Information on EC 3.4.23.B8 - human T-cell leukemia virus type 1 protease

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The expected taxonomic range for this enzyme is: Human T-lymphotropic virus 1

EC NUMBER
COMMENTARY hide
3.4.23.B8
preliminary BRENDA-supplied EC number
RECOMMENDED NAME
GeneOntology No.
human T-cell leukemia virus type 1 protease
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REACTION
REACTION DIAGRAM
COMMENTARY hide
ORGANISM
UNIPROT
LITERATURE
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.
show the reaction diagram
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REACTION TYPE
ORGANISM
UNIPROT
COMMENTARY hide
LITERATURE
hydrolysis of peptide bond
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CAS REGISTRY NUMBER
COMMENTARY hide
144114-21-6
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GENERAL INFORMATION
ORGANISM
UNIPROT
COMMENTARY hide
LITERATURE
physiological function
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HTLV-1 protease is an aspartic protease and crucial for processing of the virus proteins
SUBSTRATE
PRODUCT                       
REACTION DIAGRAM
ORGANISM
UNIPROT
COMMENTARY
(Substrate) hide
LITERATURE
(Substrate)
COMMENTARY
(Product) hide
LITERATURE
(Product)
Reversibility
r=reversible
ir=irreversible
?=not specified
(((4-((4-dimethylamino)phenyl)azo)phenyl)sulfonyl)amino-(gamma-aminobutyric acid)-PQVL-F(NO2)-VMH-(5-(2-aminoethylamino)-1-naphthalenesulfonic acid) + H2O
(((4-((4-dimethylamino)phenyl)azo)phenyl)sulfonyl)amino-(gamma-aminobutyric acid)-PQVL + F(NO2)-VMH-(5-(2-aminoethylamino)-1-naphthalenesulfonic acid)
show the reaction diagram
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-
-
?
(((4-((4-dimethylamino)phenyl)azo)phenyl)sulfonyl)amino-(gamma-aminobutyric acid)-PQVL-PVMH-(5-(2-aminoethylamino)-1-naphthalenesulfonic acid) + H2O
(((4-((4-dimethylamino)phenyl)azo)phenyl)sulfonyl)amino-(gamma-aminobutyric acid)-PQVL + PVMH-(5-(2-aminoethylamino)-1-naphthalenesulfonic acid)
show the reaction diagram
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?
4-((4-dimethylaminophenylazo)benzoyl)-(gamma-aminobutyric acid)-PQVL-(4-nitro)Phe-VMH-(5-(2-aminoethylamino)-1-naphthalenesulfonic acid) + H2O
?
show the reaction diagram
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?
Ac-Ala-Pro-Gln-Val-Sta-Val-Met-His-Pro
?
show the reaction diagram
Ac-DALLITPVLQLSPAF-OH + H2O
Ac-DALLITPVLQL-OH + SPAF-OH
show the reaction diagram
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peptide corresponding to the amino acids ranging from Asp1157 to Ala1169 of the pol open reading frame of HTLV-I
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?
Ac-KDKT-(N-o-aminobenzoyl)KVL-(4-nitro)FVQPKK-NH2 + H2O
Ac-KDKT-(N-o-aminobenzoyl)KVL + (4-nitro)FVQPKK-NH2
show the reaction diagram
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fluorogenic substrate
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-
?
Ace-Pro-Val-Ile-Leu-Pro-Ile-NMe + H2O
Ace-Pro-Val-Ile-Leu + Pro-Ile-NMe
show the reaction diagram
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-
-
?
Ala-Pro-Gln-Val-Sta-Val-Met-His-Pro-Leu + H2O
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show the reaction diagram
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substrate mimicks the natural Gag-Pol cleavage site of HTLV-1
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?
APQVLF(NO2)VMHPL + H2O
?
show the reaction diagram
APQVLF(NO2)VMHPL + H2O
APQVL + F(NO2)VMHP
show the reaction diagram
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-
-
-
?
APQVLPVMHP + H2O
APQVL + PVMHP
show the reaction diagram
APQVLPVMHPHG + H2O
APQVL + PVMHPHG
show the reaction diagram
dabsyl-(GABA)-PQVLPVMH-EDANS + H2O
dabsyl-(GABA)-PQVL + PVMH-EDANS
show the reaction diagram
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fluorogenic peptide substrate containing a MA/CA cleavage site
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-
?
dabsyl-KTKVLVVQPK-EDANS + H2O
dabsyl-KTKVL + VVQPK-EDANS
show the reaction diagram
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i.e. peptide substrate IB268, fluorescent-labeled
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?
DELILPVKRK + H2O
DELIL + PVKRK
show the reaction diagram
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?
DKELYPLTSL + H2O
DKELY + PLTSL
show the reaction diagram
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low activity
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?
DPASILPVIP + H2O
DPASIL + PVIP
show the reaction diagram
eukaryotic initiation factor eIF4GI + H2O
?
show the reaction diagram
gag precursor + H2O
?
show the reaction diagram
HTLV-1 Gag + H2O
?
show the reaction diagram
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processing of the HTLV-1 Gag protein
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-
?
IPFAAAQQRK + H2O
IPFAA + AQQRK
show the reaction diagram
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-
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?
IQPLIMAVVNR + H2O
IQPLIM + AVVNR
show the reaction diagram
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good substrate
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-
?
IRKILFLDG + H2O
IRKIL + FLDG
show the reaction diagram
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-
-
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?
IRQVLFLEKI + H2O
IRQVL + FLEKI
show the reaction diagram
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good substrate
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-
?
KAKVLVVQPK + H2O
KAKVL + VVQPK
show the reaction diagram
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-
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?
KDKVLVVQPK + H2O
KDKVL + VVQPK
show the reaction diagram
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-
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?
KGPPVICPIQA + H2O
KGPPVIC + PIQA
show the reaction diagram
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the preferred amino acids at the P1 position, except for Leu, are hydrophobic Phe and sulfur-containing amino acids (Met and Cys). Substrates which contain a charged side chain at the P1 position are not cleaved
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?
KGPPVIFPIQA + H2O
KGPPVIF + PIQA
show the reaction diagram
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the preferred amino acids at the P1 position, except for Leu, are hydrophobic Phe and sulfur-containing amino acids (Met and Cys). Substrates which contain a charged side chain at the P1 position are not cleaved
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?
KGPPVILPIQA + H2O
KGPPVIL + PIQA
show the reaction diagram
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Pro residue at the P1' position is the preferred amino acid for hydrolysis, and no replacement at the P1' position seems to be tolerated
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?
KGPPVILPIQAP + H2O
?
show the reaction diagram
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12-residue standard peptide, 100% cleavage
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?
KGPPVILPIQAP + H2O
KGPPVIL + PIQAP
show the reaction diagram
KGPPVIMPIQA + H2O
KGPPVIM + PIQA
show the reaction diagram
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the preferred amino acids at the P1 position, except for Leu, are hydrophobic Phe and sulfur-containing amino acids (Met and Cys). Substrates which contain a charged side chain at the P1 position are not cleaved
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?
KGVKVLVVQPK + H2O
KGKVL + VVQPK
show the reaction diagram
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?
KLKVLVVQPK + H2O
KLKVL + VVQPK
show the reaction diagram
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?
