-2,3-dione | Drug Info | [526832] | |||
1-(bis(3-bromophenyl)methylene)thiosemicarbazide | Drug Info | [528258] | |||
2-(cycloheptylamino)-2-oxoethyl 2-aminonicotinate | Drug Info | [530281] | |||
2-(trifluoromethyl)benzaldehyde thiosemicarbazone | Drug Info | [526354] | |||
2-methoxy-1-naphthaldehyde thiosemicarbazone | Drug Info | [526354] | |||
3',4'-dichloroacetophenonethiosemicarbazone | Drug Info | [531227] | |||
3'-bromopropiophenonethiosemicarbazone | Drug Info | [531227] | |||
3,4-dichlorobenzaldehyde thiosemicarbazone | Drug Info | [526354] | |||
3,5-dichlorobenzaldehyde thiosemicarbazone | Drug Info | [526354] | |||
3-(trifluoromethyl)benzaldehyde thiosemicarbazone | Drug Info | [526354] | |||
3-amino-5-(furan-2-yl)biphenyl-2,4-dicarbonitrile | Drug Info | [530512] | |||
3-chloro-N-(4-(phenyldiazenyl)phenyl)benzamide | Drug Info | [530512] | |||
5-(3,4-dichlorophenyl)-1H-pyrazol-3-ol | Drug Info | [530512] | |||
5-(4-bromophenyl)-2-furaldehyde thiosemicarbazone | Drug Info | [526354] | |||
5-Chloro-1-(4-chloro-benzyl)-1H-indole-2,3-dione | Drug Info | [526832] | |||
Benzoyl-Arginine-Alanine-Methyl Ketone | Drug Info | [551393] | |||
GNF-PF-4478 | Drug Info | [530968] | |||
K-777 | Drug Info | [530398] | |||
L-755507 | Drug Info | [530512] | |||
MANIDIPINE | Drug Info | [530877] | |||
N1,N4-bis(5-chloro-2-methylphenyl)succinamide | Drug Info | [530512] | |||
TRICLABENDAZOLE | Drug Info | [530877] | |||
VITAMIN K2 | Drug Info | [530877] | |||
WRR-112 | Drug Info | [551393] | |||
WRR-204 | Drug Info | [551393] | |||
WRR-99 | Drug Info | [551393] | |||
Binder | Vinylsulphones | Drug Info | [536135] | ||
References | |||||
Ref 521680 | ClinicalTrials.gov (NCT00157586) Delapril and Manidipine for Nephroprotection in Diabetes (DEMAND). U.S. National Institutes of Health. | ||||
Ref 540554 | (http://www.guidetopharmacology.org/) Nucleic Acids Res. 2015 Oct 12. pii: gkv1037. The IUPHAR/BPS Guide to PHARMACOLOGY in 2016: towards curated quantitative interactions between 1300 protein targets and 6000 ligands. (Ligand id: 3931). | ||||
Ref 526354 | J 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. | ||||
Ref 526832 | Bioorg Med Chem Lett. 2003 Oct 20;13(20):3527-30.Synthesis and evaluation of isatins and thiosemicarbazone derivatives against cruzain, falcipain-2 and rhodesain. | ||||
Ref 528258 | Bioorg 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. | ||||
Ref 530281 | J Med Chem. 2009 Aug 27;52(16):5005-8.Divergent modes of enzyme inhibition in a homologous structure-activity series. | ||||
Ref 530398 | Bioorg 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. | ||||
Ref 530512 | J 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. | ||||
Ref 530877 | J Med Chem. 2010 May 27;53(10):4259-65.Colloid formation by drugs in simulated intestinal fluid. | ||||
Ref 530968 | J Med Chem. 2010 Jul 8;53(13):4891-905.Complementarity between a docking and a high-throughput screen in discovering new cruzain inhibitors. | ||||
Ref 531227 | Bioorg 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. |
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