Literature summary for 3.4.23.B8 extracted from

Zhang, M.; Nguyen, J.T.; Kumada, H.O.; Kimura, T.; Cheng, M.; Hayashi, Y.; Kiso, Y.
Synthesis and activity of tetrapeptidic HTLV-I protease inhibitors possessing different P(3)-cap moieties (2008), Bioorg. Med. Chem., 16, 5795-5802.

Search for more literature for 3.4.23.B8

Protein Variants

Protein Variants	Comment	Organism
L40I	protease used in the assay is an L40I mutant of the wild-type protease to prevent autolysis and improve stability	Human T-cell leukemia virus type I

Inhibitors

Inhibitors	Comment	Organism	Structure
(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	-	Human T-cell leukemia virus type I
(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	-	Human T-cell leukemia virus type I
(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	-	Human T-cell leukemia virus type I
(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	-	Human T-cell leukemia virus type I
(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	-	Human T-cell leukemia virus type I
(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	-	Human T-cell leukemia virus type I
(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	-	Human T-cell leukemia virus type I
(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	-	Human T-cell leukemia virus type I
(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	-	Human T-cell leukemia virus type I
(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	-	Human T-cell leukemia virus type I
(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	-	Human T-cell leukemia virus type I
(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	-	Human T-cell leukemia virus type I
(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	-	Human T-cell leukemia virus type I
(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	-	Human T-cell leukemia virus type I
(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	-	Human T-cell leukemia virus type I
(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	-	Human T-cell leukemia virus type I
(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	-	Human T-cell leukemia virus type I

Organism

Organism	UniProt	Comment	Textmining
Human T-cell leukemia virus type I	-	-	-

Synonyms

Synonyms	Comment	Organism
HTLV-I protease	-	Human T-cell leukemia virus type I

IC50 Value

IC50 Value	IC50 Value Maximum	Comment	Organism	Inhibitor	Structure
0.0000792	-	assay performed with mutant L40I	Human T-cell leukemia virus type I	(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
0.0000804	-	assay performed with mutant L40I	Human T-cell leukemia virus type I	(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
0.0000833	-	assay performed with mutant L40I	Human T-cell leukemia virus type I	(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
0.0000842	-	assay performed with mutant L40I	Human T-cell leukemia virus type I	(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
0.0000882	-	assay performed with mutant L40I	Human T-cell leukemia virus type I	(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
0.000092	-	assay performed with mutant L40I	Human T-cell leukemia virus type I	(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
0.0000935	-	assay performed with mutant L40I	Human T-cell leukemia virus type I	(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
0.0000965	-	assay performed with mutant L40I	Human T-cell leukemia virus type I	(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
0.0000969	-	assay performed with mutant L40I	Human T-cell leukemia virus type I	(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
0.0000982	-	assay performed with mutant L40I	Human T-cell leukemia virus type I	(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
0.0001017	-	assay performed with mutant L40I	Human T-cell leukemia virus type I	(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
0.0001043	-	assay performed with mutant L40I	Human T-cell leukemia virus type I	(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
0.0001045	-	assay performed with mutant L40I	Human T-cell leukemia virus type I	(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
0.0001048	-	assay performed with mutant L40I	Human T-cell leukemia virus type I	(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
0.000107	-	assay performed with mutant L40I	Human T-cell leukemia virus type I	(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
0.000331	-	assay performed with mutant L40I	Human T-cell leukemia virus type I	(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

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Release 2023.1 (January 2023)