KPVKVLVVQPK + H2O
KPKVL + VVQPK
show the reaction diagram
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?
KQPAILVHTPG + H2O
KQPAIL + VHTPG
show the reaction diagram
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?
KSKVLVVQPK + H2O
KSKVL + VVQPK
show the reaction diagram
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?
KTAVLVVQPK + H2O
KTAVL + VVQPK
show the reaction diagram
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?
KTDVLVVQPK + H2O
KTDVL + VVQPK
show the reaction diagram
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?
KTFVLVVQPK + H2O
KTFVL + VVQPK
show the reaction diagram
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?
KTGVLVVQPK + H2O
KTGVL + VVQPK
show the reaction diagram
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?
KTKFLVVQPK + H2O
KTKFL + VVQPK
show the reaction diagram
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?
KTKILVVQPK + H2O
KTKIL + VVQPK
show the reaction diagram
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?
KTKLLVVQPK + H2O
KTKLL + VVQPK
show the reaction diagram
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?
KTKVAVVQPK + H2O
KTKVA + VVQPK
show the reaction diagram
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?
KTKVFVVQPK + H2O
KTKVF + VVQPK
show the reaction diagram
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?
KTKVGFVQPK + H2O
KTKVG + FVQPK
show the reaction diagram
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?
KTKVGIVQPK + H2O
KTKVG + IVQPK
show the reaction diagram
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?
KTKVGVVQPK + H2O
KTKVG + VVQPK
show the reaction diagram
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?
KTKVLLVQPK + H2O
KTKVL + LVQPK
show the reaction diagram
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?
KTKVLVVQPK + H2O
KTKVL + VVQPK
show the reaction diagram
KTKVMGVVQPK + H2O
KTKVM + VVQPK
show the reaction diagram
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?
KTKVYVVQPK + H2O
KTKVY + VVQPK
show the reaction diagram
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?
KTLVLVVQPK + H2O
KTLVL + VVQPK
show the reaction diagram
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?
KTSVLVVQPK + H2O
KTSVL + VVQPK
show the reaction diagram
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-
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?
KTVVLVVQPK + H2O
KTVVL + VVQPK
show the reaction diagram
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-
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?
KVKVLVVQPK + H2O
KVKVL + VVQPK
show the reaction diagram
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-
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?
LTFTFPVVFMRR + H2O
LTFTF + PVVFMRR
show the reaction diagram
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low activity
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?
N6-(7-methoxycoumarin-4-yl)acetyl-L-Lys-L-Ala-L-Pro-L-Gln-L-Val-L-Leu-4-nitro-L-phenylalanine-L-Val-L-Met-L-His-L-Pro-L-Leu + H2O
L-Lys-(7-methoxycoumarin-4-yl)acetyl-L-Ala-L-Pro-L-Gln-L-Val-L-Leu + 4-nitro-L-phenylalanine-L-Val-L-Met-L-His-L-Pro-L-Leu
show the reaction diagram
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?
PKDIFPVTET + H2O
PKDIF + PVTET
show the reaction diagram
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-
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?
PLQVLTLNIERR + H2O
PLQVL + TLNIERR
show the reaction diagram
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?
PPAILPIISE + H2O
PPAIL + PIISE
show the reaction diagram
PPMVGVLDAP + H2O
PPMVG + VLDAP
show the reaction diagram
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-
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?
PPVILPIQ + H2O
?
show the reaction diagram
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-
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?
PPVILPIQA + H2O
?
show the reaction diagram
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a 9-residue peptide is cleaved approximately at 85% of the 12-residue standard peptide
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?
PPVILPIQAP + H2O
?
show the reaction diagram
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?
PPVMGVLDAP + H2O
PPVMG + VLDAP
show the reaction diagram
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?
PQVLPVMHP + H2O
PQVL + PVMHP
show the reaction diagram
PVILPIQ + H2O
?
show the reaction diagram
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minimal sequence required for substrate recognition is a 7-residue peptide
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-
?
PVILPIQA + H2O
?
show the reaction diagram
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?
PVILPIQAP + H2O
?
show the reaction diagram
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?
PVVAMPVVIK + H2O
PVVAM + PVVIK
show the reaction diagram
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-
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?
RATVLTVALH + H2O
RATVL + TVALH
show the reaction diagram
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-
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?
TKVLVVQPK + H2O
TKVL + VVQPK
show the reaction diagram
VLQLYPIVQ + H2O
VLQLY + PIVQ
show the reaction diagram
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-
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?
VMQIYPIVQ + H2O
VMQIY + PIVQ
show the reaction diagram
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-
-
?
VSQCYPIVG + H2O
VSQCY + PIVG
show the reaction diagram
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peptides with an Ile or Leu at position P2 are the best substrate, lower activity with Val or Cys at position P2, no activity with Ala, Phe, Gly Thr or An at position P2
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-
?
VSQIYPIVG + H2O
VSQIY + PIVG
show the reaction diagram
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peptides with an Ile or Leu at position P2 are the best substrate, lower activity with Val or Cys at position P2, no activity with Ala, Phe, Gly Thr or An at position P2
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-
?
VSQLYPIVG + H2O
VSQLY + PIVG
show the reaction diagram
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peptides with an Ile or Leu at position P2 are the best substrate, lower activity with Val or Cys at position P2, no activity with Ala, Phe, Gly Thr or An at position P2
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?
VSQNYPIVQ + H2O
VSQNY + PIVQ
show the reaction diagram
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-
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?
VSQVYPIVG + H2O
VSQVY + PIVG
show the reaction diagram
-
peptides with an Ile or Leu at position P2 are the best substrate, lower activity with Val or Cys at position P2, no activity with Ala, Phe, Gly Thr or An at position P2
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?
VSQVYPIVQ + H2O
VSQVY + PIVQ
show the reaction diagram
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?
YVEPTAPQVLPVMHP + H2O
?
show the reaction diagram
additional information
?
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NATURAL SUBSTRATES
NATURAL PRODUCTS
REACTION DIAGRAM
ORGANISM
UNIPROT
COMMENTARY
(Substrate) hide
LITERATURE
(Substrate)
COMMENTARY
(Product) hide
LITERATURE
(Product)
REVERSIBILITY
r=reversible
ir=irreversible
?=not specified
eukaryotic initiation factor eIF4GI + H2O
?
show the reaction diagram
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in transfected COS-7 cells
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-
?
HTLV-1 Gag + H2O
?
show the reaction diagram
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processing of the HTLV-1 Gag protein
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?
additional information
?
