3.4.23.B8: human T-cell leukemia virus type 1 protease
This is an abbreviated version!
For detailed information about human T-cell leukemia virus type 1 protease, go to the full flat file.
Word Map on EC 3.4.23.B8
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3.4.23.B8
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retroviral
-
polyproteins
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spastic
-
retroviruses
-
myelopathy
-
tetrapeptidic
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paraparesis
-
indinavir
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hydroxyethylamine
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aspartyl
-
substrate-based
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scissile
-
peptidomimetic
-
medicine
-
hydroxymethylcarbonyl
-
autoprocessing
-
darunavir
-
gag-pro-pol
-
drug development
- 3.4.23.B8
-
retroviral
- polyproteins
-
spastic
-
retroviruses
- myelopathy
-
tetrapeptidic
- paraparesis
- indinavir
-
hydroxyethylamine
-
aspartyl
-
substrate-based
-
scissile
-
peptidomimetic
- medicine
-
hydroxymethylcarbonyl
-
autoprocessing
- darunavir
-
gag-pro-pol
- drug development
Reaction
Processing at the authentic HIV-1 PR recognition site and release of the mature p17 matrix and the p24 capsid protein, as a result of the cleavage of the -SQNY-/-PIVQ- cleavage site. =
Synonyms
C2A HTLV-1 PR, HTLV-1 PR, HTLV-1 protease, HTLV-I PR, HTLV-I protease, human T cell leukemia virus PR, human T cell leukemia virus protease, human T-cell leukemia virus type 1 protease, human T-lymphotropic virus type I protease, More, retropepsin (human T-cell leukemia virus), simian T-cell leukemia virus endopeptidase
ECTree
3.4.23.B8 human T-cell leukemia virus type 1 proteaseAdvanced search results
results (
results (Inhibitors
Inhibitors on EC 3.4.23.B8 - human T-cell leukemia virus type 1 protease
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INHIBITOR 
ORGANISM
UNIPROT
COMMENTARY 
LITERATURE
IMAGE
(2R)-2-[(3-[[(R)-amino(hydroxy)methyl][2-hydroxy-2-(naphthalen-2-yl)ethyl]amino]-3-cyclopentylpropyl)amino]-N-benzyl-2-hydroxyethanesulfonamide
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(R)-N-isobutyl-3-(((2S,3S)-3-((2S)-2-[(2S)-2-(2,2-dimethyl)butanoylamino-2-phenyl]acetylamino-3,3-dimethyl)-butanoylamino-2-hydroxy-4-phenyl))butanoyl-5,5-dimethyl-1,3-thiazolidine-4-carboxamide
-
-
(R)-N-isobutyl-3-(((2S,3S)-3-((2S)-2-[(2S)-2-(2-methyl)pentanoylamino-2-phenyl]acetylamino-3,3-dimethyl)- butanoylamino-2-hydroxy-4-phenyl))butanoyl-5,5-dimethyl-1,3-thiazolidine-4-carboxamide
-
-
(R)-N-isobutyl-3-(((2S,3S)-3-((2S)-2-[(2S)-2-(3,3-dimethyl)butanoylamino-2-phenyl]acetylamino-3,3-dimethyl)-butanoylamino-2-hydroxy-4-phenyl))butanoyl-5,5-dimethyl-1,3-thiazolidine-4-carboxamide
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-
(R)-N-isobutyl-3-(((2S,3S)-3-((2S)-2-[(2S)-2-(3-methyl)butanoylamino-2-phenyl]acetylamino-3,3-dimethyl)-butanoylamino-2-hydroxy-4-phenyl))butanoyl-5,5-dimethyl-1,3-thiazolidine-4-carboxamide
-
-
(R)-N-isobutyl-3-(((2S,3S)-3-((2S)-2-[(2S)-2-(3-methyl)pentanoylamino-2-phenyl]acetylamino-3,3-dimethyl)butanoylamino-2-hydroxy-4-phenyl))butanoyl-5,5-dimethyl-1,3-thiazolidine-4-carboxamide
