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Information on EC 3.4.21.98 - hepacivirin and Organism(s) Hepatitis C virus genotype 1a and UniProt Accession P27958
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3.4.21.98 hepacivirinSpecify your search results
Word Map
- 3.4.21.98
- ribavirin
-
virologic
- helicase
-
direct-acting
-
replicons
- telaprevir
- cirrhosis
-
pegylated
-
anti-hcv
- boceprevir
-
hcv-infected
-
resistance-associated
- simeprevir
-
macrocyclic
- dengue
-
peginterferon
- sofosbuvir
-
subgenomic
-
unwind
-
treatment-naive
-
treatment-experienced
-
interferon-free
- flaviviridae
- mavs
- flavivirus
-
hcv-specific
- rbv
-
daclatasvir
- asunaprevir
- ntpase
-
peg-ifn
-
pan-genotypic
- rig-i
-
non-nucleoside
-
ledipasvir
- ns2b
-
quasispecies
- ritonavir
- drug development
-
1-infected
- bluetongue
-
alfa-2a
-
ifn-free
-
relapsers
-
interferon-based
- pestivirus
-
hcv-rna
-
ns2b-ns3
-
all-oral
- irf-3
- hcv-1b
- molecular biology
- analysis
- pharmacology
- medicine
The enzyme appears in selected viruses and cellular organisms
Reaction Schemes
Hydrolysis of four peptide bonds in the viral precursor polyprotein, commonly with Asp or Glu in the P6 position, Cys or Thr in P1 and Ser or Ala in P1'
Synonyms
ns3 protein, ns3/4a protease, hcv ns3, ns3/4a, hcv ns3 protease, hcv ns3/4a protease, ns3-4a, hcv ns3/4a, ns3-4a protease, ns3/4a serine protease, 
more
topSYNONYM 
ORGANISM
UNIPROT
COMMENTARY 
LITERATURE
Cpro-2
-
-
-
-
Cpro-2 proteinase
-
-
-
-
Den2 protease
-
-
-
-
HCV NS3 protease
-
-
-
-
Hepacivirin
-
-
-
-
hepatitis C virus NS3 serine protease
-
-
-
-
NS2B-NS3 proteinase
-
-
-
-
NS3
-
-
-
-
NS3 protease
NS3 proteinase
-
-
-
-
NS3 serine protease
-
-
-
-
NS3 serine proteinase
NS3-4A serine protease complex
-
-
-
-
NS3-NS4A protease
-
-
-
-
NS5A-5B protease
-
-
-
-
P70
-
-
-
-
polyprotein-processing proteinase NS3
-
-
-
-
proteinase NS3
-
-
-
-
proteinase, polyprotein-processing, NS3
-
-
-
-
serine proteinase NS3
-
-
-
-
NS3 protease
-
-
-
-
NS3 serine proteinase
-
-
-
-
REACTION TYPE
ORGANISM
UNIPROT
COMMENTARY
LITERATURE
hydrolysis of peptide bond
-
-
-
-
CAS REGISTRY NUMBER
COMMENTARY
149885-80-3
-
SUBSTRATE
PRODUCT
REACTION DIAGRAM
ORGANISM
UNIPROT
COMMENTARY
(Substrate)
(Substrate)
LITERATURE
(Substrate)
(Substrate)
COMMENTARY
(Product)
(Product)
LITERATURE
(Product)
(Product)
Reversibility
r=reversible
ir=irreversible
?=not specified
r=reversible
ir=irreversible
?=not specified
INHIBITOR
ORGANISM
UNIPROT
COMMENTARY
LITERATURE
IMAGE
N-(tert-butoxycarbonyl)-3-methyl-L-valyl-(4R)-4-(3-chlorophenyl)-N-[(1R,2S)-1-[(cyclopropanesulfonyl)acetyl]-2-ethenylcyclopropyl]-4-hydroxy-L-prolinamide
hepatitis C virus genotype 1a
-
N-(tert-butoxycarbonyl)-3-methyl-L-valyl-(4R)-4-biphenyl-4-yl-N-[(1R,2S)-1-[(cyclopropylsulfonyl)acetyl]-2-ethenylcyclopropyl]-4-hydroxy-L-prolinamide
