Therapeutic Targets Database
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TTD Target ID: TTDR00103

Target Information
NameNonstructural protein NS3    
Type of targetClinical trial target    
SynonymsHCV NS3 RNA helicase    
Hepacivirin    
Hepatitis C Virus RNA Helicase    
Hepatitis C virus NS3 serine proteinase    
NS3    
NS3 protease    
NS3 protein    
Nonstructural protein 3    
ORF-C    
P70    
Protease/helicase NS3    
RNA helicase    
Ribonucleic acid (RNA) helicase    
SM protein    
DiseaseHepatitis C
[ICD9: 070.4, 070.5, 070.70   ICD10: B17.1, B18.2]
[1][2][3]
Viral infection, unspecified
[ICD9: 001-139, 042-075   ICD10: A00-B99, A80-A99, B00-B34]
[4][5]
BioChemical ClassProtease    
EC NumberEC 3.4.21.98
UniProt IDP06591
P26664
PDB Structure1RTL; 2A4G; 2GVF; 3EYD.    
SequenceAPITAYAQQTRGLLGCIITSLTGRDKNQVEGEVQIVSTAAQTFLATCINGVCWTVYHGAG TRTIASPKGPVIQMYTNVDQDLVGWPAPQGSRSLTPCTCGSSDLYLVTRHADVIPVRRRG DSRGSLLSPRPISYLKGSSGGPLLCPAGHAVGIFRAAVCTRGVAKAVDFIPVENLETTMR SPVFTDNSSPPVVPQSFQVAHLHAPTGSGKSTKVPAAYAAQGYKVLVLNPSVAATLGFGA YMSKAHGIDPNIRTGVRTITTGSPITYSTYGKFLADGGCSGGAYDIIICDECHSTDATSI LGIGTVLDQAETAGARLVVLATATPPGSVTVPHPNIEEVALSTTGEIPFYGKAIPLEVIK GGRHLIFCHSKKKCDELAAKLVALGINAVAYYRGLDVSVIPTSGDVVVVATDALMTGYTG DFDSVIDCNTCVTQTVDFSLDPTFTIETITLPQDAVSRTQRRGRTGRGKPGIYRFVAPGE RPSGMFDSSVLCECYDAGCAWYELTPAETTVRLRAYMNTPGLPVCQDHLEFWEGVFTGLT HIDAHFLSQTKQSGENLPYLVAYQATVCARAQAPPPSWDQMWKCLIRLKPTLHGPTPLLY RLGAVQNEITLTHPVTKYIMTCMSADLEVVT
Related US Patent6,608,067
6,617,309
6,642,204
6,653,295
Target ValidationClick to Find Target Validation Information.    
Inhibitor2,4,6-Trihydroxy-3-nitro-N-tridecyl-benzamide[6]
Ac-Glu-Cha-Cys[7]
AcAsp-D-Gla-Leu-Ile-Cha-Cys[6]
AcAsp-D-Glu-Leu-Glu-Cha-Cys[7]
AcAsp-D-Glu-Leu-Glu-Cha-Cys[6]
AcAsp-Gla-Leu-Ile-Cha-Cys[7]
AcAsp-Glu-Cha-Val-Prb-Cpg[6]
AcAsp-Glu-Cha-Val-Prb-Cys[6]
AcAsp-Glu-Dif-Glu-Cha-Cys[6]
AcAsp-Glu-Dif-Glu-Cha-Fab[6]
AcAsp-Glu-Dif-Ile-Cha-Cys[7]
AcAsp-Glu-Dif-Ile-Cha-Cys-Iqc-Nle-Thr-TyrNH2[6]
AcAsp-Glu-Dif-Ile-Cha-Cys-Pro-Cha-Asp-ValNH2[6]
AcAsp-Glu-Dif-Ile-Cha-Cys-Pro-Nle-Asp-ValNH2[6]
AcAsp-Glu-Dif-Lys-Cha-Cys[7]
AcAsp-Glu-Leu-Glu-Cha-Cys[7]
AcAsp-Glu-Leu-Glu-Cha-Cys[6]
AcAsp-Glu-Met-Glu-Cha-Cys[7]
AcAsp-Glu-Met-Glu-Glu-Cys[6]
AcAsp-Glu-Met-Glu-Nal-Cyse[7]
AcDif-Glu-Cha-Cys[7]
AcDif-Ile-Cha-Cys[7]
AcGlu-Asp-Val-Val-Leu-Cys-Iqc-Nle-Thr-TyrNH2[6]
AcGlu-Dif-Glu-Cha-Cys[7]
AcGlu-Dif-Ile-Cha-Cys[7]
Asp-D-Glu-Leu-Glu-Cha-Cys[7]
Azapeptide[8]
Azapeptide[8]
Azapeptide[8]
Azapeptide[8]
Azapeptide[8]
Azapeptide[8]
Azapeptide[8]
Azapeptide[8]
Azapeptide[8]
Azapeptide[8]
Azapeptide derivative[9]
Azapeptide derivative[9]
Azapeptide derivative[9]
Azapeptide derivative[9]
Azapeptide derivative[9]
Azapeptide derivative[9]
Azapeptide derivative[9]
Azapeptide derivative[9]
Azapeptide derivative[9]
Azapeptide derivative[9]
Azapeptide derivative[9]
Azapeptide derivative[9]
Azapeptide derivative[9]
Azapeptide derivative[9]
Azapeptide derivative[9]
Azapeptide derivative[9]
Azapeptide derivative[9]
Azapeptide derivative[9]
Azapeptide derivative[9]
Azapeptide derivative[9]
Azapeptide derivative[9]
Azapeptide derivative[9]
BILN-2061[10]
Boc-Ile-Leu-L- (difluoro)aminobutyric aid[6]
Cbz-Ile-Leu-L- (difluoro)aminobutyric acid[6]
GNF-PF-3464[11]
PATULIN[6]
Peptide Boronic Acid analogue[12]