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-
(R)-N-isobutyl-3-(((2S,3S)-3-((2S)-2-[(2S)-2-(3-phenyl)-propanoylamino-2-phenyl]acetylamino-3,3-dimethyl)butanoylamino-2-hydroxy-4-phenyl))butanoyl-5,5-dimethyl-1,3-thiazolidine-4-carboxamide
-
-
(R)-N-isobutyl-3-(((2S,3S)-3-((2S)-2-[(2S)-2-(4-methyl)pentanoylamino-2-phenyl]acetylamino-3,3-dimethyl) butanoylamino-2-hydroxy-4-phenyl))butanoyl-5,5-dimethyl-1,3-thiazolidine-4-carboxamide
-
-
(R)-N-isobutyl-3-(((2S,3S)-3-((2S)-2-[(2S)-2-acetylamino-2-phenyl]acetylamino-3,3-dimethyl)butanoylamino-2-hydroxy-4-phenyl))butanoyl-5,5-dimethyl-1,3-thiazolidine-4-carboxamide
-
-
(R)-N-isobutyl-3-(((2S,3S)-3-((2S)-2-[(2S)-2-amino-2-phenyl]acetylamino-3,3-dimethyl)butanoylamino-2-hydroxy-4-phenylbutanoyl))-5,5-dimethyl-1,3-thiazolidine-4-carboxamide
-
-
(R)-N-isobutyl-3-(((2S,3S)-3-((2S)-2-[(2S)-2-benzoylamino-2-phenyl]acetylamino-3,3-dimethyl)butanoylamino-2-hydroxy-4-phenyl))butanoyl-5,5-dimethyl-1,3-thiazolidine-4-carboxamide
-
-
(R)-N-isobutyl-3-(((2S,3S)-3-((2S)-2-[(2S)-2-cyclohexanecarbonylamino-2-phenyl]acetylamino-3,3-dimethyl)-butanoylamino-2-hydroxy-4-phenyl))butanoyl-5,5-dimethyl-1,3-thiazolidine-4-carboxamide
-
-
(R)-N-isobutyl-3-(((2S,3S)-3-((2S)-2-[(2S)-2-isobutyrylamino-2-phenyl]acetylamino-3,3-dimethyl)butanoylamino-2-hydroxy-4-phenyl))butanoyl-5,5-dimethyl-1,3-thiazolidine-4-carboxamide
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(R)-N-isobutyl-3-(((2S,3S)-3-((2S)-2-[(2S)-2-pentanoylamino-2-phenyl]acetylamino-3,3-dimethyl)butanoylamino-2-hydroxy-4-phenyl))butanoyl-5,5-dimethyl-1,3-thiazolidine-4-carboxamide
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(R)-N-isobutyl-3-(((2S,3S)-3-((2S)-2-[(2S)-2-propionylamino-2-phenyl]acetylamino-3,3-dimethyl)butanoylamino-2-hydroxy-4-phenyl))butanoyl-5,5-dimethyl-1,3-thiazolidine-4-carboxamide
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-
(R)-N-isobutyl-3-[[(2S,3S)-3-[(2S)-2-[(2S)-2-butyrylamino-2-phenyl]acetylamino-3,3-dimethyl]butanoylamino-2-hydroxy-4-phenyl]]butanoyl-5,5-dimethyl-1,3-thiazolidine-4-carboxamide
-
-
(R)-N-isobutyl-3-[[(2S,3S)-3-[(2S)-2-[(2S)-2-cyclopropanecarbonylamino-2-phenyl]acetylamino-3,3-dimethyl]butanoylamino-2-hydroxy-4-phenyl]]butanoyl-5,5-dimethyl-1,3-thiazolidine-4-carboxamide
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-
(R)-N-Isobutyl-3-[[(2S,3S)-3-[(2S)-2-[(2S)-2-pivaloylamino-2-phenyl]acetylamino-3,3-dimethyl]butanoylamino-2-hydroxy-4-phenyl]]butanoyl-5,5-dimethyl-1,3-thiazolidine-4-carboxamide
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2-(4-tert-butylphenyl)-N-carbamoyl-N-[3-([[(pyridin-1(2H)-ylmethyl)sulfamoyl]carbonyl]amino)-3-(pyrrolidin-1-yl)propyl]acetamide
-
-
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2-(4-tert-butylphenyl)-N-carbamoyl-N-[3-[([[(3,5-dichloro-4-oxopyridin-1(4H)-yl)methyl]sulfamoyl]carbonyl)amino]-3-[3-(hydroxyamino)-4-oxopyrrolidin-1-yl]propyl]acetamide
-
4-[(anilinocarbonyl)amino]-6-chlorobenzene-1,3-disulfonamide
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Ac-Ala-Pro-Gln-Val-Sta-Val-Met-His-Pro
-