hepatitis C virus genotype 1a
-
N-(tert-butoxycarbonyl)-3-methyl-L-valyl-(4R)-4-biphenyl-4-yl-N-[(1R,2S)-1-[(cyclopropylsulfonyl)acetyl]-2-ethenylcyclopropyl]-4-methoxy-L-prolinamide
hepatitis C virus genotype 1a
-
N-(tert-butoxycarbonyl)-3-methyl-L-valyl-(4R)-N-[(1R)-2-carboxy-2-ethenylcyclopropyl]-4-[(7-methoxy-2-phenylquinolin-4-yl)oxy]-L-prolinamide
hepatitis C virus genotype 1a
-
N-(tert-butoxycarbonyl)-3-methyl-L-valyl-(4R)-N-[(1R)-2-[(cyclopropylsulfonyl)carbamoyl]-2-ethenylcyclopropyl]-4-[(6-methoxyisoquinolin-1-yl)oxy]-L-prolinamide
hepatitis C virus genotype 1a
-
N-(tert-butoxycarbonyl)-3-methyl-L-valyl-(4R)-N-[(1R,2S)-1-[(cyclopropanesulfonyl)acetyl]-2-ethenylcyclopropyl]-4-(3-fluorophenyl)-4-hydroxy-L-prolinamide
hepatitis C virus genotype 1a
-
N-(tert-butoxycarbonyl)-3-methyl-L-valyl-(4R)-N-[(1R,2S)-1-[(cyclopropanesulfonyl)acetyl]-2-ethenylcyclopropyl]-4-(4-fluorophenyl)-4-hydroxy-L-prolinamide
hepatitis C virus genotype 1a
-
N-(tert-butoxycarbonyl)-3-methyl-L-valyl-(4R)-N-[(1R,2S)-1-[(cyclopropanesulfonyl)acetyl]-2-ethenylcyclopropyl]-4-hydroxy-4-(3-methoxyphenyl)-L-prolinamide
hepatitis C virus genotype 1a
-
N-(tert-butoxycarbonyl)-3-methyl-L-valyl-(4R)-N-[(1R,2S)-1-[(cyclopropanesulfonyl)acetyl]-2-ethenylcyclopropyl]-4-hydroxy-4-(3-methylphenyl)-L-prolinamide
hepatitis C virus genotype 1a
-
N-(tert-butoxycarbonyl)-3-methyl-L-valyl-(4R)-N-[(1R,2S)-1-[(cyclopropanesulfonyl)acetyl]-2-ethenylcyclopropyl]-4-hydroxy-4-(4-methoxyphenyl)-L-prolinamide
hepatitis C virus genotype 1a
-
N-(tert-butoxycarbonyl)-3-methyl-L-valyl-(4R)-N-[(1R,2S)-1-[(cyclopropanesulfonyl)acetyl]-2-ethenylcyclopropyl]-4-hydroxy-4-phenyl-L-prolinamide
hepatitis C virus genotype 1a
-
N-(tert-butoxycarbonyl)-3-methyl-L-valyl-(4R)-N-[(1R,2S)-1-[(cyclopropylsulfonyl)acetyl]-2-ethenylcyclopropyl]-4-(2,5-dimethylphenyl)-4-hydroxy-L-prolinamide
hepatitis C virus genotype 1a
-
N-(tert-butoxycarbonyl)-3-methyl-L-valyl-(4R)-N-[(1R,2S)-1-[(cyclopropylsulfonyl)acetyl]-2-ethenylcyclopropyl]-4-(3,5-dimethylphenyl)-4-hydroxy-L-prolinamide
hepatitis C virus genotype 1a
-
N-(tert-butoxycarbonyl)-3-methyl-L-valyl-(4R)-N-[(1R,2S)-1-[(cyclopropylsulfonyl)acetyl]-2-ethenylcyclopropyl]-4-(3-fluoro-4-methylphenyl)-4-hydroxy-L-prolinamide
hepatitis C virus genotype 1a
-
N-(tert-butoxycarbonyl)-3-methyl-L-valyl-(4R)-N-[(1R,2S)-1-[(cyclopropylsulfonyl)acetyl]-2-ethenylcyclopropyl]-4-(4-fluoro-3-methylphenyl)-4-hydroxy-L-prolinamide
hepatitis C virus genotype 1a
-
N-(tert-butoxycarbonyl)-3-methyl-L-valyl-(4R)-N-[(1R,2S)-1-[(cyclopropylsulfonyl)acetyl]-2-ethenylcyclopropyl]-4-(5-fluoro-2-methoxyphenyl)-4-hydroxy-L-prolinamide
hepatitis C virus genotype 1a
-
N-(tert-butoxycarbonyl)-3-methyl-L-valyl-(4R)-N-[(1R,2S)-1-[(cyclopropylsulfonyl)acetyl]-2-ethenylcyclopropyl]-4-hydroxy-4-(2'-methoxybiphenyl-4-yl)-L-prolinamide