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METALS and IONS
ORGANISM
UNIPROT
COMMENTARY hide
LITERATURE
NaCl
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activates at 4 M
INHIBITORS
ORGANISM
UNIPROT
COMMENTARY hide
LITERATURE
IMAGE
(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
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(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
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(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
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(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
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(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
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(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
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(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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(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
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(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
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-
(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
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(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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4-[(anilinocarbonyl)amino]-6-chlorobenzene-1,3-disulfonamide
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Ac-Ala-Pro-Gln-Val-Sta-Val-Met-His-Pro
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19% inhibition at 50 nM
Ac-Ala-Pro-Gln-Val-statine-Val-Met-His-Pro
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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
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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
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HTLV-I inhibition below 30%
Ac-Gln-Val-allophenylnorstatine-(R)-5,5-dimethyl-1,3-thiazolidine-4-carboxylic acid-Ile-Met-NH2
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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
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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-Lys-Ala-Gln-Ile-His-Phe
-
-
Ac-Leu-Val-allophenylnorstatine-(R)-5,5-dimethyl-1,3-thiazolidine-4-carboxylic acid-Val-Met-NH2
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HTLV-I inhibition 83%
Ac-Leu-Val-Phe-H
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-
Ac-Phe-Val-allophenylnorstatine-(R)-5,5-dimethyl-1,3-thiazolidine-4-carboxylic acid-Val-Met-NH2
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HTLV-I inhibition 74%
Ac-Pro-Gln-Ile-Thr-Leu-Trp-Gln-Arg-Pro-NH2
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-
Ac-Ser-Leu-Asn-Phe-CH(OH)CH2NH-Pro-Ile-Val-methyl ester
Ac-Thr-Leu-Asn-Phe
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-
Ac-Thr-Val-Ser-Phe-Asn-Phe
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-
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)
-
-
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)
-
-
acetyl-(L-(+)-alpha-phenylglycine)-(L-tert-leucine)-(allophenylnorstatine)-[(R)-5,5-dimethyl-1,3-thiazolidine-4-carboxylic acid]-((cyclopropyl)amino)
-
-
acetyl-(L-(+)-alpha-phenylglycine)-(L-tert-leucine)-(allophenylnorstatine)-[(R)-5,5-dimethyl-1,3-thiazolidine-4-carboxylic acid]-(2-methylbenzylamino)
-
-
acetyl-(L-(+)-alpha-phenylglycine)-(L-tert-leucine)-(allophenylnorstatine)-[(R)-5,5-dimethyl-1,3-thiazolidine-4-carboxylic acid]-(3-iodobenzylamino)
-
-
acetyl-(L-(+)-alpha-phenylglycine)-(L-tert-leucine)-(allophenylnorstatine)-[(R)-5,5-dimethyl-1,3-thiazolidine-4-carboxylic acid]-(prop-2-en-1-ylamino)
-
-
acetyl-(L-(+)-alpha-phenylglycine)-(L-tert-leucine)-(allophenylnorstatine)-[(R)-5,5-dimethyl-1,3-thiazolidine-4-carboxylic acid]-(propylamino)
-
-
acetyl-(L-(+)-alpha-phenylglycine)-(L-tert-leucine)-(allophenylnorstatine)-[(R)-5,5-dimethyl-1,3-thiazolidine-4-carboxylic acid]-Ile-Gln-NH2
-
-
acetyl-(L-(+)-alpha-phenylglycine)-(L-tert-leucine)-(allophenylnorstatine)-[(R)-5,5-dimethyl-1,3-thiazolidine-4-carboxylic acid]-Ile-Met-NH2
-
-
acetyl-(L-(+)-alpha-phenylglycine)-(L-tert-leucine)-(allophenylnorstatine)-[(R)-5,5-dimethyl-1,3-thiazolidine-4-carboxylic acid]-Ile-NH2
-
-
acetyl-(L-(+)-alpha-phenylglycine)-Ile-(allophenylnorstatine)-[(R)-5,5-dimethyl-1,3-thiazolidine-4-carboxylic acid]-Ile-Met-NH2
-
-
acetyl-(L-tert-leucine)-Ile-(allophenylnorstatine)-[(R)-5,5-dimethyl-1,3-thiazolidine-4-carboxylic acid]-Ile-Met-NH2
-
-
acetyl-Gln-Val-(allophenylnorstatine)-[(R)-5,5-dimethyl-1,3-thiazolidine-4-carboxylic acid]-Val-Met-NH2
-
-
acetyl-Ile-(L-(+)-alpha-phenylglycine)-(allophenylnorstatine)-[(R)-5,5-dimethyl-1,3-thiazolidine-4-carboxylic acid]-Ile-Met-NH2
-
-
acetyl-Ile-Ile-(allophenylnorstatine)-[(R)-5,5-dimethyl-1,3-thiazolidine-4-carboxylic acid]-(L-(+)-alpha-phenylglycine)-Met-NH2
-
-
acetyl-Ile-Ile-(allophenylnorstatine)-[(R)-5,5-dimethyl-1,3-thiazolidine-4-carboxylic acid]-(L-tert-leucine)-Met-NH2
-
-
acetyl-Ile-Ile-(allophenylnorstatine)-[(R)-5,5-dimethyl-1,3-thiazolidine-4-carboxylic acid]-Ile-Ala-NH2
-
-
acetyl-Ile-Ile-(allophenylnorstatine)-[(R)-5,5-dimethyl-1,3-thiazolidine-4-carboxylic acid]-Ile-Gln-NH2
-
-
