Literature summary for 3.4.23.16 extracted from

Mosebi, S.; Morris, L.; Dirr, H.W.; Sayed, Y.
Active-site mutations in the South african human immunodeficiency virus type 1 subtype C protease have a significant impact on clinical inhibitor binding: kinetic and thermodynamic study (2008), J. Virol., 82, 11476-11479.

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Protein Variants

Protein Variants	Comment	Organism
V82A	mutation isolated in South African subtype C protease, no significant impact on proteolytic abilities. Decrease in binding abilities for inhibitors saquinavir, ritonavir, indinavir, and nelfinavir	Human immunodeficiency virus 1
V82F/I84V	mutation isolated in South African subtype C protease, no significant impact on proteolytic abilities. Decrease in binding abilities for inhibitors saquinavir, ritonavir, indinavir, and nelfinavir to levels significantly lower than that required for effective inhibition	Human immunodeficiency virus 1

Inhibitors

Inhibitors	Comment	Organism	Structure
indinavir	-	Human immunodeficiency virus 1
nelfinavir	-	Human immunodeficiency virus 1
ritonavir	-	Human immunodeficiency virus 1
saquinavir	-	Human immunodeficiency virus 1

Organism

Organism	UniProt	Comment	Textmining
Human immunodeficiency virus 1	-	South African subtype C	-

Ki Value [mM]

Ki Value [mM]	Ki Value maximum [mM]	Inhibitor	Comment	Organism	Structure
0.00000049	-	indinavir	wild-type	Human immunodeficiency virus 1
0.0000005	-	ritonavir	wild-type	Human immunodeficiency virus 1
0.00000052	-	nelfinavir	wild-type	Human immunodeficiency virus 1
0.00000062	-	saquinavir	wild-type	Human immunodeficiency virus 1
0.0000009	-	nelfinavir	mutant V82A	Human immunodeficiency virus 1
0.00000097	-	saquinavir	mutant V82A	Human immunodeficiency virus 1
0.00000108	-	ritonavir	mutant V82A	Human immunodeficiency virus 1
0.0000012	-	indinavir	mutant V82A	Human immunodeficiency virus 1
0.000029	-	saquinavir	mutant V82F/I84V	Human immunodeficiency virus 1
0.000056	-	nelfinavir	mutant V82F/I84V	Human immunodeficiency virus 1
0.000097	-	ritonavir	mutant V82F/I84V	Human immunodeficiency virus 1
0.000219	-	indinavir	mutant V82F/I84V	Human immunodeficiency virus 1

IC50 Value

IC50 Value	IC50 Value Maximum	Comment	Organism	Inhibitor	Structure
0.00000012	-	wild-type	Human immunodeficiency virus 1	saquinavir
0.00000028	-	mutant V82A	Human immunodeficiency virus 1	saquinavir
0.00000125	-	wild-type	Human immunodeficiency virus 1	ritonavir
0.00000234	-	wild-type	Human immunodeficiency virus 1	nelfinavir
0.00000287	-	mutant V82A	Human immunodeficiency virus 1	nelfinavir
0.00000302	-	wild-type	Human immunodeficiency virus 1	indinavir
0.00000626	-	mutant V82A	Human immunodeficiency virus 1	ritonavir
0.000012	-	mutant V82F/I84V	Human immunodeficiency virus 1	saquinavir
0.000026	-	mutant V82A	Human immunodeficiency virus 1	indinavir
0.00024	-	mutant V82F/I84V	Human immunodeficiency virus 1	nelfinavir
0.00025	-	mutant V82F/I84V	Human immunodeficiency virus 1	ritonavir
0.0015	-	mutant V82F/I84V	Human immunodeficiency virus 1	indinavir

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Release 2023.1 (January 2023)