hepatitis C virus genotype 1a
-
N-(tert-butoxycarbonyl)-3-methyl-L-valyl-(4R)-N-[(1R,2S)-1-[(cyclopropylsulfonyl)acetyl]-2-ethenylcyclopropyl]-4-hydroxy-4-(4'-methoxybiphenyl-3-yl)-L-prolinamide
hepatitis C virus genotype 1a
-
N-(tert-butoxycarbonyl)-3-methyl-L-valyl-(4R)-N-[(1R,2S)-1-[(cyclopropylsulfonyl)acetyl]-2-ethenylcyclopropyl]-4-hydroxy-4-(4-phenoxyphenyl)-L-prolinamide
hepatitis C virus genotype 1a
-
N-(tert-butoxycarbonyl)-3-methyl-L-valyl-(4R)-N-[(1R,2S)-1-[(cyclopropylsulfonyl)acetyl]-2-ethenylcyclopropyl]-4-hydroxy-4-naphthalen-2-yl-L-prolinamide
hepatitis C virus genotype 1a
-
N-(tert-butoxycarbonyl)-3-methyl-L-valyl-(4R)-N-[(1R,2S)-1-[(cyclopropylsulfonyl)acetyl]-2-ethenylcyclopropyl]-4-hydroxy-4-[2-(morpholin-4-ylmethyl)phenyl]-L-prolinamide
hepatitis C virus genotype 1a
-
N-(tert-butoxycarbonyl)-3-methyl-L-valyl-(4R)-N-[(1R,2S)-1-[(cyclopropylsulfonyl)acetyl]-2-ethenylcyclopropyl]-4-hydroxy-4-[3-(morpholin-4-ylmethyl)phenyl]-L-prolinamide
hepatitis C virus genotype 1a
-
N-(tert-butoxycarbonyl)-3-methyl-L-valyl-(4R)-N-[(1R,2S)-1-[(cyclopropylsulfonyl)acetyl]-2-ethenylcyclopropyl]-4-hydroxy-4-[3-(propan-2-yl)phenyl]-L-prolinamide
hepatitis C virus genotype 1a
-
N-(tert-butoxycarbonyl)-3-methyl-L-valyl-(4R)-N-[(1R,2S)-1-[(cyclopropylsulfonyl)acetyl]-2-ethenylcyclopropyl]-4-hydroxy-4-[3-(propan-2-yloxy)phenyl]-L-prolinamide
hepatitis C virus genotype 1a
-
N-(tert-butoxycarbonyl)-3-methyl-L-valyl-(4R)-N-[(1R,2S)-1-[(cyclopropylsulfonyl)acetyl]-2-ethenylcyclopropyl]-4-hydroxy-4-[4-(1,3-thiazol-2-yl)phenyl]-L-prolinamide
hepatitis C virus genotype 1a
-
N-(tert-butoxycarbonyl)-3-methyl-L-valyl-(4R)-N-[(1R,2S)-1-[(cyclopropylsulfonyl)acetyl]-2-ethenylcyclopropyl]-4-hydroxy-4-[4-(1H-pyrrol-1-yl)phenyl]-L-prolinamide
hepatitis C virus genotype 1a
-
N-(tert-butoxycarbonyl)-3-methyl-L-valyl-(4R)-N-[(1R,2S)-1-[(cyclopropylsulfonyl)acetyl]-2-ethenylcyclopropyl]-4-hydroxy-4-[4-(pyridin-2-yl)phenyl]-L-prolinamide
hepatitis C virus genotype 1a
-
N-(tert-butoxycarbonyl)-3-methyl-L-valyl-(4R)-N-[(1R,2S)-1-[(cyclopropylsulfonyl)acetyl]-2-ethenylcyclopropyl]-4-[3-(dimethylamino)phenyl]-4-hydroxy-L-prolinamide
hepatitis C virus genotype 1a
-
N-(tert-butoxycarbonyl)-3-methyl-L-valyl-(4S)-4-(1,3-benzothiazol-2-yl)-N-[(1R,2S)-1-[(cyclopropylsulfonyl)acetyl]-2-ethenylcyclopropyl]-4-hydroxy-L-prolinamide
hepatitis C virus genotype 1a
-
N-(tert-butoxycarbonyl)-3-methyl-L-valyl-(4S)-N-[(1R,2S)-1-[(cyclopropylsulfonyl)acetyl]-2-ethenylcyclopropyl]-4-hydroxy-4-prop-2-en-1-yl-L-prolinamide
hepatitis C virus genotype 1a
-
N-(tert-butoxycarbonyl)-3-methyl-L-valyl-N-[(1R,2S)-1-[(cyclopropylsulfonyl)acetyl]-2-ethenylcyclopropyl]-4-oxo-L-prolinamide
hepatitis C virus genotype 1a
-
