Literature summary for 3.4.23.16 extracted from

Coman, R.M.; Robbins, A.H.; Fernandez, M.A.; Gilliland, C.T.; Sochet, A.A.; Goodenow, M.M.; McKenna, R.; Dunn, B.M.
The contribution of naturally occurring polymorphisms in altering the biochemical and structural characteristics of HIV-1 subtype C protease (2008), Biochemistry, 47, 731-743.

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Crystallization (Commentary)

Crystallization (Comment)	Organism
crystallization of a protein-inhibitor complex	Human immunodeficiency virus 1

Protein Variants

Protein Variants	Comment	Organism
D30N	mutant of HIV-1 protease subtype B, kcat/Km is 4.2fold lower than wild-type value	Human immunodeficiency virus 1
D30N	mutant of HIV-1 protease subtype C, kcat/Km is 1.8fold lower than wild-type value	Human immunodeficiency virus 1
D30N/L90M	mutant of HIV-1 protease subtype B, kcat/Km is 9.2fold lower than wild-type value	Human immunodeficiency virus 1
D30N/L90M	mutant of HIV-1 protease subtype C, kcat/Km is 1.9fold lower than wild-type value	Human immunodeficiency virus 1
D30N/N88D	mutant of HIV-1 protease subtype B, kcat/Km is 1.4fold lower than wild-type value	Human immunodeficiency virus 1
D30N/N88D	mutant of HIV-1 protease subtype C, kcat/Km is 1.9fold lower than wild-type value	Human immunodeficiency virus 1
L90M	mutant of HIV-1 protease subtype B, kcat/Km is nearly identical to wild-type value	Human immunodeficiency virus 1
L90M	mutant of HIV-1 protease subtype C, kcat/Km is 1.6fold lower than wild-type value	Human immunodeficiency virus 1
N88D	mutant of HIV-1 protease subtype B, kcat/Km is 1.4fold higher than wild-type value	Human immunodeficiency virus 1
N88D	mutant of HIV-1 protease subtype C, kcat/Km is 1.7fold lower than wild-type value	Human immunodeficiency virus 1
N88D/L90M	mutant of HIV-1 protease subtype B, kcat/Km is 1.6fold lower than wild-type value	Human immunodeficiency virus 1
N88D/L90M	mutant of HIV-1 protease subtype C, kcat/Km is 1.1fold higher than wild-type value	Human immunodeficiency virus 1

Inhibitors

Inhibitors	Comment	Organism	Structure
amprenavir	-	Human immunodeficiency virus 1
atazanavir	-	Human immunodeficiency virus 1
indinavir	structural analyses of the subtype C protease bound to nelfinavir and indinavir showed that these inhibitors form similar interactions with the residues in the active site of subtype B and C proteases	Human immunodeficiency virus 1
lopinavir	-	Human immunodeficiency virus 1
additional information	inhibition analysis with eight clinically used protease inhibitors reveales that the natural polymorphisms found in subtype C protease, in combination with drug resistance mutations, can influence enzymatic catalytic efficiency and inhibitor resistance	Human immunodeficiency virus 1
nelfinavir	structural analyses of the subtype C protease bound to nelfinavir and indinavir showed that these inhibitors form similar interactions with the residues in the active site of subtype B and C proteases	Human immunodeficiency virus 1
ritonavir	-	Human immunodeficiency virus 1
saquinavir	-	Human immunodeficiency virus 1
tipranavir	-	Human immunodeficiency virus 1

KM Value [mM]