Peptide Boronic Acid analogue[12]
Peptide Boronic Acid analogue[12]
Peptide Boronic Acid analogue[12]
Peptide Boronic Acid analogue[12]
Peptide Boronic Acid analogue[12]
Peptide Boronic Acid analogue[12]
Peptide Boronic Acid analogue[12]
Peptide Boronic Acid analogue[12]
Peptide Boronic Acid analogue[12]
Peptide Boronic Acid analogue[12]
Peptide Boronic Acid analogue[12]
Peptide Boronic Acid analogue[12]
Peptide Boronic Acid analogue[12]
Peptide Boronic Acid analogue[12]
Peptide Boronic Acid analogue[12]
Peptide Boronic Acid analogue[12]
Peptide Boronic Acid analogue[12]
Peptide Boronic Acid analogue[12]
Peptide Boronic Acid analogue[12]
Peptide Boronic Acid analogue[12]
Peptide Boronic Acid analogue[12]
Peptide Boronic Acid analogue[12]
Peptide Boronic Acid analogue[12]
Peptide Boronic Acid analogue[12]
Peptide Boronic Acid analogue[12]
Peptide Boronic Acid analogue[12]
Peptide Boronic Acid analogue[12]
Peptide Boronic Acid analogue[12]
Peptide Boronic Acid analogue[12]
Peptide Boronic Acid analogue[12]
Peptide Boronic Acid analogue[12]
SCH-68631[6]
AptamerSE RNA[13]
Cross References 3D Structure
Related Literature
On-Line Medical Dictionary
Ref 1Characterization of ATPase activity of a hepatitis C virus NS3 helicase domain, and analysis involving mercuric reagents. J Biochem. 2003 Oct;134(4):505-11. To Reference
Ref 2A novel high throughput screening assay for HCV NS3 serine protease inhibitors. J Virol Methods. 2003 Feb;107(2):245-55. To Reference
Ref 3The hepatitis C viral NS3 protein is a processive DNA helicase with cofactor enhanced RNA unwinding. EMBO J. 2002 Mar 1;21(5):1168-76. To Reference
Ref 4Hepatitis C virus NS3 ATPase/helicase: an ATP switch regulates the cooperativity among the different substrate binding sites. Biochemistry. 2002 Aug 13;41(32):10332-42. To Reference
Ref 5Design, high-level expression, purification and characterization of soluble fragments of the hepatitis C virus NS3 RNA helicase suitable for NMR-based drug discovery methods and mechanistic studies. Protein Eng. 2001 Aug;14(8):573-82. To Reference
Ref 6J Med Chem. 2005 Jan 13;48(1):1-20.Control of hepatitis C: a medicinal chemistry perspective. To Reference
Ref 7Bioorg Med Chem Lett. 2001 Jan 22;11(2):203-6.Inhibition of hepatitis C virus NS3 protease activity by product-based peptides is dependent on helicase domain. To Reference
Ref 8Bioorg Med Chem Lett. 2002 Apr 8;12(7):1005-8.Azapeptides as inhibitors of the hepatitis C virus NS3 serine protease. To Reference
Ref 9J Med Chem. 2004 Jul 15;47(15):3788-99.Novel azapeptide inhibitors of hepatitis C virus serine protease. To Reference
Ref 10Antiviral efficacy of NS3-serine protease inhibitor BILN-2061 in patients with chronic genotype 2 and 3 hepatitis C. Hepatology. 2005 Apr;41(4):832-5. To Reference
Ref 11Bioorg Med Chem Lett. 2010 Dec 15;20(24):7331-6. Epub 2010 Oct 21.In silico identification and biochemical evaluation of novel inhibitors of NRH:quinone oxidoreductase 2 (NQO2). To Reference
Ref 12Bioorg Med Chem Lett. 2002 Nov 4;12(21):3199-202.P1 Phenethyl peptide boronic acid inhibitors of HCV NS3 protease. To Reference
Ref 13Therapeutic applications of aptamers. Expert Opin Investig Drugs. 2008 Jan;17(1):43-60. To Reference



 

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