N-[17-[2-(4-isopropylthiazole-2-yl)-7-methoxy-8-methylquinolin-4-yloxy]-13-methyl-2,14-dioxo-3,13-diazatricyclo [13.3.0.0(4,6)]octadec-7-ene-4-carbonyl](cyclopropyl)sulfonamide
hepatitis C virus genotype 1a
-
HCV replication in a cellular assay (subgenomic 1b replicon) is inhibited with a half-maximal effective concentration (EC50) of 8 nM. The compound is synergistic with alpha interferon and an NS5B inhibitor in the replicon model and additive with ribavirin. In rats, the compound is extensively distributed to the liver and intestinal tract, and the absolute bioavailability is 44% after a single oral administration. Compound concentrations detected in both plasma and liver at 8 h postdosing are above the EC99 value measured in the replicon
additional information
hepatitis C virus genotype 1a
design and synthesis of a series of potent NS3 protease inhibitors for the treatment of hepatitis C virus, structure-activity relationships of 4-hydroxy-4-biaryl-proline acylsulfonamide tripeptides, overview
-
additional information
hepatitis C virus genotype 1a
-
susceptibility/efficiency and resistance, respectively, of virus genotypes and variants with respect to antiviral agents, EC50 values, detailed overview
-
Ki VALUE [mM]
INHIBITOR
ORGANISM
UNIPROT
COMMENTARY
LITERATURE
IMAGE
0.0000005
N-[17-[2-(4-isopropylthiazole-2-yl)-7-methoxy-8-methylquinolin-4-yloxy]-13-methyl-2,14-dioxo-3,13-diazatricyclo [13.3.0.0(4,6)]octadec-7-ene-4-carbonyl](cyclopropyl)sulfonamide
hepatitis C virus genotype 1a
-
-
IC50 VALUE [mM]
INHIBITOR
ORGANISM
UNIPROT
COMMENTARY
LITERATURE
IMAGE
0.000001
BMS-605339
hepatitis C virus genotype 1a
pH and temperature not specified in the publication
0.00008
N-(tert-butoxycarbonyl)-3-methyl-L-valyl-(4R)-4-(3-chlorophenyl)-N-[(1R,2S)-1-[(cyclopropanesulfonyl)acetyl]-2-ethenylcyclopropyl]-4-hydroxy-L-prolinamide
hepatitis C virus genotype 1a
pH and temperature not specified in the publication
0.000004
N-(tert-butoxycarbonyl)-3-methyl-L-valyl-(4R)-4-biphenyl-4-yl-N-[(1R,2S)-1-[(cyclopropylsulfonyl)acetyl]-2-ethenylcyclopropyl]-4-hydroxy-L-prolinamide
hepatitis C virus genotype 1a
pH and temperature not specified in the publication
0.000002
N-(tert-butoxycarbonyl)-3-methyl-L-valyl-(4R)-4-biphenyl-4-yl-N-[(1R,2S)-1-[(cyclopropylsulfonyl)acetyl]-2-ethenylcyclopropyl]-4-methoxy-L-prolinamide
hepatitis C virus genotype 1a
pH and temperature not specified in the publication
0.000057
N-(tert-butoxycarbonyl)-3-methyl-L-valyl-(4R)-N-[(1R,2S)-1-[(cyclopropanesulfonyl)acetyl]-2-ethenylcyclopropyl]-4-(3-fluorophenyl)-4-hydroxy-L-prolinamide
hepatitis C virus genotype 1a
pH and temperature not specified in the publication
0.00019
N-(tert-butoxycarbonyl)-3-methyl-L-valyl-(4R)-N-[(1R,2S)-1-[(cyclopropanesulfonyl)acetyl]-2-ethenylcyclopropyl]-4-(4-fluorophenyl)-4-hydroxy-L-prolinamide
