Literature summary for 3.4.23.B4 extracted from

Lin, Y.C.; Brik, A.; de Parseval, A.; Tam, K.; Torbett, B.E.; Wong, C.H.; Elder, J.H.
Altered Gag polyprotein cleavage specificity of feline immunodeficiency virus/human immunodeficiency virus mutant proteases as demonstrated in a cell-based expression system (2006), J. Virol., 80, 7832-7843.

Search for more literature for 3.4.23.B4

Application

Application	Comment	Organism
molecular biology	the FIV-PR mutant is a mutational model system to study the molecular basis of substrate-inhibitor specificity for lentivirus proteases, especially HIV-1 protease	feline immunodeficiency virus

Cloned(Commentary)

Cloned (Comment)	Organism
expression of wild-type and mutant FIV PRs in human 293T cells	feline immunodeficiency virus

Protein Variants

Protein Variants	Comment	Organism
D30N	site-directed mutagenesis, the mutant shows highly reduced activity compared to the wild-type enzyme	feline immunodeficiency virus
I35D	site-directed mutagenesis, the mutant shows about 30% reduced activity compared to the wild-type enzyme	feline immunodeficiency virus
I57G	site-directed mutagenesis, the mutant shows about 50% reduced activity compared to the wild-type enzyme	feline immunodeficiency virus
additional information	generation of different FIV PR mutants, by single point mutations and exchange of several amino acids comprising fragments, which show altered substrate specificity to Gag-Pol polyprotein precursor and an altered processing order compared to wild-type enzyme assessed in pseudovirions in transduced cells, FIV PR exchange mutants are much more susceptible to HIV-1 protease inhibitors than the wild-type FIV protease, overview	feline immunodeficiency virus
N55D	site-directed mutagenesis, the mutant shows similar activity compared to the wild-type enzyme	feline immunodeficiency virus

Inhibitors

Inhibitors	Comment	Organism	Structure
additional information	FIV PR exchange mutants are much more susceptible to HIV-1 protease inhibitors than the wild-type FIV protease	feline immunodeficiency virus
protease inhibitor AB-2	a HIV-1 protease inhibitor, IC50: 0.0011 mM	feline immunodeficiency virus
protease inhibitor AB-6	a HIV-1 protease inhibitor, IC50: 0.001 mM	feline immunodeficiency virus
protease inhibitor AB-8	a HIV-1 protease inhibitor, IC50: 0.008 mM	feline immunodeficiency virus
protease inhibitor APV-1	a HIV-1 protease inhibitor, IC50: 0.001 mM	feline immunodeficiency virus
protease inhibitor RTV	a HIV-1 protease inhibitor, weak inhibition of wild-type FIV protease, IC50: 0.045 mM	feline immunodeficiency virus
protease inhibitor TL-3	IC50: 90 nM	feline immunodeficiency virus
saquinovir	weak inhibition of wild-type protease	feline immunodeficiency virus

Natural Substrates/ Products (Substrates)

Natural Substrates	Organism	Comment (Nat. Sub.)	Natural Products	Comment (Nat. Pro.)	Rev.	Reac.
Gag-Pol polyprotein + H2O	feline immunodeficiency virus	processing of the precursor protein	?	-	?
Gag-Pol polyprotein + H2O	feline immunodeficiency virus FIV	processing of the precursor protein	?	-	?

Organism

Organism	UniProt	Comment	Textmining
feline immunodeficiency virus	-	FIV	-
feline immunodeficiency virus FIV	-	FIV	-

Substrates and Products (Substrate)

Substrates	Comment Substrates	Organism	Products	Comment (Products)	Rev.	Reac.
Gag-Pol polyprotein + H2O	-	feline immunodeficiency virus	?	-	?
Gag-Pol polyprotein + H2O	processing of the precursor protein	feline immunodeficiency virus	?	-	?
Gag-Pol polyprotein + H2O	-	feline immunodeficiency virus FIV	?	-	?
Gag-Pol polyprotein + H2O	processing of the precursor protein	feline immunodeficiency virus FIV	?	-	?

Synonyms

Synonyms	Comment	Organism
feline immunodeficiency virus protease	-	feline immunodeficiency virus
FIV-PR	-	feline immunodeficiency virus

IC50 Value

IC50 Value	IC50 Value Maximum	Comment	Organism	Inhibitor	Structure
0.00009	-	IC50: 90 nM	feline immunodeficiency virus	protease inhibitor TL-3
0.001	-	a HIV-1 protease inhibitor, IC50: 0.001 mM	feline immunodeficiency virus	protease inhibitor APV-1
0.001	-	a HIV-1 protease inhibitor, IC50: 0.001 mM	feline immunodeficiency virus	protease inhibitor AB-6
0.0011	-	a HIV-1 protease inhibitor, IC50: 0.0011 mM	feline immunodeficiency virus	protease inhibitor AB-2
0.008	-	a HIV-1 protease inhibitor, IC50: 0.008 mM	feline immunodeficiency virus	protease inhibitor AB-8
0.045	-	a HIV-1 protease inhibitor, weak inhibition of wild-type FIV protease, IC50: 0.045 mM	feline immunodeficiency virus	protease inhibitor RTV

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Release 2023.1 (January 2023)