Literature summary for 3.4.23.16 extracted from

Agniswamy, J.; Kneller, D.W.; Brothers, R.; Wang, Y.F.; Harrison, R.W.; Weber, I.T.
Highly drug-resistant HIV-1 protease mutant PRS17 shows enhanced binding to substrate analogues (2019), ACS Omega, 4, 8707-8719 .

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Cloned(Commentary)

Cloned (Comment)	Organism
expressed in Escherichia coli BL21(DE3) cells	Human immunodeficiency virus 1

Crystallization (Commentary)

Crystallization (Comment)	Organism
PRS17-D25N alone and in complex with substrate analogues RVLrFEANle and Ace-TINlerNleQR , hanging drop vapor diffusion method, using 1.95 M sodium chloride and 0.1 M bis-Tris pH 7.5 (inhibitor-free), 2.1 M sodium chloride and 0.1 M 4-(2-hydroxyethyl)-1-piperazineethanesulfonic acid at pH 7.6 (with RVLrFEANle) or 29.5% (w/v) poly(ethylene glycol) 4000, 0.2 M ammonium acetate, and 0.1 M sodium acetate buffer at pH 4.6 (with Ace-TINlerNleQR)	Human immunodeficiency virus 1

Crystallization (Comment)

Organism

PRS17-D25N alone and in complex with substrate analogues RVLrFEANle and Ace-TINlerNleQR , hanging drop vapor diffusion method, using 1.95 M sodium chloride and 0.1 M bis-Tris pH 7.5 (inhibitor-free), 2.1 M sodium chloride and 0.1 M 4-(2-hydroxyethyl)-1-piperazineethanesulfonic acid at pH 7.6 (with RVLrFEANle) or 29.5% (w/v) poly(ethylene glycol) 4000, 0.2 M ammonium acetate, and 0.1 M sodium acetate buffer at pH 4.6 (with Ace-TINlerNleQR)

Human immunodeficiency virus 1

Protein Variants

Protein Variants	Comment	Organism
PRS17	the highly drug-resistant mutant enzyme shows enhanced binding to substrate analogues RVLrFEANle and Ace-TINlerNleQR	Human immunodeficiency virus 1
PRS17-D25N	inactive	Human immunodeficiency virus 1
PRV82A	the highly drug-resistant mutant enzyme shows enhanced binding to substrate analogues RVLrFEANle and Ace-TINlerNleQR	Human immunodeficiency virus 1

Inhibitors

Inhibitors	Comment	Organism
Ace-TINlerNleQR	-	Human immunodeficiency virus 1
amprenavir	-	Human immunodeficiency virus 1
darunavir	-	Human immunodeficiency virus 1
indinavir	-	Human immunodeficiency virus 1
RVLrFEANle	-	Human immunodeficiency virus 1

Organism

Organism	UniProt	Comment	Textmining
Human immunodeficiency virus 1	Q5RZ08	-	-

Purification (Commentary)

Purification (Comment)	Organism
Source 15RPC column chromatography and Superdex 75 gel filtration	Human immunodeficiency virus 1

Synonyms

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

Ki Value [mM]

Ki Value [mM]	Ki Value maximum [mM]	Inhibitor	Comment	Organism
0.000022	-	Ace-TINlerNleQR	mutant enzyme PRS17, at pH 5.6 and 37°C	Human immunodeficiency virus 1
0.000024	-	Ace-TINlerNleQR	mutant enzyme PRV82A, at pH 5.6 and 37°C	Human immunodeficiency virus 1
0.000075	-	Ace-TINlerNleQR	wild type enzyme, at pH 5.6 and 37°C	Human immunodeficiency virus 1
0.000514	-	RVLrFEANle	mutant enzyme PRS17, at pH 5.6 and 37°C	Human immunodeficiency virus 1
0.00053	-	RVLrFEANle	mutant enzyme PRV82A, at pH 5.6 and 37°C	Human immunodeficiency virus 1
0.00217	-	RVLrFEANle	wild type enzyme, at pH 5.6 and 37°C	Human immunodeficiency virus 1