hepatitis C virus genotype 1a
pH and temperature not specified in the publication
0.000052
N-(tert-butoxycarbonyl)-3-methyl-L-valyl-(4R)-N-[(1R,2S)-1-[(cyclopropanesulfonyl)acetyl]-2-ethenylcyclopropyl]-4-hydroxy-4-(3-methoxyphenyl)-L-prolinamide
hepatitis C virus genotype 1a
pH and temperature not specified in the publication
0.000076
N-(tert-butoxycarbonyl)-3-methyl-L-valyl-(4R)-N-[(1R,2S)-1-[(cyclopropanesulfonyl)acetyl]-2-ethenylcyclopropyl]-4-hydroxy-4-(3-methylphenyl)-L-prolinamide
hepatitis C virus genotype 1a
pH and temperature not specified in the publication
0.000105
N-(tert-butoxycarbonyl)-3-methyl-L-valyl-(4R)-N-[(1R,2S)-1-[(cyclopropanesulfonyl)acetyl]-2-ethenylcyclopropyl]-4-hydroxy-4-(4-methoxyphenyl)-L-prolinamide
hepatitis C virus genotype 1a
pH and temperature not specified in the publication
0.00014
N-(tert-butoxycarbonyl)-3-methyl-L-valyl-(4R)-N-[(1R,2S)-1-[(cyclopropanesulfonyl)acetyl]-2-ethenylcyclopropyl]-4-hydroxy-4-phenyl-L-prolinamide
hepatitis C virus genotype 1a
pH and temperature not specified in the publication
0.000136
N-(tert-butoxycarbonyl)-3-methyl-L-valyl-(4R)-N-[(1R,2S)-1-[(cyclopropylsulfonyl)acetyl]-2-ethenylcyclopropyl]-4-(2,5-dimethylphenyl)-4-hydroxy-L-prolinamide
hepatitis C virus genotype 1a
pH and temperature not specified in the publication
0.00008
N-(tert-butoxycarbonyl)-3-methyl-L-valyl-(4R)-N-[(1R,2S)-1-[(cyclopropylsulfonyl)acetyl]-2-ethenylcyclopropyl]-4-(3,5-dimethylphenyl)-4-hydroxy-L-prolinamide
hepatitis C virus genotype 1a
pH and temperature not specified in the publication
0.000568
N-(tert-butoxycarbonyl)-3-methyl-L-valyl-(4R)-N-[(1R,2S)-1-[(cyclopropylsulfonyl)acetyl]-2-ethenylcyclopropyl]-4-(3-fluoro-4-methylphenyl)-4-hydroxy-L-prolinamide
hepatitis C virus genotype 1a
pH and temperature not specified in the publication
0.000134
N-(tert-butoxycarbonyl)-3-methyl-L-valyl-(4R)-N-[(1R,2S)-1-[(cyclopropylsulfonyl)acetyl]-2-ethenylcyclopropyl]-4-(4-fluoro-3-methylphenyl)-4-hydroxy-L-prolinamide
hepatitis C virus genotype 1a
pH and temperature not specified in the publication
0.000728
N-(tert-butoxycarbonyl)-3-methyl-L-valyl-(4R)-N-[(1R,2S)-1-[(cyclopropylsulfonyl)acetyl]-2-ethenylcyclopropyl]-4-(5-fluoro-2-methoxyphenyl)-4-hydroxy-L-prolinamide
hepatitis C virus genotype 1a
pH and temperature not specified in the publication
0.000005
N-(tert-butoxycarbonyl)-3-methyl-L-valyl-(4R)-N-[(1R,2S)-1-[(cyclopropylsulfonyl)acetyl]-2-ethenylcyclopropyl]-4-hydroxy-4-(2'-methoxybiphenyl-4-yl)-L-prolinamide
hepatitis C virus genotype 1a
pH and temperature not specified in the publication
0.00062
N-(tert-butoxycarbonyl)-3-methyl-L-valyl-(4R)-N-[(1R,2S)-1-[(cyclopropylsulfonyl)acetyl]-2-ethenylcyclopropyl]-4-hydroxy-4-(4'-methoxybiphenyl-3-yl)-L-prolinamide
hepatitis C virus genotype 1a
pH and temperature not specified in the publication
