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Literature summary for 3.4.23.47 extracted from

  • Tong, L.; Pav, S.; Mui, S.; Lamarre, D.; Yoakim, C.; Beaulieu, P.; Anderson, P.C.
    Crystal structures of HIV-2 protease in complex with inhibitors containing the hydroxyethylamine dipeptide isostere (1995), Structure, 3, 33-40.
    View publication on PubMed

Application

Application Comment Organism
medicine potential target for chemotherapy of virus infection and associated diseases, essential for maturation of infectious virions, development of drugs against the protease should be effective against HIV-2 Human immunodeficiency virus 2

Cloned(Commentary)

Cloned (Comment) Organism
-
Human immunodeficiency virus 2

Crystallization (Commentary)

Crystallization (Comment) Organism
crystallized by hanging drop method in complex with a reduced amide inhibitor, BI-LA-398 Human immunodeficiency virus 2
crystals grown by hanging-drop vapor diffusion method, thin tetragonal prisms, space group P4(1)2(1)2 or P4(3)2(1)2 with a=b=62.6 A and c=115.8 A Human immunodeficiency virus 2

Inhibitors

Inhibitors Comment Organism Structure
2,6-dimethylbenzyl (2S,3R)-4-((2S,4R)-2-(tert-butylcarbamoyl)-4-(4,6-dimethylpyrimidin-2-ylthio)piperidin-1-yl)-3-hydroxy-1-phenylbutan-2-ylcarbamate hydroxyethylamine dipeptide isostere inhibitor 3 Human immunodeficiency virus 2
2,6-dimethylbenzyl (2S,3R)-4-((2S,4R)-2-(tert-butylcarbamoyl)-4-(pyridin-3-ylmethoxy)piperidin-1-yl)-3-hydroxy-1-phenylbutan-2-ylcarbamate hydroxyethylamine dipeptide isostere inhibitor 5 Human immunodeficiency virus 2
2,6-dimethylbenzyl (2S,3R)-4-((2S,4R)-2-(tert-butylcarbamoyl)-4-(pyridin-3-ylthio)piperidin-1-yl)-3-hydroxy-1-phenylbutan-2-ylcarbamate hydroxyethylamine dipeptide isostere inhibitor 2 Human immunodeficiency virus 2
2,6-dimethylbenzyl (2S,3R)-4-((2S,4R)-2-(tert-butylcarbamoyl)-4-(pyridin-4-ylsulfonyl)piperidin-1-yl)-3-hydroxy-1-phenylbutan-2-ylcarbamate hydroxyethylamine dipeptide isostere inhibitor 4 Human immunodeficiency virus 2
2,6-dimethylbenzyl (2S,3R)-4-((2S,4R)-2-(tert-butylcarbamoyl)-4-(pyridin-4-ylthio)piperidin-1-yl)-3-hydroxy-1-phenylbutan-2-ylcarbamate hydroxyethylamine dipeptide isostere inhibitor 1 Human immunodeficiency virus 2
N-((S)-1-((2S,3R)-4-((2S,4R)-2-(tert-butylcarbamoyl)-4-(pyridin-3-ylmethoxy)piperidin-1-yl)-3-hydroxy-1-phenylbutan-2-ylamino)-3-methyl-1-oxobutan-2-yl)quinoline-2-carboxamide hydroxyethylamine dipeptide isostere inhibitor 8 Human immunodeficiency virus 2
N-((S)-1-((2S,3R)-4-((2S,4R)-2-(tert-butylcarbamoyl)-4-(pyridin-3-ylmethylthio)piperidin-1-yl)-3-hydroxy-1-phenylbutan-2-ylamino)-3-methyl-1-oxobutan-2-yl)quinoline-2-carboxamide hydroxyethylamine dipeptide isostere inhibitor 6 Human immunodeficiency virus 2
N-((S)-1-((2S,3R)-4-((2S,4R)-2-(tert-butylcarbamoyl)-4-(pyridin-3-ylthio)piperidin-1-yl)-3-hydroxy-1-phenylbutan-2-ylamino)-3-methyl-1-oxobutan-2-yl)quinoline-2-carboxamide hydroxyethylamine dipeptide isostere inhibitor 7 Human immunodeficiency virus 2

Natural Substrates/ Products (Substrates)

Natural Substrates Organism Comment (Nat. Sub.) Natural Products Comment (Nat. Pro.) Rev. Reac.
GAG precursor protein of HIV-2 + H2O Human immunodeficiency virus 2
-
?
-
?

Organism

Organism UniProt Comment Textmining
Human immunodeficiency virus 2
-
human immunodeficiency virus type 2
-

Purification (Commentary)

Purification (Comment) Organism
-
Human immunodeficiency virus 2

Substrates and Products (Substrate)

Substrates Comment Substrates Organism Products Comment (Products) Rev. Reac.
GAG precursor protein of HIV-2 + H2O
-
Human immunodeficiency virus 2 ?
-
?
additional information catalyzes hydrolysis of Phe-Pro, Tyr-Pro and other peptide bonds in the gag and gag-pol polyproteins Human immunodeficiency virus 2 ?
-
?

Subunits

Subunits Comment Organism
dimer 2 identical subunits, homodimer Human immunodeficiency virus 2