acetyl-Ile-Ile-(allophenylnorstatine)-[(R)-5,5-dimethyl-1,3-thiazolidine-4-carboxylic acid]-Ile-Met-NH2
-
-
acetyl-Ile-Ile-(allophenylnorstatine)-[(R)-5,5-dimethyl-1,3-thiazolidine-4-carboxylic acid]-Ile-NH2
-
-
acetyl-Ile-Ile-(allophenylnorstatine)-[(R)-5,5-dimethyl-1,3-thiazolidine-4-carboxylic acid]-Ile-Phe-NH2
-
-
acetyl-Ile-Ile-(phenylnorstatine)-[(R)-5,5-dimethyl-1,3-thiazolidine-4-carboxylic acid]-Ile-Met-NH2
-
-
Ala-Pro-Gln-Val-statine-Val-Met-His-Pro
-
-
Gln-Met-Gln-Gly-Val-Leu-Tyr-Leu
-
-
H-allophenylnorstatine-Pro-Val-Met-His-OH
-
HTLV-I inhibition below 30%
H-Gln-Val-allophenylnorstatine-Pro-Val-Met-His-OH
-
HTLV-I inhibition below 30%
H-Ile- NHCH(CH2CH(CH3)2)CH(OH)CH2-Pro-NHCH2C6H5I
-
-
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
-
HTLV-I inhibition 86%
H-Pro-Gln-Val-allophenylnorstatine-Pro-Val-NH2
-
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
-
-
H-Pro-Val-Ile-hydroxyethylamine[(R)-isobutyl,(S)-hydroxy]-Pro-NH-CH2-C6H4I
-
-
H-Pro-Val-Ile-hydroxyethylamine[(S)-isobutyl,(R)-hydroxy]-Pro-NH-CH2-C6H4I
-
-
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
-
-
H-Pro-Val-Ile-NHCH(CH2CH(CH3)2)CH(OH)CH2-Pro-NHCH2C6H5I
-
-
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
-
-
H-Val-Ile-NHCH(CH2CH(CH3)2)CH(OH)CH2-Pro-NHCH2C6H5I
-
-
isobutyl oxycarbonyl-Lys--Val-Val-(3S,4S)-statine-Ala-isoamylamine
-
i.e. CS-I-27
isovaleryl-Lys-Val-(3S,4S)-statine-Ala-isoamylamine
-
i.e. CS-I-25
isovaleryl-Val-Nle-(3S,4S)-statine-Ala-isoamylamine
-
i.e. CS-I-22
isovaleryl-Val-Val-(3S,4S)-statine-Ala-Lys-methyl ester
-
i.e. CS-I-52
isovaleryl-Val-Val-(3S,4S)-statine-Lys-isoamylamine
-
i.e. CS-I-51
KNI-10220
-
HTLV-1 PR-specific inhibitor, 61% inhibition at 50 nM
KNI-10296c
-
HTLV-1 PR-specific inhibitor, 28% inhibition at 50 nM
KNI-10516
-
HTLV-1 PR-specific inhibitor, 86% inhibition at 50 nM
KNI-10562
-
78% inhibition at 50 nM
KNI-10673
-
29% inhibition at 50 nM
KNI-10681
-
HTLV-1 PR-specific inhibitor, 40% inhibition at 50 nM
KNI-10683
-
HTLV-1 PR-specific inhibitor, 76% inhibition at 50 nM
KNI-10729
-
HTLV-1 PR-specific inhibitor, 79% inhibition at 50 nM
KNI-1595b
-
HTLV-1 PR-specific inhibitor, 5% inhibition at 50 nM
N-[(2R)-2-[(1R)-2-[(2R)-1-(benzylcarbamoyl)pyrrolidin-2-yl]-1-hydroxyethyl]-4-methylpentanoyl]-D-isoleucyl-D-valyl-D-prolyl-D-prolinamide
-
-
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
-
-
Pro-Gln-Val-(allophenylnorstatine)-[(R)-5,5-dimethyl-1,3-thiazolidine-4-carboxylic acid]-Val-Met-His-Pro
-
-
Pro-Gln-Val-allophenylnorstatine-Pro-Val-Met-His-Pro
-
-
Pro-Gln-Val-[(4S,3S)-4-amino-3-hydroxy-6-methylheptanoic acid]-Ala-Leu
-
-
Pro-Val-Ile-Pro-Leu-Asp-Pro-Ala-Arg-Arg-Pro-Val
-
-
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
Tyr-Leu-Pro-Glu-Ala-Lys-Arg-Pro-Pro-Val-Ile-Leu
-
-
additional information
-
KM VALUE [mM]
SUBSTRATE
ORGANISM
UNIPROT
COMMENTARY hide
LITERATURE
IMAGE
0.058
(((4-((4-dimethylamino)phenyl)azo)phenyl)sulfonyl)amino-(gamma-aminobutyric acid)-PQVL-F(NO2)-VMH-(5-(2-aminoethylamino)-1-naphthalenesulfonic acid)
-
pH 5.2, 37C
0.06
(((4-((4-dimethylamino)phenyl)azo)phenyl)sulfonyl)amino-(gamma-aminobutyric acid)-PQVL-PVMH-(5-(2-aminoethylamino)-1-naphthalenesulfonic acid)
-
pH 5.2, 37C
0.055
4-((4-dimethylaminophenylazo)benzoyl)-(gamma-aminobutyric acid)-PQVL-(4-nitro)Phe-VMH-(5-(2-aminoethylamino)-1-naphthalenesulfonic acid)
-
pH 5.2, 37C
0.031 - 0.047
Ala-Pro-Gln-Val-Sta-Val-Met-His-Pro-Leu
-
0.042 - 0.062
APQVLF(NO2)VMHPL
0.061
APQVLNphVMHPL
-
pH 5.3, 37C
-
0.098 - 0.8
APQVLPVMHP
0.3 - 0.47
APQVLPVMHPHG
0.0068 - 0.01
dabsyl-(GABA)-PQVLPVMH-EDANS
0.23 - 0.244
DPASILPVIP
0.086
KAKVLVVQPK
-
5.6, 37C
0.48
KDKVLVVQPK
-
5.6, 37C
0.069
KGKVLVVQPK
-
5.6, 37C
0.03 - 0.034
KGPPVILPIQAP
0.23
KSKVLVVQPK
-
5.6, 37C
0.18
KTDVLVVQPK
-
5.6, 37C
0.13
KTFVLVVQPK
-
5.6, 37C
0.062
KTGVLVVQPK
-
5.6, 37C
0.04
KTKILVVQPK
-
5.6, 37C
0.028
KTKLLVVQPK
-
5.6, 37C
0.19
KTKVAVVQPK
-
5.6, 37C
0.049
KTKVFVVQPK
-
5.6, 37C
0.12
KTKVGVVQPK
-
5.6, 37C
0.18
KTKVLFVQPK
-
5.6, 37C
0.12
KTKVLIVQPK
-
5.6, 37C
0.032 - 2
KTKVLVVQPK
0.15
KTKVMVVQPK
-
5.6, 37C
0.19
KTKVYVVQPK
-
5.6, 37C
0.053
KTSVLVVQPK
-
5.6, 37C
7.31 - 54.7
N6-(7-methoxycoumarin-4-yl)acetyl-L-Lys-L-Ala-L-Pro-L-Gln-L-Val-L-Leu-4-nitro-L-phenylalanine-L-Val-L-Met-L-His-L-Pro-L-Leu
0.02
PPAILPIISE
-
-
0.014
PPVMGVLDAP
-
-
0.087
TKVLVVQPK
0.26
VSQIYPIVQ
-
pH 5.6, 37C
0.26
VSQLYPIVQ
-
pH 5.6, 37C
0.42
VSQVYPIVQ
-
pH 5.6, 37C
0.5
YVEPTAPQVLPVMHP
additional information
additional information
-
TURNOVER NUMBER [1/s]
SUBSTRATE
ORGANISM
UNIPROT
COMMENTARY hide
LITERATURE
IMAGE
0.2
(((4-((4-dimethylamino)phenyl)azo)phenyl)sulfonyl)amino-(gamma-aminobutyric acid)-PQVL-F(NO2)-VMH-(5-(2-aminoethylamino)-1-naphthalenesulfonic acid)
Human T-lymphotropic virus 1
-
pH 5.2, 37C
0.2
(((4-((4-dimethylamino)phenyl)azo)phenyl)sulfonyl)amino-(gamma-aminobutyric acid)-PQVL-PVMH-(5-(2-aminoethylamino)-1-naphthalenesulfonic acid)
Human T-lymphotropic virus 1
-
pH 5.2, 37C
0.2
4-((4-dimethylaminophenylazo)benzoyl)-(gamma-aminobutyric acid)-PQVL-(4-nitro)Phe-VMH-(5-(2-aminoethylamino)-1-naphthalenesulfonic acid)
Human T-lymphotropic virus 1
-
pH 5.2, 37C
0.000065 - 0.0009
Ala-Pro-Gln-Val-Sta-Val-Met-His-Pro-Leu
-
0.023 - 2.16
APQVLF(NO2)VMHPL
4.3 - 8.67
APQVLPVMHP
0.143
APQVLPVMHPHG
Human T-lymphotropic virus 1
-
-
0.0046 - 0.0057
dabsyl-(GABA)-PQVLPVMH-EDANS
0.62 - 0.7
DPASILPVIP
3.1
KAKVLVVQPK
Human T-lymphotropic virus 1
-
pH 5.6, 37C
1.1
KDKVLVVQPK