KM Value [mM]	KM Value Maximum [mM]	Substrate	Comment	Organism	Structure
0.01	-	Lys-Ala-Arg-Val-Nle-Phe(4-NO2)-Glu-Ala-Nle-Gly	37°C, pH 4.7, HIV-1 subtype B protease mutant L90M	Human immunodeficiency virus 1
0.016	-	Lys-Ala-Arg-Val-Nle-Phe(4-NO2)-Glu-Ala-Nle-Gly	37°C, pH 4.7, HIV-1 subtype B protease mutant N88D	Human immunodeficiency virus 1
0.017	-	Lys-Ala-Arg-Val-Nle-Phe(4-NO2)-Glu-Ala-Nle-Gly	37°C, pH 4.7, HIV-1 subtype C protease	Human immunodeficiency virus 1
0.019	-	Lys-Ala-Arg-Val-Nle-Phe(4-NO2)-Glu-Ala-Nle-Gly	37°C, pH 4.7, HIV-1 subtype B protease D30N/N88D	Human immunodeficiency virus 1
0.0195	-	Lys-Ala-Arg-Val-Nle-Phe(4-NO2)-Glu-Ala-Nle-Gly	37°C, pH 4.7, HIV-1 subtype B protease	Human immunodeficiency virus 1
0.022	-	Lys-Ala-Arg-Val-Nle-Phe(4-NO2)-Glu-Ala-Nle-Gly	37°C, pH 4.7, HIV-1 subtype B protease mutant N88D	Human immunodeficiency virus 1
0.023	-	Lys-Ala-Arg-Val-Nle-Phe(4-NO2)-Glu-Ala-Nle-Gly	37°C, pH 4.7, HIV-1 subtype B protease D30N/L90M	Human immunodeficiency virus 1
0.023	-	Lys-Ala-Arg-Val-Nle-Phe(4-NO2)-Glu-Ala-Nle-Gly	37°C, pH 4.7, HIV-1 subtype B protease mutant L90M	Human immunodeficiency virus 1
0.024	-	Lys-Ala-Arg-Val-Nle-Phe(4-NO2)-Glu-Ala-Nle-Gly	37°C, pH 4.7, HIV-1 subtype B protease N88D/L90M	Human immunodeficiency virus 1
0.03	-	Lys-Ala-Arg-Val-Nle-Phe(4-NO2)-Glu-Ala-Nle-Gly	37°C, pH 4.7, HIV-1 subtype B protease N88D/L90M	Human immunodeficiency virus 1
0.035	-	Lys-Ala-Arg-Val-Nle-Phe(4-NO2)-Glu-Ala-Nle-Gly	37°C, pH 4.7, HIV-1 subtype B protease mutant 0.061 D30N/N88D	Human immunodeficiency virus 1
0.0386	-	Lys-Ala-Arg-Val-Nle-Phe(4-NO2)-Glu-Ala-Nle-Gly	37°C, pH 4.7, HIV-1 subtype B protease mutant D30N	Human immunodeficiency virus 1
0.061	-	Lys-Ala-Arg-Val-Nle-Phe(4-NO2)-Glu-Ala-Nle-Gly	37°C, pH 4.7, HIV-1 subtype B protease mutant 0.03 D30M/L90M	Human immunodeficiency virus 1
0.064	-	Lys-Ala-Arg-Val-Nle-Phe(4-NO2)-Glu-Ala-Nle-Gly	37°C, pH 4.7, HIV-1 subtype C protease mutant D30N	Human immunodeficiency virus 1

Organism

Organism	UniProt	Comment	Textmining
Human immunodeficiency virus 1	-	-	-

Substrates and Products (Substrate)

Substrates	Comment Substrates	Organism	Products	Comment (Products)	Rev.	Reac.
Lys-Ala-Arg-Val-Nle-Phe(4-NO2)-Glu-Ala-Nle-Gly + H2O	-	Human immunodeficiency virus 1	Lys-Ala-Arg-Val-Nle + Phe(4-NO2)-Glu-Ala-Nle-Gly	-	?

Turnover Number [1/s]