19% inhibition at 50 nM
Ac-Ala-Pro-Gln-Val-statine-Val-Met-His-Pro
-
binding mode in an extended conformation at the active site, competitive, binding-involved residues of the S2/S2'-subsite, overview
Ac-Ala-Val-allophenylnorstatine-(R)-5,5-dimethyl-1,3-thiazolidine-4-carboxylic acid-Val-Met-NH2
-
HTLV-I inhibition 56%
Ac-allophenylnorstatine-Pro-Val-Met-His-OH
-
HTLV-I inhibition below 30%
Ac-Gln-(R)-S-methyl-L-cysteine-allophenylnorstatine-(R)-5,5-dimethyl-1,3-thiazolidine-4-carboxylic acid-Val-Met-NH2
-
HTLV-I inhibition 51%
Ac-Gln-Ile-allophenylnorstatine-(R)-5,5-dimethyl-1,3-thiazolidine-4-carboxylic acid-Val-Met-NH2
-
HTLV-I inhibition 85%
Ac-Gln-Leu-allophenylnorstatine-(R)-5,5-dimethyl-1,3-thiazolidine-4-carboxylic acid-Val-Met-NH2
-
HTLV-I inhibition 54%
Ac-Gln-Val-allophenylnorstatine-(R)-5,5-dimethyl-1,3-thiazolidine-4-carboxylic acid- (R)-S-methyl-L-Cys-Met-NH2
-
HTLV-I inhibition below 30%
Ac-Gln-Val-allophenylnorstatine-(R)-5,5-dimethyl-1,3-thiazolidine-4-carboxylic acid-Ile-Met-NH2
-
HTLV-I inhibition 74%
Ac-Gln-Val-allophenylnorstatine-(R)-5,5-dimethyl-1,3-thiazolidine-4-carboxylic acid-Leu-Met-NH2
-
HTLV-I inhibition 30%
Ac-Gln-Val-allophenylnorstatine-(R)-5,5-dimethyl-1,3-thiazolidine-4-carboxylic acid-Thr-Met-NH2
-
HTLV-I inhibition below 30%
Ac-Gln-Val-allophenylnorstatine-(R)-5,5-dimethyl-1,3-thiazolidine-4-carboxylic acid-Val-Met-NH2
-
HTLV-I inhibition 66%; HTLV-I inhibition 99%
Ac-Gln-Val-allophenylnorstatine-Pro-Val-Met-His-OH
-
HTLV-I inhibition 49%
Ac-Ile-Val-allophenylnorstatine-(R)-5,5-dimethyl-1,3-thiazolidine-4-carboxylic acid-Ile-Met-NH2
-
HTLV-I inhibition 94%
Ac-Ile-Val-allophenylnorstatine-(R)-5,5-dimethyl-1,3-thiazolidine-4-carboxylic acid-Val-Gln-NH2
-
HTLV-I inhibition 86%
Ac-Ile-Val-allophenylnorstatine-(R)-5,5-dimethyl-1,3-thiazolidine-4-carboxylic acid-Val-Ile-NH2
-
HTLV-I inhibition 78%
Ac-Ile-Val-allophenylnorstatine-(R)-5,5-dimethyl-1,3-thiazolidine-4-carboxylic acid-Val-Leu-NH2
-
HTLV-I inhibition 54%
Ac-Ile-Val-allophenylnorstatine-(R)-5,5-dimethyl-1,3-thiazolidine-4-carboxylic acid-Val-Met-NH2
-
HTLV-I inhibition 87%
Ac-Ile-Val-allophenylnorstatine-(R)-5,5-dimethyl-1,3-thiazolidine-4-carboxylic acid-Val-Phe-NH2
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HTLV-I inhibition 84%
Ac-Ile-Val-allophenylnorstatine-(R)-5,5-dimethyl-1,3-thiazolidine-4-carboxylic acid-Val-Val-NH2
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HTLV-I inhibition 70%
Ac-Leu-Val-allophenylnorstatine-(R)-5,5-dimethyl-1,3-thiazolidine-4-carboxylic acid-Val-Met-NH2
-
HTLV-I inhibition 83%
Ac-Phe-Val-allophenylnorstatine-(R)-5,5-dimethyl-1,3-thiazolidine-4-carboxylic acid-Val-Met-NH2
-
HTLV-I inhibition 74%
Ac-Val-allophenylnorstatine-Pro-Val-Met-His-OH
-
HTLV-I inhibition below 30%
Ac-Val-Val-allophenylnorstatine-(R)-5,5-dimethyl-1,3-thiazolidine-4-carboxylic acid-Val-Met-NH2
-
HTLV-I inhibition 77%
acetyl-(L-(+)-alpha-phenylglycine)-(L-tert-leucine)-(allophenylnorstatine)-[(R)-5,5-dimethyl-1,3-thiazolidine-4-carboxylic acid]-((2,2-dimethylpropyl)amino)