Human T-lymphotropic virus 1
-
pH 5.6, 37C
6.8
KGKVLVVQPK
Human T-lymphotropic virus 1
-
pH 5.6, 37C
6.26 - 6.91
KGPPVILPIQAP
2.5
KLKVLVVQPK
Human T-lymphotropic virus 1
-
pH 5.6, 37C
2.3
KPKVLVVQPK
Human T-lymphotropic virus 1
-
pH 5.6, 37C
9.2
KSKVLVVQPK
Human T-lymphotropic virus 1
-
pH 5.6, 37C
2.4
KTAVLVVQPK
Human T-lymphotropic virus 1
-
pH 5.6, 37C
2.3
KTDVLVVQPK
Human T-lymphotropic virus 1
-
pH 5.6, 37C
0.44
KTFVLVVQPK
Human T-lymphotropic virus 1
-
pH 5.6, 37C
1.2
KTGVLVVQPK
Human T-lymphotropic virus 1
-
pH 5.6, 37C
1.5
KTKFLVVQPK
Human T-lymphotropic virus 1
-
pH 5.6, 37C
2.5
KTKILVVQPK
Human T-lymphotropic virus 1
-
pH 5.6, 37C
3.3
KTKLLVVQPK
Human T-lymphotropic virus 1
-
pH 5.6, 37C
5.7
KTKVAVVQPK
Human T-lymphotropic virus 1
-
pH 5.6, 37C
16.4
KTKVFVVQPK
Human T-lymphotropic virus 1
-
pH 5.6, 37C
0.27
KTKVGVVQPK
Human T-lymphotropic virus 1
-
pH 5.6, 37C
0.36
KTKVLFVQPK
Human T-lymphotropic virus 1
-
pH 5.6, 37C
1.5
KTKVLIVQPK
Human T-lymphotropic virus 1
-
pH 5.6, 37C
3.7
KTKVLLVQPK
Human T-lymphotropic virus 1
-
pH 5.6, 37C
0.006 - 10
KTKVLVVQPK
4.1
KTKVMVVQPK
Human T-lymphotropic virus 1
-
pH 5.6, 37C
11.7
KTKVYVVQPK
Human T-lymphotropic virus 1
-
pH 5.6, 37C
0.52
KTLVLVVQPK
Human T-lymphotropic virus 1
-
pH 5.6, 37C
2.08
KTSVLVVQPK
Human T-lymphotropic virus 1
-
pH 5.6, 37C
0.48
KTVVLVVQPK
Human T-lymphotropic virus 1
-
pH 5.6, 37C
2.7
KVKVLVVQPK
Human T-lymphotropic virus 1
-
pH 5.6, 37C
0.64 - 42.9
N6-(7-methoxycoumarin-4-yl)acetyl-L-Lys-L-Ala-L-Pro-L-Gln-L-Val-L-Leu-4-nitro-L-phenylalanine-L-Val-L-Met-L-His-L-Pro-L-Leu
3.3
PPAILPIISE
Human T-lymphotropic virus 1
-
-
0.00833
PPVMGVLDAP
Human T-lymphotropic virus 1
-
-
0.22
PQVLPVMHP
Human T-lymphotropic virus 1
-
-
2.7
TKVLVVQPK
0.05
VSQIYPIVQ
Human T-lymphotropic virus 1
-
pH 5.6, 37C
0.05
VSQLYPIVQ
Human T-lymphotropic virus 1
-
pH 5.6, 37C
0.02
VSQVYPIVQ
Human T-lymphotropic virus 1
-
pH 5.6, 37C
0.085 - 0.184
YVEPTAPQVLPVMHP
additional information
additional information
Human T-lymphotropic virus 1
-
-
-
kcat/KM VALUE [1/mMs-1]
SUBSTRATE
ORGANISM
UNIPROT
COMMENTARY hide
LITERATURE
IMAGE
0.019 - 0.024
Ala-Pro-Gln-Val-Sta-Val-Met-His-Pro-Leu
206888
0.37 - 3.82
APQVLF(NO2)VMHPL
11285
1.14 - 10.4
APQVLPVMHP
6188
1.87 - 12.8
KTKVLVVQPK
3141
11.7 - 5860
N6-(7-methoxycoumarin-4-yl)acetyl-L-Lys-L-Ala-L-Pro-L-Gln-L-Val-L-Leu-4-nitro-L-phenylalanine-L-Val-L-Met-L-His-L-Pro-L-Leu
19615
Ki VALUE [mM]
INHIBITOR
ORGANISM
UNIPROT
COMMENTARY hide
LITERATURE
IMAGE
0.00008
4-[(anilinocarbonyl)amino]-6-chlorobenzene-1,3-disulfonamide
-
pH 5.6, 37C
0.00005
Ac-Ala-Pro-Gln-Val-statine-Val-Met-His-Pro
-
recombinant enzyme, pH 5.5, 37C
0.0506
Ac-Leu-Lys-Ala-Gln-Ile-His-Phe
-
-
0.093
Ac-Leu-Val-Phe-H
-
-
1.7
Ac-Pro-Gln-Ile-Thr-Leu-Trp-Gln-Arg-Pro-NH2
-
-
0.000006
Ac-Ser-Leu-Asn-Phe-CH(OH)CH2NH-Pro-Ile-Val-methyl ester
0.252
Ac-Thr-Leu-Asn-Phe
-
-
0.217
Ac-Thr-Val-Ser-Phe-Asn-Phe
-
-
0.00005
Ala-Pro-Gln-Val-statine-Val-Met-His-Pro
0.000466
CS-I-51
-
pH 5.3, 37C
0.07
Gln-Met-Gln-Gly-Val-Leu-Tyr-Leu
-
-
0.00494
H-Pro-Val-Ile-hydroxyethylamine[(R)-isobutyl,(R)-hydroxy]-Pro-NH-CH2-C6H4I
-
-
0.292
H-Pro-Val-Ile-hydroxyethylamine[(R)-isobutyl,(S)-hydroxy]-Pro-NH-CH2-C6H4I
-
-
0.038
H-Pro-Val-Ile-hydroxyethylamine[(S)-isobutyl,(R)-hydroxy]-Pro-NH-CH2-C6H4I
-
-
0.00549
H-Pro-Val-Ile-hydroxyethylamine[(S)-isobutyl,(S)-hydroxy]-Pro-NH-CH2-C6H4I
-
-
0.000142
isobutyl oxycarbonyl-Lys--Val-Val-(3S,4S)-statine-Ala-isoamylamine
-
pH 5.3, 37C
0.0000072
isovaleryl-Lys-Val-(3S,4S)-statine-Ala-isoamylamine
-
pH 5.3, 37C
0.000138
isovaleryl-Val-Nle-(3S,4S)-statine-Ala-isoamylamine
-
pH 5.3, 37C
0.0072
isovaleryl-Val-Val-(3S,4S)-statine-Ala-Lys-methyl ester
-
pH 5.3, 37C
0.00024 - 0.00243
MES13-099
0.017 - 0.2
pepstatin A
0.0872
Pro-Val-Ile-Pro-Leu-Asp-Pro-Ala-Arg-Arg-Pro-Val
-
-
0.00008
tert-butyloxycarbonyl-Val-Val-Phe[P(O)(OH)-]-Phe-Val-Val-NH2
-
-
0.0008
tetradecahydrophenazine-2,3-diamine
-
pH 5.6, 37C
0.0057
Tyr-Leu-Pro-Glu-Ala-Lys-Arg-Pro-Pro-Val-Ile-Leu
-
-
IC50 VALUE [mM]
INHIBITOR
ORGANISM
UNIPROT
COMMENTARY hide
LITERATURE
IMAGE
0.0000804
(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-lymphotropic virus 1
-
assay performed with mutant L40I
0.0000842
(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-lymphotropic virus 1
-
assay performed with mutant L40I
0.0000833
(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-lymphotropic virus 1
-
assay performed with mutant L40I
0.0001017
(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-lymphotropic virus 1
-
assay performed with mutant L40I
0.0000882
(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-lymphotropic virus 1
-
assay performed with mutant L40I
0.0001048
(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-lymphotropic virus 1
-
assay performed with mutant L40I
0.0000965
(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-lymphotropic virus 1
-
assay performed with mutant L40I
0.000107
(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-lymphotropic virus 1
-
assay performed with mutant L40I
0.000331
(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-lymphotropic virus 1
-
assay performed with mutant L40I
0.0000792
(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-lymphotropic virus 1
-
assay performed with mutant L40I
0.0000982
(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-lymphotropic virus 1
-
assay performed with mutant L40I