0.00005
N-(tert-butoxycarbonyl)-3-methyl-L-valyl-(4R)-N-[(1R,2S)-1-[(cyclopropylsulfonyl)acetyl]-2-ethenylcyclopropyl]-4-hydroxy-4-(4-phenoxyphenyl)-L-prolinamide
hepatitis C virus genotype 1a
pH and temperature not specified in the publication
0.000026
N-(tert-butoxycarbonyl)-3-methyl-L-valyl-(4R)-N-[(1R,2S)-1-[(cyclopropylsulfonyl)acetyl]-2-ethenylcyclopropyl]-4-hydroxy-4-naphthalen-2-yl-L-prolinamide
hepatitis C virus genotype 1a
pH and temperature not specified in the publication
0.000291
N-(tert-butoxycarbonyl)-3-methyl-L-valyl-(4R)-N-[(1R,2S)-1-[(cyclopropylsulfonyl)acetyl]-2-ethenylcyclopropyl]-4-hydroxy-4-[2-(morpholin-4-ylmethyl)phenyl]-L-prolinamide
hepatitis C virus genotype 1a
pH and temperature not specified in the publication
0.000162
N-(tert-butoxycarbonyl)-3-methyl-L-valyl-(4R)-N-[(1R,2S)-1-[(cyclopropylsulfonyl)acetyl]-2-ethenylcyclopropyl]-4-hydroxy-4-[3-(morpholin-4-ylmethyl)phenyl]-L-prolinamide
hepatitis C virus genotype 1a
pH and temperature not specified in the publication
0.000703
N-(tert-butoxycarbonyl)-3-methyl-L-valyl-(4R)-N-[(1R,2S)-1-[(cyclopropylsulfonyl)acetyl]-2-ethenylcyclopropyl]-4-hydroxy-4-[3-(propan-2-yl)phenyl]-L-prolinamide
hepatitis C virus genotype 1a
pH and temperature not specified in the publication
0.000101
N-(tert-butoxycarbonyl)-3-methyl-L-valyl-(4R)-N-[(1R,2S)-1-[(cyclopropylsulfonyl)acetyl]-2-ethenylcyclopropyl]-4-hydroxy-4-[3-(propan-2-yloxy)phenyl]-L-prolinamide
hepatitis C virus genotype 1a
pH and temperature not specified in the publication
0.000002
N-(tert-butoxycarbonyl)-3-methyl-L-valyl-(4R)-N-[(1R,2S)-1-[(cyclopropylsulfonyl)acetyl]-2-ethenylcyclopropyl]-4-hydroxy-4-[4-(1,3-thiazol-2-yl)phenyl]-L-prolinamide
hepatitis C virus genotype 1a
pH and temperature not specified in the publication
0.000007
N-(tert-butoxycarbonyl)-3-methyl-L-valyl-(4R)-N-[(1R,2S)-1-[(cyclopropylsulfonyl)acetyl]-2-ethenylcyclopropyl]-4-hydroxy-4-[4-(1H-pyrrol-1-yl)phenyl]-L-prolinamide
hepatitis C virus genotype 1a
pH and temperature not specified in the publication
0.000002
N-(tert-butoxycarbonyl)-3-methyl-L-valyl-(4R)-N-[(1R,2S)-1-[(cyclopropylsulfonyl)acetyl]-2-ethenylcyclopropyl]-4-hydroxy-4-[4-(pyridin-2-yl)phenyl]-L-prolinamide
hepatitis C virus genotype 1a
pH and temperature not specified in the publication
0.00096
N-(tert-butoxycarbonyl)-3-methyl-L-valyl-(4R)-N-[(1R,2S)-1-[(cyclopropylsulfonyl)acetyl]-2-ethenylcyclopropyl]-4-[3-(dimethylamino)phenyl]-4-hydroxy-L-prolinamide
hepatitis C virus genotype 1a
pH and temperature not specified in the publication
0.000127
N-(tert-butoxycarbonyl)-3-methyl-L-valyl-(4S)-4-(1,3-benzothiazol-2-yl)-N-[(1R,2S)-1-[(cyclopropylsulfonyl)acetyl]-2-ethenylcyclopropyl]-4-hydroxy-L-prolinamide
hepatitis C virus genotype 1a
pH and temperature not specified in the publication
