| Reaction Details |
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 | Report a problem with these data |
| Target | Dimer of Gag-Pol polyprotein [501-599,Q508K,L534I,L564I,C568A,C596A] |
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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 | 0.22±0.05 nM |
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| Km | 36000±8000 nM |
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| Comments | Kcat/Km=75±20 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] |
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| Name: | Dimer of Gag-Pol polyprotein [501-599,Q508K,L534I,L564I,C568A,C596A] |
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| Synonyms: | HIV-1 Protease |
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| Type: | Protein Complex |
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| Mol. Mass.: | n/a |
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| Description: | n/a |
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| Components: | This complex has 2 components. |
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| Component 1 |
| Name: | Gag-Pol polyprotein [501-599,Q508K,L534I,L564I,C568A,C596A] |
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| Synonyms: | HIV-1 Protease chain A | POL_HV1BR | gag-pol |
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| Type: | Enzyme Subunit |
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| Mol. Mass.: | 10732.11 |
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| Organism: | Human immunodeficiency virus type 1 |
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| Description: | The HIV-1 protease (Genbank HIVHXB2CG) clone was constructed with the substitutions Q7K, L33I, and L63I, to minimize the autoproteolysis of the protease, and C67A and C95A, to prevent cysteine-thiol oxidation. |
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| Residue: | 99 |
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| Sequence: | PQITLWKRPLVTIKIGGQLKEALLDTGADDTVIEEMSLPGRWKPKMIGGIGGFIKVRQYD
QIIIEIAGHKAIGTVLVGPTPVNIIGRNLLTQIGATLNF
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|
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| Component 2 |
| Name: | Gag-Pol polyprotein [501-599,Q508K,L534I,L564I,C568A,C596A] |
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| Synonyms: | HIV-1 Protease chain A | POL_HV1BR | gag-pol |
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| Type: | Enzyme Subunit |
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| Mol. Mass.: | 10732.11 |
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| Organism: | Human immunodeficiency virus type 1 |
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| Description: | The HIV-1 protease (Genbank HIVHXB2CG) clone was constructed with the substitutions Q7K, L33I, and L63I, to minimize the autoproteolysis of the protease, and C67A and C95A, to prevent cysteine-thiol oxidation. |
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| Residue: | 99 |
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| Sequence: | PQITLWKRPLVTIKIGGQLKEALLDTGADDTVIEEMSLPGRWKPKMIGGIGGFIKVRQYD
QIIIEIAGHKAIGTVLVGPTPVNIIGRNLLTQIGATLNF
|
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| BDBM8125 |
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| HIV Peptide Substrate |
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| Name: | HIV Peptide Substrate |
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| Synonyms: | n/a |
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| Type: | Peptide |
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| Mol. Mass.: | 3156.95 |
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| Organism: | n/a |
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| Description: | n/a |
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| Residue: | 27 |
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| Sequence: | Ac-RE(Edans)SQNY*PIVRK(Dabcyl)R-CO-NH2
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