0.0000935
(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-lymphotropic virus 1
-
assay performed with mutant L40I
0.000092
(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-lymphotropic virus 1
-
assay performed with mutant L40I
0.0001045
(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-lymphotropic virus 1
-
assay performed with mutant L40I
0.0001043
(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-lymphotropic virus 1
-
assay performed with mutant L40I
0.0000969
(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-lymphotropic virus 1
-
assay performed with mutant L40I
0.000113
acetyl-(L-(+)-alpha-phenylglycine)-(L-tert-leucine)-(allophenylnorstatine)-[(R)-5,5-dimethyl-1,3-thiazolidine-4-carboxylic acid]-((2,2-dimethylpropyl)amino)
Human T-lymphotropic virus 1
-
-
0.00014
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)
Human T-lymphotropic virus 1
-
-
0.000107
acetyl-(L-(+)-alpha-phenylglycine)-(L-tert-leucine)-(allophenylnorstatine)-[(R)-5,5-dimethyl-1,3-thiazolidine-4-carboxylic acid]-((2-methylpropyl)amino)
Human T-lymphotropic virus 1
-
-
0.000146
acetyl-(L-(+)-alpha-phenylglycine)-(L-tert-leucine)-(allophenylnorstatine)-[(R)-5,5-dimethyl-1,3-thiazolidine-4-carboxylic acid]-((cyclopropyl)amino)
Human T-lymphotropic virus 1
-
-
0.000103
acetyl-(L-(+)-alpha-phenylglycine)-(L-tert-leucine)-(allophenylnorstatine)-[(R)-5,5-dimethyl-1,3-thiazolidine-4-carboxylic acid]-(2-methylbenzylamino)
Human T-lymphotropic virus 1
-
-
0.000473
acetyl-(L-(+)-alpha-phenylglycine)-(L-tert-leucine)-(allophenylnorstatine)-[(R)-5,5-dimethyl-1,3-thiazolidine-4-carboxylic acid]-(3-iodobenzylamino)
Human T-lymphotropic virus 1
-
-
0.000131
acetyl-(L-(+)-alpha-phenylglycine)-(L-tert-leucine)-(allophenylnorstatine)-[(R)-5,5-dimethyl-1,3-thiazolidine-4-carboxylic acid]-(prop-2-en-1-ylamino)
Human T-lymphotropic virus 1
-
-
0.000193
acetyl-(L-(+)-alpha-phenylglycine)-(L-tert-leucine)-(allophenylnorstatine)-[(R)-5,5-dimethyl-1,3-thiazolidine-4-carboxylic acid]-(propylamino)
Human T-lymphotropic virus 1
-
-
0.000084
acetyl-(L-(+)-alpha-phenylglycine)-(L-tert-leucine)-(allophenylnorstatine)-[(R)-5,5-dimethyl-1,3-thiazolidine-4-carboxylic acid]-Ile-Gln-NH2
Human T-lymphotropic virus 1
-
-
0.000101
acetyl-(L-(+)-alpha-phenylglycine)-(L-tert-leucine)-(allophenylnorstatine)-[(R)-5,5-dimethyl-1,3-thiazolidine-4-carboxylic acid]-Ile-Met-NH2
Human T-lymphotropic virus 1
-
-
0.000144
acetyl-(L-(+)-alpha-phenylglycine)-(L-tert-leucine)-(allophenylnorstatine)-[(R)-5,5-dimethyl-1,3-thiazolidine-4-carboxylic acid]-Ile-NH2
Human T-lymphotropic virus 1
-
-
0.000102
acetyl-(L-(+)-alpha-phenylglycine)-Ile-(allophenylnorstatine)-[(R)-5,5-dimethyl-1,3-thiazolidine-4-carboxylic acid]-Ile-Met-NH2
Human T-lymphotropic virus 1
-
-
0.000201
acetyl-(L-tert-leucine)-Ile-(allophenylnorstatine)-[(R)-5,5-dimethyl-1,3-thiazolidine-4-carboxylic acid]-Ile-Met-NH2
Human T-lymphotropic virus 1
-
-
0.000353
acetyl-Gln-Val-(allophenylnorstatine)-[(R)-5,5-dimethyl-1,3-thiazolidine-4-carboxylic acid]-Val-Met-NH2
Human T-lymphotropic virus 1
-
-
0.000145 - 0.00032
acetyl-Ile-(L-(+)-alpha-phenylglycine)-(allophenylnorstatine)-[(R)-5,5-dimethyl-1,3-thiazolidine-4-carboxylic acid]-Ile-Met-NH2
0.000123
acetyl-Ile-Ile-(allophenylnorstatine)-[(R)-5,5-dimethyl-1,3-thiazolidine-4-carboxylic acid]-(L-(+)-alpha-phenylglycine)-Met-NH2
Human T-lymphotropic virus 1
-
-
0.00018
acetyl-Ile-Ile-(allophenylnorstatine)-[(R)-5,5-dimethyl-1,3-thiazolidine-4-carboxylic acid]-(L-tert-leucine)-Met-NH2
Human T-lymphotropic virus 1
-
-
0.00016
acetyl-Ile-Ile-(allophenylnorstatine)-[(R)-5,5-dimethyl-1,3-thiazolidine-4-carboxylic acid]-Ile-Ala-NH2
Human T-lymphotropic virus 1
-
-
0.000159
acetyl-Ile-Ile-(allophenylnorstatine)-[(R)-5,5-dimethyl-1,3-thiazolidine-4-carboxylic acid]-Ile-Gln-NH2
Human T-lymphotropic virus 1
-
-
0.000088
acetyl-Ile-Ile-(allophenylnorstatine)-[(R)-5,5-dimethyl-1,3-thiazolidine-4-carboxylic acid]-Ile-Met-NH2
Human T-lymphotropic virus 1
-
-
0.000249
acetyl-Ile-Ile-(allophenylnorstatine)-[(R)-5,5-dimethyl-1,3-thiazolidine-4-carboxylic acid]-Ile-NH2
Human T-lymphotropic virus 1
-
-
0.000095
acetyl-Ile-Ile-(allophenylnorstatine)-[(R)-5,5-dimethyl-1,3-thiazolidine-4-carboxylic acid]-Ile-Phe-NH2
Human T-lymphotropic virus 1
-
-
0.00018
acetyl-Ile-Ile-(phenylnorstatine)-[(R)-5,5-dimethyl-1,3-thiazolidine-4-carboxylic acid]-Ile-Met-NH2
Human T-lymphotropic virus 1
-
-
0.0024
H-Pro-Pro-Val-Ile-NHCH(CH2CH(CH3)2)CH(OH)CH2-Pro-NHCH2C6H5I
Human T-lymphotropic virus 1
-
-
0.00013
H-Pro-Val-Ile-NHCH(CH2CH(CH3)2)CH(OH)CH2-Pro-Ile-NHCH2C6H5I
Human T-lymphotropic virus 1
-
-
0.0058
H-Pro-Val-Ile-NHCH(CH2CH(CH3)2)CH(OH)CH2-Pro-NHCH2C6H5I
Human T-lymphotropic virus 1
-
-
0.0183
H-Val-Ile-NHCH(CH2CH(CH3)2)CH(OH)CH2-Pro-Ile-NHCH2C6H5I
Human T-lymphotropic virus 1
-
-
0.0196
H-Val-Ile-NHCH(CH2CH(CH3)2)CH(OH)CH2-Pro-NHCH2C6H5I
Human T-lymphotropic virus 1
-
-
0.35
N-[(2R)-2-[(1R)-2-[(2R)-1-(benzylcarbamoyl)pyrrolidin-2-yl]-1-hydroxyethyl]-4-methylpentanoyl]-D-isoleucyl-D-valyl-D-prolyl-D-prolinamide
Human T-lymphotropic virus 1
-
in 0.5 M sodium acetate buffer, pH 5.6, containing 10% (v/v) glycerol, 10 mM dithiothretiol and 4 M NaCl, temperature not specified in the publication
1.5
N-[(2R)-2-[(1S)-2-[(2R)-1-(benzylcarbamoyl)pyrrolidin-2-yl]-1-hydroxyethyl]-4-methylpentanoyl]-D-isoleucyl-D-valyl-D-prolyl-D-prolinamide