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acetyl-(L-(+)-alpha-phenylglycine)-(L-tert-leucine)-(allophenylnorstatine)-[(R)-5,5-dimethyl-1,3-thiazolidine-4-carboxylic acid]-((2-methylprop-2-en-1-yl)amino)
-
-
acetyl-(L-(+)-alpha-phenylglycine)-(L-tert-leucine)-(allophenylnorstatine)-[(R)-5,5-dimethyl-1,3-thiazolidine-4-carboxylic acid]-((2-methylpropyl)amino)
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-
acetyl-(L-(+)-alpha-phenylglycine)-(L-tert-leucine)-(allophenylnorstatine)-[(R)-5,5-dimethyl-1,3-thiazolidine-4-carboxylic acid]-((cyclopropyl)amino)
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acetyl-(L-(+)-alpha-phenylglycine)-(L-tert-leucine)-(allophenylnorstatine)-[(R)-5,5-dimethyl-1,3-thiazolidine-4-carboxylic acid]-(2-methylbenzylamino)
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acetyl-(L-(+)-alpha-phenylglycine)-(L-tert-leucine)-(allophenylnorstatine)-[(R)-5,5-dimethyl-1,3-thiazolidine-4-carboxylic acid]-(3-iodobenzylamino)
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acetyl-(L-(+)-alpha-phenylglycine)-(L-tert-leucine)-(allophenylnorstatine)-[(R)-5,5-dimethyl-1,3-thiazolidine-4-carboxylic acid]-(prop-2-en-1-ylamino)
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acetyl-(L-(+)-alpha-phenylglycine)-(L-tert-leucine)-(allophenylnorstatine)-[(R)-5,5-dimethyl-1,3-thiazolidine-4-carboxylic acid]-(propylamino)
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acetyl-(L-(+)-alpha-phenylglycine)-(L-tert-leucine)-(allophenylnorstatine)-[(R)-5,5-dimethyl-1,3-thiazolidine-4-carboxylic acid]-Ile-Gln-NH2
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acetyl-(L-(+)-alpha-phenylglycine)-(L-tert-leucine)-(allophenylnorstatine)-[(R)-5,5-dimethyl-1,3-thiazolidine-4-carboxylic acid]-Ile-Met-NH2
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acetyl-(L-(+)-alpha-phenylglycine)-(L-tert-leucine)-(allophenylnorstatine)-[(R)-5,5-dimethyl-1,3-thiazolidine-4-carboxylic acid]-Ile-NH2
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acetyl-(L-(+)-alpha-phenylglycine)-Ile-(allophenylnorstatine)-[(R)-5,5-dimethyl-1,3-thiazolidine-4-carboxylic acid]-Ile-Met-NH2
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acetyl-(L-tert-leucine)-Ile-(allophenylnorstatine)-[(R)-5,5-dimethyl-1,3-thiazolidine-4-carboxylic acid]-Ile-Met-NH2
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acetyl-Gln-Val-(allophenylnorstatine)-[(R)-5,5-dimethyl-1,3-thiazolidine-4-carboxylic acid]-Val-Met-NH2
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acetyl-Ile-(L-(+)-alpha-phenylglycine)-(allophenylnorstatine)-[(R)-5,5-dimethyl-1,3-thiazolidine-4-carboxylic acid]-Ile-Met-NH2
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acetyl-Ile-Ile-(allophenylnorstatine)-[(R)-5,5-dimethyl-1,3-thiazolidine-4-carboxylic acid]-(L-(+)-alpha-phenylglycine)-Met-NH2
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acetyl-Ile-Ile-(allophenylnorstatine)-[(R)-5,5-dimethyl-1,3-thiazolidine-4-carboxylic acid]-(L-tert-leucine)-Met-NH2
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acetyl-Ile-Ile-(allophenylnorstatine)-[(R)-5,5-dimethyl-1,3-thiazolidine-4-carboxylic acid]-Ile-Ala-NH2
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acetyl-Ile-Ile-(allophenylnorstatine)-[(R)-5,5-dimethyl-1,3-thiazolidine-4-carboxylic acid]-Ile-Gln-NH2