Turnover Number Minimum [1/s]	Turnover Number Maximum [1/s]	Substrate	Comment	Organism	Structure
3.2	-	Lys-Ala-Arg-Val-Nle-Phe(4-NO2)-Glu-Ala-Nle-Gly	37°C, pH 4.7, HIV-1 subtype B protease D30N/N88D	Human immunodeficiency virus 1
3.5	-	Lys-Ala-Arg-Val-Nle-Phe(4-NO2)-Glu-Ala-Nle-Gly	37°C, pH 4.7, HIV-1 subtype B protease mutant D30M/L90M	Human immunodeficiency virus 1
4	-	Lys-Ala-Arg-Val-Nle-Phe(4-NO2)-Glu-Ala-Nle-Gly	37°C, pH 4.7, HIV-1 subtype B protease D30N/L90M	Human immunodeficiency virus 1
4.3	-	Lys-Ala-Arg-Val-Nle-Phe(4-NO2)-Glu-Ala-Nle-Gly	37°C, pH 4.7, HIV-1 subtype B protease mutant N88D	Human immunodeficiency virus 1
4.8	-	Lys-Ala-Arg-Val-Nle-Phe(4-NO2)-Glu-Ala-Nle-Gly	37°C, pH 4.7, HIV-1 subtype B protease mutant L90M	Human immunodeficiency virus 1
5	-	Lys-Ala-Arg-Val-Nle-Phe(4-NO2)-Glu-Ala-Nle-Gly	37°C, pH 4.7, HIV-1 subtype B protease mutant D30N	Human immunodeficiency virus 1
5.6	-	Lys-Ala-Arg-Val-Nle-Phe(4-NO2)-Glu-Ala-Nle-Gly	37°C, pH 4.7, HIV-1 subtype C protease	Human immunodeficiency virus 1
5.8	-	Lys-Ala-Arg-Val-Nle-Phe(4-NO2)-Glu-Ala-Nle-Gly	37°C, pH 4.7, HIV-1 subtype B protease mutant L90M	Human immunodeficiency virus 1
10	-	Lys-Ala-Arg-Val-Nle-Phe(4-NO2)-Glu-Ala-Nle-Gly	37°C, pH 4.7, HIV-1 subtype B protease	Human immunodeficiency virus 1
10.2	-	Lys-Ala-Arg-Val-Nle-Phe(4-NO2)-Glu-Ala-Nle-Gly	37°C, pH 4.7, HIV-1 subtype B protease N88D/L90M	Human immunodeficiency virus 1
12	-	Lys-Ala-Arg-Val-Nle-Phe(4-NO2)-Glu-Ala-Nle-Gly	37°C, pH 4.7, HIV-1 subtype B protease mutant N88D	Human immunodeficiency virus 1
12	-	Lys-Ala-Arg-Val-Nle-Phe(4-NO2)-Glu-Ala-Nle-Gly	37°C, pH 4.7, HIV-1 subtype C protease mutant D30N	Human immunodeficiency virus 1
12.4	-	Lys-Ala-Arg-Val-Nle-Phe(4-NO2)-Glu-Ala-Nle-Gly	37°C, pH 4.7, HIV-1 subtype B protease mutant D30N/N88D	Human immunodeficiency virus 1
13	-	Lys-Ala-Arg-Val-Nle-Phe(4-NO2)-Glu-Ala-Nle-Gly	37°C, pH 4.7, HIV-1 subtype B protease N88D/L90M	Human immunodeficiency virus 1

Ki Value [mM]

Ki Value [mM]	Ki Value maximum [mM]	Inhibitor	Comment	Organism	Structure
additional information	-	additional information	influence of mutations (D30N, N88D, L90M, D30N/L90M, D30N/N88D, N88D/L90M) on Ki-values for ritonavir, indinavir, nelfinavir, saquinavir, amprenavir, lopinavir, atazanavir, tipranavir	Human immunodeficiency virus 1
0.00000007	-	ritonavir	HIV-1 subtype B protease	Human immunodeficiency virus 1
0.00000007	-	atazanavir	HIV-1 subtype B protease	Human immunodeficiency virus 1
0.00000011	-	lopinavir	HIV-1 subtype B protease	Human immunodeficiency virus 1
0.00000011	-	tipranavir	HIV-1 subtype C protease	Human immunodeficiency virus 1
0.00000013	-	atazanavir	HIV-1 subtype C protease	Human immunodeficiency virus 1
0.00000019	-	lopinavir	HIV-1 subtype C protease	Human immunodeficiency virus 1
0.00000027	-	ritonavir	HIV-1 subtype C protease	Human immunodeficiency virus 1
0.00000029	-	amprenavir	HIV-1 subtype C protease	Human immunodeficiency virus 1
0.0000004	-	amprenavir	HIV-1 subtype B protease	Human immunodeficiency virus 1
0.0000004	-	tipranavir	HIV-1 subtype B protease	Human immunodeficiency virus 1
0.0000017	-	nelfinavir	HIV-1 subtype B protease	Human immunodeficiency virus 1
0.0000018	-	indinavir	HIV-1 subtype B protease	Human immunodeficiency virus 1
0.0000022	-	saquinavir	HIV-1 subtype B protease	Human immunodeficiency virus 1
0.0000026	-	saquinavir	HIV-1 subtype C protease	Human immunodeficiency virus 1
0.0000027	-	nelfinavir	HIV-1 subtype C protease	Human immunodeficiency virus 1
0.0000033	-	indinavir	HIV-1 subtype C protease	Human immunodeficiency virus 1

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Release 2023.1 (January 2023)