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Literature summary for 3.4.23.16 extracted from

  • Chang, M.W.; Giffin, M.J.; Muller, R.; Savage, J.; Lin, Y.C.; Hong, S.; Jin, W.; Whitby, L.R.; Elder, J.H.; Boger, D.L.; Torbett, B.E.
    Identification of broad-based HIV-1 protease inhibitors from combinatorial libraries (2010), Biochem. J., 429, 527-532.
    View publication on PubMedView publication on EuropePMC
Search for more literature for 3.4.23.16

Cloned(Commentary)

Cloned (Comment) Organism
-
 Human immunodeficiency virus 1

Protein Variants

Protein Variants Comment Organism
L24I/M46I/F53L/L63P/V77I/V82A associated with resistance to saquinavir, nelfinavir, ritonavir and TL3 Human immunodeficiency virus 1

Inhibitors

Inhibitors Comment Organism Structure
4-[[(6-[[(4-aminothiophen-2-yl)carbonyl]amino]-1,3-benzoxazol-2-yl)carbonyl]amino]thiophene-2-carboxylic acid non-competitive Human immunodeficiency virus 1
methyl 4-[([6-[([4-[(tert-butoxycarbonyl)amino]thiophen-2-yl]carbonyl)amino]-1,3-benzoxazol-2-yl]carbonyl)amino]thiophene-2-carboxylate non-competitive Human immunodeficiency virus 1

KM Value [mM]

KM Value [mM] KM Value Maximum [mM] Substrate Comment Organism Structure
0.03
-
 2-aminobenzoyl-Thr-Ile-Nle-4-nitro-Phe-Gln-Arg
-
 Human immunodeficiency virus 1

Organism

Organism UniProt Comment Textmining
Human immunodeficiency virus 1
-
-
-

Purification (Commentary)

Purification (Comment) Organism
-
 Human immunodeficiency virus 1

Substrates and Products (Substrate)

Substrates Comment Substrates Organism Products Comment (Products) Rev. Reac.
2-aminobenzoyl-Thr-Ile-Nle-4-nitro-Phe-Gln-Arg-NH2 + H2O
-
 Human immunodeficiency virus 1 2-aminobenzoyl-Thr-Ile-Nle + 4-nitro-Phe-Gln-Arg-NH2
-
 ?
2-aminobenzoyl-Thr-Ile-Nle-p-nitro-Phe-Gln-Arg-NH2 + H2O
-
 Human immunodeficiency virus 1 2-aminobenzoyl-Thr-Ile-Nle + p-nitro-Phe-Gln-Arg-NH2
-
 ?

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
0.0016
-
 4-[[(6-[[(4-aminothiophen-2-yl)carbonyl]amino]-1,3-benzoxazol-2-yl)carbonyl]amino]thiophene-2-carboxylic acid wild-type protein Human immunodeficiency virus 1
0.0061
-
 methyl 4-[([6-[([4-[(tert-butoxycarbonyl)amino]thiophen-2-yl]carbonyl)amino]-1,3-benzoxazol-2-yl]carbonyl)amino]thiophene-2-carboxylate wild-type protein Human immunodeficiency virus 1

IC50 Value

IC50 Value IC50 Value Maximum Comment Organism Inhibitor Structure
0.0106
-
 L24I/M46I/F53L/L63P/V77I/V82A mutant protein Human immunodeficiency virus 1 methyl 4-[([6-[([4-[(tert-butoxycarbonyl)amino]thiophen-2-yl]carbonyl)amino]-1,3-benzoxazol-2-yl]carbonyl)amino]thiophene-2-carboxylate
0.0172
-
 wild-type protein Human immunodeficiency virus 1 methyl 4-[([6-[([4-[(tert-butoxycarbonyl)amino]thiophen-2-yl]carbonyl)amino]-1,3-benzoxazol-2-yl]carbonyl)amino]thiophene-2-carboxylate