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acetyl-Ile-Ile-(allophenylnorstatine)-[(R)-5,5-dimethyl-1,3-thiazolidine-4-carboxylic acid]-Ile-Met-NH2
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acetyl-Ile-Ile-(allophenylnorstatine)-[(R)-5,5-dimethyl-1,3-thiazolidine-4-carboxylic acid]-Ile-NH2
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acetyl-Ile-Ile-(allophenylnorstatine)-[(R)-5,5-dimethyl-1,3-thiazolidine-4-carboxylic acid]-Ile-Phe-NH2
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acetyl-Ile-Ile-(phenylnorstatine)-[(R)-5,5-dimethyl-1,3-thiazolidine-4-carboxylic acid]-Ile-Met-NH2
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H-allophenylnorstatine-Pro-Val-Met-His-OH
-
HTLV-I inhibition below 30%
H-Gln-Val-allophenylnorstatine-Pro-Val-Met-His-OH
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HTLV-I inhibition below 30%
H-Pro-Gln-Val-allophenylnorstatine-(R)-5,5-dimethyl-1,3-thiazolidine-4-carboxylic acid-Val-Met-His-OH
-
HTLV-I inhibition 99%
H-Pro-Gln-Val-allophenylnorstatine-Pro-NH2
-
HTLV-I inhibition below 30%
H-Pro-Gln-Val-allophenylnorstatine-Pro-Val-Met-His-OH
-
HTLV-I inhibition 94%
H-Pro-Gln-Val-allophenylnorstatine-Pro-Val-Met-NH2
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HTLV-I inhibition 86%
H-Pro-Gln-Val-allophenylnorstatine-Pro-Val-NH2
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HTLV-I inhibition below 30%
H-Pro-Pro-Val-Ile-NHCH(CH2CH(CH3)2)CH(OH)CH2-Pro-NHCH2C6H5I
-
-
H-Pro-Val-Ile-hydroxyethylamine[(R)-isobutyl,(R)-hydroxy]-Pro-NH-CH2-C6H4I
-
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H-Pro-Val-Ile-hydroxyethylamine[(R)-isobutyl,(S)-hydroxy]-Pro-NH-CH2-C6H4I
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H-Pro-Val-Ile-hydroxyethylamine[(S)-isobutyl,(R)-hydroxy]-Pro-NH-CH2-C6H4I
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H-Pro-Val-Ile-hydroxyethylamine[(S)-isobutyl,(S)-hydroxy]-Pro-NH-CH2-C6H4I
-
-
H-Pro-Val-Ile-NHCH(CH2CH(CH3)2)CH(OH)CH2-Pro-Ile-NHCH2C6H5I
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H-Pro-Val-Ile-NHCH(CH2CH(CH3)2)CH(OH)CH2-Pro-NHCH2C6H5I
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H-Val-allophenylnorstatine-Pro-Val-Met-His-OH
-
HTLV-I inhibition below 30%
H-Val-Ile-NHCH(CH2CH(CH3)2)CH(OH)CH2-Pro-Ile-NHCH2C6H5I
-
-
isobutyl oxycarbonyl-Lys--Val-Val-(3S,4S)-statine-Ala-isoamylamine
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i.e. CS-I-27
isovaleryl-Lys-Val-(3S,4S)-statine-Ala-isoamylamine
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i.e. CS-I-25
isovaleryl-Val-Nle-(3S,4S)-statine-Ala-isoamylamine
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i.e. CS-I-22
isovaleryl-Val-Val-(3S,4S)-statine-Ala-Lys-methyl ester
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i.e. CS-I-52
isovaleryl-Val-Val-(3S,4S)-statine-Lys-isoamylamine
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i.e. CS-I-51
KNI-10220
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HTLV-1 PR-specific inhibitor, 61% inhibition at 50 nM
KNI-10296c
