Reaction Details |
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Target | Dimer of Gag-Pol polyprotein [501-599,Q508K,L534I,L564I,C568A,C596A,I551V] |
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Ligand | BDBM13935 |
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Substrate/Competitor | Chromogenic Substrate |
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Meas. Tech. | Protease Inhibition Assay |
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pH | 5±n/a |
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Temperature | 295.15±n/a K |
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Ki | 230±n/a nM |
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Km | 500000±36000 nM |
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Comments | kcat/Km=0.93 +/- 0.08 min-1uM-1 |
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Citation | Liu, F; Boross, PI; Wang, YF; Tozser, J; Louis, JM; Harrison, RW; Weber, IT Kinetic, stability, and structural changes in high-resolution crystal structures of HIV-1 protease with drug-resistant mutations L24I, I50V, and G73S. J Mol Biol354:789-800 (2005) [PubMed] Article |
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More Info.: | Get all data from this article, Solution Info, Assay Method |
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Dimer of Gag-Pol polyprotein [501-599,Q508K,L534I,L564I,C568A,C596A,I551V] |
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Name: | Dimer of Gag-Pol polyprotein [501-599,Q508K,L534I,L564I,C568A,C596A,I551V] |
Synonyms: | HIV-1 Protease Mutant (I50V) |
Type: | Protein Complex |
Mol. Mass.: | n/a |
Description: | The HIV-1 PR DNA for all of wildtype and mutants was cloned, and protein was expressed, purified, and refolded from Escherichia coli strain BL21. |
Components: | This complex has 2 components. |
Component 1 |
Name: | Gag-Pol polyprotein [501-599,Q508K,L534I,L564I,C568A,C596A,I551V] |
Synonyms: | HIV-1 Protease Mutant (I50V) chain A | HIV-1 Protease Mutant (I50V) chain B | POL_HV1BR | gag-pol |
Type: | Enzyme Subunit |
Mol. Mass.: | 10718.08 |
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: | PQITLWKRPLVTIKIGGQLKEALLDTGADDTVIEEMSLPGRWKPKMIGGVGGFIKVRQYD
QIIIEIAGHKAIGTVLVGPTPVNIIGRNLLTQIGATLNF
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Component 2 |
Name: | Gag-Pol polyprotein [501-599,Q508K,L534I,L564I,C568A,C596A,I551V] |
Synonyms: | HIV-1 Protease Mutant (I50V) chain A | HIV-1 Protease Mutant (I50V) chain B | POL_HV1BR | gag-pol |
Type: | Enzyme Subunit |
Mol. Mass.: | 10718.08 |
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: | PQITLWKRPLVTIKIGGQLKEALLDTGADDTVIEEMSLPGRWKPKMIGGVGGFIKVRQYD
QIIIEIAGHKAIGTVLVGPTPVNIIGRNLLTQIGATLNF
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BDBM13935 |
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Chromogenic Substrate |
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Name: | Chromogenic Substrate |
Synonyms: | CA/p2# |
Type: | Peptide |
Mol. Mass.: | 2887.67 |
Organism: | n/a |
Description: | n/a |
Residue: | 25 |
Sequence: | K-A-R-V-Nle-(p-nitroPhe)-E-A-Nle-amide
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