Human T-lymphotropic virus 1
-
in 0.5 M sodium acetate buffer, pH 5.6, containing 10% (v/v) glycerol, 10 mM dithiothretiol and 4 M NaCl, temperature not specified in the publication
0.16
N-[(2S)-2-[(1R)-2-[(2R)-1-(benzylcarbamoyl)pyrrolidin-2-yl]-1-hydroxyethyl]-4-methylpentanoyl]-D-isoleucyl-D-valyl-D-prolyl-D-prolinamide
Human T-lymphotropic virus 1
-
in 0.5 M sodium acetate buffer, pH 5.6, containing 10% (v/v) glycerol, 10 mM dithiothretiol and 4 M NaCl, temperature not specified in the publication
0.55
N-[(2S)-2-[(1S)-2-[(2R)-1-(benzylcarbamoyl)pyrrolidin-2-yl]-1-hydroxyethyl]-4-methylpentanoyl]-D-isoleucyl-D-valyl-D-prolyl-D-prolinamide
Human T-lymphotropic virus 1
-
in 0.5 M sodium acetate buffer, pH 5.6, containing 10% (v/v) glycerol, 10 mM dithiothretiol and 4 M NaCl, temperature not specified in the publication
0.0000072
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
Human T-lymphotropic virus 1
-
recombinant protease mutant L40I, pH not specified in the publication, temperature not specified in the publication
0.0000104
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
Human T-lymphotropic virus 1
-
recombinant protease mutant L40I, pH not specified in the publication, temperature not specified in the publication
10
N-[(2S,3R)-3-(acetylamino)-2-hydroxy-5-methylhexyl]-D-isoleucyl-D-valyl-D-prolinamide
Human T-lymphotropic virus 1
-
IC50 above 10 mM, in 0.5 M sodium acetate buffer, pH 5.6, containing 10% (v/v) glycerol, 10 mM dithiothretiol and 4 M NaCl, temperature not specified in the publication
10
N-[(2S,3R)-3-[(1-acetyl-D-prolyl)amino]-2-hydroxy-5-methylhexyl]-D-isoleucyl-D-valyl-D-prolinamide
Human T-lymphotropic virus 1
-
IC50 above 10 mM, in 0.5 M sodium acetate buffer, pH 5.6, containing 10% (v/v) glycerol, 10 mM dithiothretiol and 4 M NaCl, temperature not specified in the publication
0.0000057
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
Human T-lymphotropic virus 1
-
recombinant protease mutant L40I, pH not specified in the publication, temperature not specified in the publication
0.0000064
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
Human T-lymphotropic virus 1
-
recombinant protease mutant L40I, pH not specified in the publication, temperature not specified in the publication
0.000013
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
Human T-lymphotropic virus 1
-
pH 5.6, 37C
0.000152
Pro-Gln-Val-(allophenylnorstatine)-[(R)-5,5-dimethyl-1,3-thiazolidine-4-carboxylic acid]-Val-Met-His-Pro
Human T-lymphotropic virus 1
-
-
0.000159
Pro-Gln-Val-allophenylnorstatine-Pro-Val-Met-His-Pro
Human T-lymphotropic virus 1
-
-
SPECIFIC ACTIVITY [µmol/min/mg]
ORGANISM
UNIPROT
COMMENTARY hide
LITERATURE
additional information
-
-
pH OPTIMUM
ORGANISM
UNIPROT
COMMENTARY hide
LITERATURE
pH RANGE
ORGANISM
UNIPROT
COMMENTARY hide
LITERATURE
5 - 5.4
-
pH 5.0: about 40% of maximal activity, pH 5.4: about 55% of maximal activity
TEMPERATURE OPTIMUM
ORGANISM
UNIPROT
COMMENTARY hide
LITERATURE
MOLECULAR WEIGHT
ORGANISM
UNIPROT
COMMENTARY hide
LITERATURE
13000
-
x * 13000, SDS-PAGE of recombinant enzyme
13672
-
x * 13672, ESI-MS of full length enzyme
14400
-
1 * 14400, SDS-PAGE; 2 * 14400, SDS-PAGE
27000
-
gel filtration
SUBUNITS
ORGANISM
UNIPROT
COMMENTARY hide
LITERATURE
monomer
-
1 * 14400, SDS-PAGE
trimer
-
the trimer consists of three homodimers
additional information
POSTTRANSLATIONAL MODIFICATION
ORGANISM
UNIPROT
COMMENTARY hide
LITERATURE
additional information
-
formation of a disulfide bridge, reversible oxidative modification as a mechanism for regulating retroviral protease dimerization and activation, regulation through reversible glutathionylation of its two conserved cysteine residues
Crystallization/COMMENTARY
ORGANISM
UNIPROT
LITERATURE
all-atom molecular dynamics simulations for both retroviral proteases from HIV-1 and HTLV-I in their ligand-free states and in complex with model substrates. The two catalytic aspartates D32/D32' of HTLV-PR exhibit slightly repulsive interactions with the substrate. Inspection of the electrostatic interaction energy, reveals a large attractive electrostatic interaction of D32/D32' with the substrate that overcompensates for the repulsive van der Waals interactions. The nonconserved residues HIV-PR D30/D30' and HTLV-PR M37/M37' also contribute strongly to the binding of the substrate analogs in both proteases. Interactions in both proteases occur at the same spatial sites and with similar binding energies. There care high similarities between the dynamic behaviors of the flap structures, especially in the ligand-free state
computer-assisted modeling experiments on inhibitor 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 in complex with a truncated L40I mutation HTLV-I protease show that hydrogen bond interactions are present throughout the backbone anchoring the docked compound with the catalytic Asp32 and Asp320 residues from each respective chain of the homodimeric protease, along with Gly340, Asp360, and Leu570. Hydrogen bond interactions with Asp36 and the flap residues Ala59 and Ala590 are mediated through water. Hydration of the terminal free amino group mediates a link with the amide nitrogen of Leu570
-
computer-assisted modeling using inhibitors 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 and 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
-