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HTLV-1 PR-specific inhibitor, 28% inhibition at 50 nM
KNI-10516
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HTLV-1 PR-specific inhibitor, 86% inhibition at 50 nM
N,N'-(3S,4S)-pyrrolidine-3,4-diylbis(4-amino-N-benzylbenzenesulfonamide)
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N,N'-(3S,4S)-pyrrolidine-3,4-diylbis(N-benzyl-2-chlorobenzenesulfonamide)
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N,N'-(3S,4S)-pyrrolidine-3,4-diylbis(N-benzyl-2-methylbenzenesulfonamide)
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-
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N,N'-(3S,4S)-pyrrolidine-3,4-diylbis(N-benzyl-4-nitrobenzenesulfonamide)
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-
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N,N'-(3S,4S)-pyrrolidine-3,4-diylbis(N-benzylbenzenesulfonamide)
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-
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N,N'-(3S,4S)-pyrrolidine-3,4-diylbis[N-(2-methylprop-2-en-1-yl)benzenesulfonamide]
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-
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N,N'-(3S,4S)-pyrrolidine-3,4-diylbis[N-(3-methylbut-2-en-1-yl)benzenesulfonamide]
-
-
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N,N'-(3S,4S)-pyrrolidine-3,4-diylbis[N-(4-iodobenzyl)benzenesulfonamide]
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N,N'-(3S,4S)-pyrrolidine-3,4-diylbis[N-(prop-2-en-1-yl)benzenesulfonamide]
-
-
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N,N'-(3S,4S)-pyrrolidine-3,4-diylbis[N-[4-(trifluoromethyl)benzyl]benzenesulfonamide]
-
-
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N-(3-[[(benzylsulfamoyl)carbonyl]amino]-1-cyclopentylpropyl)-N-carbamoyl-N2-hydroxy-N2-(hydroxymethyl)glycinamide
-
N-[(2R)-2-[(1R)-2-[(2R)-1-(benzylcarbamoyl)pyrrolidin-2-yl]-1-hydroxyethyl]-4-methylpentanoyl]-D-isoleucyl-D-valyl-D-prolyl-D-prolinamide
-
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N-[(2R)-2-[(1S)-2-[(2R)-1-(benzylcarbamoyl)pyrrolidin-2-yl]-1-hydroxyethyl]-4-methylpentanoyl]-D-isoleucyl-D-valyl-D-prolyl-D-prolinamide
-
-
N-[(2S)-2-[(1R)-2-[(2R)-1-(benzylcarbamoyl)pyrrolidin-2-yl]-1-hydroxyethyl]-4-methylpentanoyl]-D-isoleucyl-D-valyl-D-prolyl-D-prolinamide
-
-
N-[(2S)-2-[(1S)-2-[(2R)-1-(benzylcarbamoyl)pyrrolidin-2-yl]-1-hydroxyethyl]-4-methylpentanoyl]-D-isoleucyl-D-valyl-D-prolyl-D-prolinamide
-
-
N-[(2S)-4-[(4R)-4-[(2,2-dimethylpropyl)carbamoyl]-5,5-dimethyl-1,3-thiazolidin-3-yl]-4-oxo-1-phenylbutan-2-yl]-N2-[(2S)-2-[(methoxycarbonyl)amino]-2-phenylacetyl]-3-methyl-L-valinamide
-
-
N-[(2S)-4-[(4R)-4-[(2-tert-butylhydrazinyl)carbonyl]-5,5-dimethyl-1,3-thiazolidin-3-yl]-4-oxo-1-phenylbutan-2-yl]-N2-[(2S)-2-[(methoxycarbonyl)amino]-2-phenylacetyl]-3-methyl-L-valinamide
-
-
N-[(2S,3R)-3-(acetylamino)-2-hydroxy-5-methylhexyl]-D-isoleucyl-D-valyl-D-prolinamide
-
-
N-[(2S,3R)-3-[(1-acetyl-D-prolyl)amino]-2-hydroxy-5-methylhexyl]-D-isoleucyl-D-valyl-D-prolinamide
-
-
N2-[(2S)-2-(b-alanylamino)-2-phenylacetyl]-N-[(2S)-4-[(4R)-4-[(2,2-dimethylpropyl)carbamoyl]-5,5-dimethyl-1,3-thiazolidin-3-yl]-4-oxo-1-phenylbutan-2-yl]-3-methyl-L-valinamide
