Reaction Details |
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Target | Dimer of Gag-Pol polyprotein [501-599,Q508K,L534I,L564I,C568A,C596A,V583A] |
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Ligand | BDBM8125 |
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Substrate/Competitor | HIV Peptide Substrate |
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Meas. Tech. | Protease Inhibition Assay |
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pH | 5.6±n/a |
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Temperature | 310.15±n/a K |
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Ki | 0.8±0.06 nM |
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Km | 26000±2000 nM |
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Comments | Kcat/Km=92±8 min-1nM-1 |
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Citation | Kovalevsky, AY; Tie, Y; Liu, F; Boross, PI; Wang, YF; Leshchenko, S; Ghosh, AK; Harrison, RW; Weber, IT Effectiveness of nonpeptide clinical inhibitor TMC-114 on HIV-1 protease with highly drug resistant mutations D30N, I50V, and L90M. J Med Chem49:1379-87 (2006) [PubMed] Article |
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More Info.: | Get all data from this article, Inhibition_Run data, Solution Info, Assay Method |
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Dimer of Gag-Pol polyprotein [501-599,Q508K,L534I,L564I,C568A,C596A,V583A] |
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Name: | Dimer of Gag-Pol polyprotein [501-599,Q508K,L534I,L564I,C568A,C596A,V583A] |
Synonyms: | HIV-1 Protease Mutant (V82A) |
Type: | Protein Complex |
Mol. Mass.: | n/a |
Description: | n/a |
Components: | This complex has 2 components. |
Component 1 |
Name: | Gag-Pol polyprotein [501-599,Q508K,L534I,L564I,C568A,C596A,V583A] |
Synonyms: | HIV-1 Protease Mutant (V82A) chain A | HIV-1 Protease Mutant (V82A) chain B | POL_HV1BR | gag-pol |
Type: | Enzyme Subunit |
Mol. Mass.: | 10704.05 |
Organism: | Human immunodeficiency virus type 1 |
Description: | All of the mutant constructs in this study are on the wild type containing the substitutions Q7K, L33I, and L63I, to minimize the autoproteolysis of the protease, and C67A and C95A, to prevent cysteine-thiol oxidation. |
Residue: | 99 |
Sequence: | PQITLWKRPLVTIKIGGQLKEALLDTGADDTVIEEMSLPGRWKPKMIGGIGGFIKVRQYD
QIIIEIAGHKAIGTVLVGPTPANIIGRNLLTQIGATLNF
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Component 2 |
Name: | Gag-Pol polyprotein [501-599,Q508K,L534I,L564I,C568A,C596A,V583A] |
Synonyms: | HIV-1 Protease Mutant (V82A) chain A | HIV-1 Protease Mutant (V82A) chain B | POL_HV1BR | gag-pol |
Type: | Enzyme Subunit |
Mol. Mass.: | 10704.05 |
Organism: | Human immunodeficiency virus type 1 |
Description: | All of the mutant constructs in this study are on the wild type containing the substitutions Q7K, L33I, and L63I, to minimize the autoproteolysis of the protease, and C67A and C95A, to prevent cysteine-thiol oxidation. |
Residue: | 99 |
Sequence: | PQITLWKRPLVTIKIGGQLKEALLDTGADDTVIEEMSLPGRWKPKMIGGIGGFIKVRQYD
QIIIEIAGHKAIGTVLVGPTPANIIGRNLLTQIGATLNF
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BDBM8125 |
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HIV Peptide Substrate |
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Name: | HIV Peptide Substrate |
Synonyms: | n/a |
Type: | Peptide |
Mol. Mass.: | 3156.95 |
Organism: | n/a |
Description: | n/a |
Residue: | 27 |
Sequence: | Ac-RE(Edans)SQNY*PIVRK(Dabcyl)R-CO-NH2
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