HTLV-1 PR complexed with Ac-Ala-Pro-Gln-Val-Sta-Val-Met-His-Pro, hanging drop vapor diffusion method, using 17% (w/v) PEG 8000, 16% PEG (w/v) 300, 0.1 M sodium acetate (pH 5.2), at 20C. HTLV-1 PR complexed with KNI-10562, hanging drop vapor diffusion method, using 26% (w/v) pentaerythritol ethoxylate and 0.2 M ZnSO4 in 0.1 M Bis-Tris buffer (pH 5.2), at 20C. HTLV-1PR complexed with KNI-10683, hanging drop vapor diffusion method, using 17% (w/v) PEG 8000, 16% (w/v) PEG 300, 10 mM dithiothreitol, and 0.2M KH2PO4 in 0.1 M Bis-Tris buffer, pH 5.2, at 20C
-
molecular dynamics simulation. In the apo-enzyme, the two catalytic residues are chemically equivalent and are expected to be both unprotonated. Upon substrate binding, the catalytic residues of HTLV-1 protease evolve to a singly protonated state, in which the carboxylic oxygen atom OD1 of Asp32 is protonated and forms a hydrogen bond with the OD1 atom of Asp32' , which is unprotonated
purified recombinant HTLV-1 PR in complex with inhibitor Ac-Ala-Pro-Gln-Val-statine-Val-Met-His-Pro, enzyme-inhibitor ratio of 1:10, 5C, hanging drop vapor diffusion method, mxing of 0.004 ml of protein solution and of well solution, the latter containing 17% PEG 8000, 16% PEG 300, and 10 mM DTT, in 0.1 M acetate buffer, pH 5.2, X-ray diffraction structure determination and analysis at 2.6 A resolution, structure analysis and modeling, overview
-
sequence and structural alignments of HTLV-1 protease and HIV-1 protease. 95% of ligand recognizing active site amino acids are common in both receptors, the approved drugs of HIV proteases are unable to function as HTLV-1 protease inhibitors. The reported amino acid Asp30 from HIV-1 proease is substituted as Met37 in HTLV protease. Met37 is playing the vital role in ejection of HIV protease inhibitors from the binding pocket of HTLV protease
STORAGE STABILITY
ORGANISM
UNIPROT
LITERATURE
mutant L40I does not form aggregates and is stable as a 240 microM pH 7.0 stock solution for at least 2 months at 4C, even with freeze-thawing
-
Purification/COMMENTARY
ORGANISM
UNIPROT
LITERATURE
HTLV1-protease and HTLV-I protease fused to the 27 amino acid pET10-b histidine tag
-
pET19-based expression clone containing HTLV-1 protease fused to a decahistidine-containing leader peptide
-
Q Sepharose column chromatography and SP Sepharose column chromatography
-
recombinant enzyme from inclusion bodies
-
Cloned/COMMENTARY
ORGANISM
UNIPROT
LITERATURE
amplification of a HTLV-1 protease gene fragment by polymerase chain reaction and cloning it into a pUC plasmid vector. The protease gene fragment contains an open reading frame capable of encoding the active HTLV-1 protease. To express a fusion protein of beta-galactosidase linked with the HTLV-1 protease in Escherichia coli, a plasmid DNA is constructed by insering the HTLV-1 protease gen DNA into a procaryotic expression vector, pUEX-2, consisting of a lacZ gene directed by a lambda phage Pr promoter and designated pUEX-pro. The fusion protein is successfully expressed
-
construction of a pET19-based expression clone containing HTLV-1 protease fused to a decahistidine-containing leader peptide, expression in Escherichia coli, autoprocessing of the purified fusion protein yields a 14000 Da protease
-
expressed in Escherichia coli Rosetta2(DE3)pLysS cells
-
expression of mutant L40I which prevents autolysis and enhances enzyme stability and substrate cleavage, in Escherichia coli
-
expression of truncated enzyme forms in Escherichia coli
-
expression of wild-type and mutant enzyme in Escherichia coli strain BL21(DE3)
-
expression of wild-type and mutant enzymes as maltose-binding protein fusion proteins
-
ENGINEERING
ORGANISM
UNIPROT
COMMENTARY hide
LITERATURE
A59I
-
site-directed mutagenesis, highly reduced activity compared to the wild-type enzyme, no folding
F67Q
-
site-directed mutagenesis, inactive mutant, no folding
L49I
-
autoproteolysis resistant mutant enzyme. KM-values and turnover-numbers are comparable to that of wild-type enzyme
L57G
-
site-directed mutagenesis, inactive mutant, no folding
M37A
-
site-directed mutagenesis, inactive mutant, no folding
M37I
-
site-directed mutagenesis, reduced activity and highly reduced folding efficiency compared to the wild-type enzyme
M37N
-
site-directed mutagenesis, inactive mutant, no folding
M37V
-
site-directed mutagenesis, reduced activity and folding efficiency compared to the wild-type enzyme
N96T
-
site-directed mutagenesis, highly reduced activity compared to the wild-type enzyme, no folding
N96T/N97P/W98V
-
site-directed mutagenesis, inactive mutant, no folding
N97P
-
site-directed mutagenesis, highly reduced activity compared to the wild-type enzyme, no folding
V56I
-
site-directed mutagenesis, inactive mutant, no folding
V56I/L57G/A59I
-
site-directed mutagenesis, reduced activity and folding efficiency compared to the wild-type enzyme
V56I/L57G/A59I/N96T/N97P/W98V
-
site-directed mutagenesis, inactive mutant, no folding
W98V
-
site-directed mutagenesis, highly reduced activity compared to the wild-type enzyme, no folding
additional information
Renatured/COMMENTARY
ORGANISM
UNIPROT
LITERATURE
recombinant enzyme from inclusion bodies by dialysis
-
the purified unfolded HTLV-1 PR is refolded by dialysis against 15 mM sodium acetate (pH 3.0), 5% (w/v) PEG 300, and 5 mM dithiothreitol
-
APPLICATION
ORGANISM
UNIPROT
COMMENTARY hide
LITERATURE
medicine