-
-
N2-[(2S)-2-(butanoylamino)-2-phenylacetyl]-N-[(2S)-4-[(4R)-4-[(2,2-dimethylpropyl)carbamoyl]-5,5-dimethyl-1,3-thiazolidin-3-yl]-4-oxo-1-phenylbutan-2-yl]-3-methyl-L-valinamide
-
-
N2-[(2S)-2-amino-2-(2,4,6-trifluorophenyl)ethyl]-N-[(2S)-4-[(4R)-4-[(2,2-dimethylpropyl)carbamoyl]-5,5-dimethyl-1,3-thiazolidin-3-yl]-4-oxo-1-phenylbutan-2-yl]-3-methyl-L-valinamide
-
-
phenyl (9S)-5-cyclopentyl-3,6,9-trihydroxy-2-(naphthalen-2-yl)-2,5,8,10-tetraazadodecane-12-sulfonate
-
-
Pro-Gln-Val-(allophenylnorstatine)-[(R)-5,5-dimethyl-1,3-thiazolidine-4-carboxylic acid]-Val-Met-His-Pro
-
-
Pro-Gln-Val-[(4S,3S)-4-amino-3-hydroxy-6-methylheptanoic acid]-Ala-Leu
-
-
purvalanol-A
-
shows interactions with both chain A Gly34 and chain B Asp32 and Gly34 amino acid residues of the wild-type enzyme. Purvalanol A shows week interactions with the mutant HTLV-1 PR
tert-butyloxycarbonyl-Val-Val-Phe-Psi[P(O)(OH)]-Phe-Val-Val-NH2
-
-
tetradecahydrophenazine-2,3-diamine
-
inhibitory to both protease and HTLV-1 infected cells
2-(4-tert-butylphenyl)-N-carbamoyl-N-[3-[([[(3,5-dichloro-4-oxopyridin-1(4H)-yl)methyl]sulfamoyl]carbonyl)amino]-3-[3-(hydroxyamino)-4-oxopyrrolidin-1-yl]propyl]acetamide
-
strong inhibition, enzyme-bound structure modelling and molecular dynamics
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2-(4-tert-butylphenyl)-N-carbamoyl-N-[3-[([[(3,5-dichloro-4-oxopyridin-1(4H)-yl)methyl]sulfamoyl]carbonyl)amino]-3-[3-(hydroxyamino)-4-oxopyrrolidin-1-yl]propyl]acetamide
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Ac-Ser-Leu-Asn-Phe-CH(OH)CH2NH-Pro-Ile-Val-methyl ester
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i.e. JG-365
Ac-Ser-Leu-Asn-Phe-CH(OH)CH2NH-Pro-Ile-Val-methyl ester
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KNI-10681
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HTLV-1 PR-specific inhibitor, 40% inhibition at 50 nM
KNI-10683
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HTLV-1 PR-specific inhibitor, 76% inhibition at 50 nM
KNI-10729
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HTLV-1 PR-specific inhibitor, 79% inhibition at 50 nM
KNI-1595b
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HTLV-1 PR-specific inhibitor, 5% inhibition at 50 nM
N-(3-[[(benzylsulfamoyl)carbonyl]amino]-1-cyclopentylpropyl)-N-carbamoyl-N2-hydroxy-N2-(hydroxymethyl)glycinamide
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strong inhibition, enzyme-bound structure modelling and molecular dynamics
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N-(3-[[(benzylsulfamoyl)carbonyl]amino]-1-cyclopentylpropyl)-N-carbamoyl-N2-hydroxy-N2-(hydroxymethyl)glycinamide
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additional information
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currently employed HIV protease inhibitors can not be used to treat HTLV infections
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additional information
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several inhibitors of HIV-1 or other retrovitral proteinases are tested on HTLV-1 proteinase, only two inhibit with a Ki-value lower than 100 nM
