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Literature summary for 3.4.23.16 extracted from

  • Skalova, T.; Dohnalek, J.; Duskova, J.; Petrokova, H.; Hradilek, M.; Soucek, M.; Konvalinka, J.; Hasek, J.
    HIV-1 protease mutations and inhibitor modifications monitored on a series of complexes. Structural basis for the effect of the A71V mutation on the active site (2006), J. Med. Chem., 49, 5777-5784.
    View publication on PubMed

Crystallization (Commentary)

Crystallization (Comment) Organism
wild-type and mutant A71V/V82T/I84V enzymes in complex with inhibitors SE, and SQ, hanging drop vapour diffusion method, 25°C, the reservoir solution contains 0.1 M sodium citrate, pH 4.4, 0.5 M sodium chloride, and 10% v/v glycerol, X-ray diffraction structure determination and analysis at 1.93-2.38 A resolution Human immunodeficiency virus 1

Protein Variants

Protein Variants Comment Organism
A71V/V82T/I84V site-directed mutagenesis, the mutant enzyme shows altered interactions with inhibitors compared to the wild-type enzyme Human immunodeficiency virus 1

Inhibitors

Inhibitors Comment Organism Structure
tert-butoxycarbonyl-Phe-psi[CH2CH2NH]-Phe-Glu-Phe-NH2 i.e. tert-butoxycarbonyl-Phe-psi[CH2CH2NH]-Phe-Glu-Phe-NH2, an ethyleneamine inhibitor, interactions with the enzyme, overview Human immunodeficiency virus 1
tert-butoxycarbonyl-Phe-psi[S-CH(OH)CH2NH]-Phe-Gln-Phe-NH2 i.e. tert-butoxycarbonyl-Phe-psi[S-CH(OH)CH2NH]-Phe-Gln-Phe-NH2, a pseudotetrapeptide inhibitor with an acyclic S-hydroxyethylamine isostere, interactions with the enzyme and binding structure, overview Human immunodeficiency virus 1
tert-butoxycarbonyl-Phe-psi[S-CH(OH)CH2NH]-Phe-Glu-Phe-NH2 i.e. tert-butoxycarbonyl-Phe-psi[S-CH(OH)CH2NH]-Phe-Glu-Phe-NH2, a pseudotetrapeptide inhibitor with an acyclic S-hydroxyethylamine isostere, interactions with the enzyme and binding structure, overview Human immunodeficiency virus 1
tert-butoxycarbonyl-Phe-psi[S-CH(OH)CH2]-Phe-Gln-Phe-NH2 i.e. tert-butoxycarbonyl-Phe-psi[S-CH(OH)CH2]-Phe-Gln-Phe-NH2, a hydroxyethylene inhibitor, interactions with the enzyme, overview Human immunodeficiency virus 1

Organism

Organism UniProt Comment Textmining
Human immunodeficiency virus 1
-
i.e. HIV-1
-

Synonyms

Synonyms Comment Organism
HIV-1 protease
-
Human immunodeficiency virus 1

Ki Value [mM]

Ki Value [mM] Ki Value maximum [mM] Inhibitor Comment Organism Structure
0.00000002
-
tert-butoxycarbonyl-Phe-psi[S-CH(OH)CH2]-Phe-Gln-Phe-NH2 wild-type enzyme Human immunodeficiency virus 1
0.00000015
-
tert-butoxycarbonyl-Phe-psi[S-CH(OH)CH2NH]-Phe-Glu-Phe-NH2 wild-type enzyme Human immunodeficiency virus 1
0.00000026
-
tert-butoxycarbonyl-Phe-psi[S-CH(OH)CH2]-Phe-Gln-Phe-NH2 mutant A71V/V82T/I84V enzyme Human immunodeficiency virus 1
0.0000015
-
tert-butoxycarbonyl-Phe-psi[CH2CH2NH]-Phe-Glu-Phe-NH2 wild-type enzyme Human immunodeficiency virus 1
0.0000041
-
tert-butoxycarbonyl-Phe-psi[CH2CH2NH]-Phe-Glu-Phe-NH2 mutant A71V/V82T/I84V enzyme Human immunodeficiency virus 1
0.000033
-
tert-butoxycarbonyl-Phe-psi[S-CH(OH)CH2NH]-Phe-Gln-Phe-NH2 wild-type enzyme Human immunodeficiency virus 1
0.000086
-
tert-butoxycarbonyl-Phe-psi[S-CH(OH)CH2NH]-Phe-Glu-Phe-NH2 mutant A71V/V82T/I84V enzyme Human immunodeficiency virus 1
0.001
-
tert-butoxycarbonyl-Phe-psi[S-CH(OH)CH2NH]-Phe-Gln-Phe-NH2 mutant A71V/V82T/I84V enzyme Human immunodeficiency virus 1