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TargetDimer of Gag-Pol polyprotein [501-599,Q508K,L534I,L564I,C568A,C596A]
LigandBDBM35969
Substrate/CompetitorHIV Protease Substrate
Meas. Tech.Enzyme Inhibition Assay (Ki) and Antiviral Activity Assay (EC50/IC50)
pH6.4±n/a
Temperature298.15±n/a K
Ki 0.47±0.002 nM
EC50 22±n/a nM
Citation Ghosh, AKKulkarni, SAnderson, DDHong, LBaldridge, AWang, YFChumanevich, AAKovalevsky, AYTojo, YAmano, MKoh, YTang, JWeber, ITMitsuya, H Design, synthesis, protein-ligand X-ray structure, and biological evaluation of a series of novel macrocyclic human immunodeficiency virus-1 protease inhibitors to combat drug resistance. J Med Chem52:7689-705 (2009) [PubMed]  Article
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Dimer of Gag-Pol polyprotein [501-599,Q508K,L534I,L564I,C568A,C596A]
Name:Dimer of Gag-Pol polyprotein [501-599,Q508K,L534I,L564I,C568A,C596A]
Synonyms:HIV-1 Protease
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]
Synonyms:HIV-1 Protease chain A | POL_HV1BR | gag-pol
Type:Enzyme Subunit
Mol. Mass.:10732.11
Organism:Human immunodeficiency virus type 1
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.
Residue:99
Sequence:
PQITLWKRPLVTIKIGGQLKEALLDTGADDTVIEEMSLPGRWKPKMIGGIGGFIKVRQYD
QIIIEIAGHKAIGTVLVGPTPVNIIGRNLLTQIGATLNF
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Component 2
Name:Gag-Pol polyprotein [501-599,Q508K,L534I,L564I,C568A,C596A]
Synonyms:HIV-1 Protease chain A | POL_HV1BR | gag-pol
Type:Enzyme Subunit
Mol. Mass.:10732.11
Organism:Human immunodeficiency virus type 1
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.
Residue:99
Sequence:
PQITLWKRPLVTIKIGGQLKEALLDTGADDTVIEEMSLPGRWKPKMIGGIGGFIKVRQYD
QIIIEIAGHKAIGTVLVGPTPVNIIGRNLLTQIGATLNF
Blast this sequence in BindingDB or PDB
  Blast E-value cutoff:
BDBM35969
HIV Protease Substrate
Name:HIV Protease Substrate
Synonyms:n/a
Type:Fluorogenic peptide
Mol. Mass.:3467.28
Organism:n/a
Description:n/a
Residue:30
Sequence:
2-(aminobenzoyl)-Thr-Ile-Nle-Phe(p-NO2)-Gln-ArgNH2