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additional information
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the HIV type 1 protease inhibitors indinavir, saquinavir, ritonavir, or nelfinavir fail to block processing of HTLV-1 Gag
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additional information
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Ac-Thr-Ile-Nle(reduced peptide bond)-Nle-Gln-Arg; Arg-Val-Leu(reduced peptide bond)-Phe-Glu-Ala-Nle-NH2; Ser-Gln-Asn-Phe(reduced peptide bond)-Pro-Ile-Val
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additional information
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results show that a tetrapeptide sequence is necessary to achieve potent inhibition
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additional information
design of inhibitory compounds that circumvent the dominant residue Met37 in the binding pocket
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additional information
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design of inhibitory compounds that circumvent the dominant residue Met37 in the binding pocket
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additional information
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structure-function relationships and binding mode analysis, detailed overview. Comparisons with HIV protease
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additional information
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inhibitor design and evaluation of 15 inhibitory compounds based on the conformations of a class of HIV-1 aspartyl protease inhibitor sulfonamid-peptoid, molecular docking study and molecular dynamics simulations, hydrogen bond patterns, overview. The addition of two cyclic hydrocarbons to both ends of sulfonamide peptoids leads to the formation of new hydrophobic interactions due to the semi-circular form of these compounds, connecting the first chain of protease to the two ends of tested ligands via hydrophobic interactions. The strongest H-bond interaction has occurs between 2-(4-tert-butylphenyl)-N-carbamoyl-N-[3-[([[(3,5-dichloro-4-oxopyridin-1(4H)-yl)methyl]sulfamoyl]carbonyl)amino]-3-[3-(hydroxyamino)-4-oxopyrrolidin-1-yl]propyl]acetamide and N-(3-[[(benzylsulfamoyl)carbonyl]amino]-1-cyclopentylpropyl)-N-carbamoyl-N2-hydroxy-N2-(hydroxymethyl)glycinamide inhibitors with both S3 and S4 subsite in first chain of HTLV-1 protease
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additional information
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inhibitor library screening, free energy calculation, molecular docking, and molecular dynamics simulations, molecular modelling using the crystal structure of HTLV-1 PR (PDB ID 2B7F), overview. Molecular recognition and interaction analysis. HIV protease drugs fail to inhibit HTLV-1 infections. The active site region is expanded in HTLV-1 protease, and the known HIV protease drugs cannot sustain the inhibitory profile against the HTLV-1 PR
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