0.0015
N-(tert-butoxycarbonyl)-3-methyl-L-valyl-(4S)-N-[(1R,2S)-1-[(cyclopropylsulfonyl)acetyl]-2-ethenylcyclopropyl]-4-hydroxy-4-prop-2-en-1-yl-L-prolinamide
hepatitis C virus genotype 1a
pH and temperature not specified in the publication
ORGANISM
COMMENTARY
LITERATURE
UNIPROT
SEQUENCE DB
SOURCE
PROTEIN VARIANTS
ORGANISM
UNIPROT
COMMENTARY
LITERATURE
additional information
hepatitis C virus genotype 1a
-
for hepatitis C virus (HCV) genotype 1, substitutions at NS3 protease positions 155, 156, and 168 are the main determinants of PI resistance. For other genotypes, similar substitutions are selected during protease inhibitor treatment but are not characterized systematically. Most mutant variants show decreased fitness compared to that of the original viruses. Fitness characteristics of HCV genotype 1 to 6 recombinants with substitutions at NS3P positions 155, 156, or 168, overview
CLONED (Commentary)
ORGANISM
UNIPROT
LITERATURE
genotyping, expression of wild-type and mutant variant viruses in Huh7.5 cells
hepatitis C virus genotype 1a
-
APPLICATION
ORGANISM
UNIPROT
COMMENTARY
LITERATURE
medicine
hepatitis C virus genotype 1a
-
inhibitor shows selective and potent in vitro anti-HCV activity, the potential for combination with other anti-HCV agents, and a favorable pharmacokinetic profile
REF.
AUTHORS
TITLE
JOURNAL
VOL.
PAGES
YEAR
ORGANISM (UNIPROT)
PUBMED ID
SOURCE
Lin, T.I.; Lenz, O.; Fanning, G.; Verbinnen, T.; Delouvroy, F.; Scholliers, A.; Vermeiren, K.; Rosenquist, A.; Edlund, M.; Samuelsson, B.; Vrang, L.; de Kock, H.; Wigerinck, P.; Raboisson, P.; Simmen, K.
In vitro activity and preclinical profile of TMC435350, a potent hepatitis C virus protease inhibitor
Antimicrob. Agents Chemother.
53
1377-1385
2009
Hepacivirus C, hepatitis C virus genotype 1a
Jensen, S.B.; Serre, S.B.; Humes, D.G.; Ramirez, S.; Li, Y.P.; Bukh, J.; Gottwein, J.M.
Substitutions at NS3 residue 155, 156, or 168 of hepatitis C virus genotypes 2 to 6 induce complex patterns of protease inhibitor resistance
Antimicrob. Agents Chemother.
59
7426-7436
2015
hepatitis C virus genotype 1a, Hepatitis C virus subtype 3a, Hepatitis C virus genotype 4a (O39929), Hepatitis C virus genotype 5a (O91936), Hepatitis C virus genotype 2a (Q99IB8)
Wang, A.X.; Chen, J.; Zhao, Q.; Sun, L.Q.; Friborg, J.; Yu, F.; Hernandez, D.; Good, A.C.; Klei, H.E.; Rajamani, R.; Mosure, K.; Knipe, J.O.; Li, D.; Zhu, J.; Levesque, P.C.; McPhee, F.; Meanwell, N.A.; Scola, P.M.
Structure-activity relationships of 4-hydroxy-4-biaryl-proline acylsulfonamide tripeptides A series of potent NS3 protease inhibitors for the treatment of hepatitis C virus
Bioorg. Med. Chem. Lett.
27
590-596
2017
Hepatitis C virus genotype 1b (P26663), hepatitis C virus genotype 1a (P27958)
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