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Literature summary extracted from

  • Lin, X.; Kurz, J.L.; Patel, K.M.; Wun, S.J.; Hussein, W.M.; Lonhienne, T.; West, N.P.; McGeary, R.P.; Schenk, G.; Guddat, L.W.
    Discovery of a pyrimidinedione derivative with potent inhibitory activity against Mycobacterium tuberculosis ketol-acid reductoisomerase (2021), Chemistry, 27, 3130-3141 .
    View publication on PubMed

Cloned(Commentary)

EC Number Cloned (Comment) Organism
1.1.1.86
-
Mycobacterium tuberculosis

Crystallization (Commentary)

EC Number Crystallization (Comment) Organism
1.1.1.86 hanging drop method Mycobacterium tuberculosis

Inhibitors

EC Number Inhibitors Comment Organism Structure
1.1.1.86 6-hydroxy-2-methylthiazolo[4,5-d]pyrimidine-5,7(4H,6H)-dione NSC116565, potent time-dependent inhibitor. The inhibitor binds to Mycobacterium tuberculosis KARI in the presence and absence of the cofactor, NADPH. Inhibits the growth of Mycobacterium tuberculosis H37Ra strain with MIC50 value of 0.00293 mM; NSC116565, potent time-dependent inhibitor. The inhibitor binds to Mycobacterium tuberculosis KARI in the presence and absence of the cofactor, NADPH. Inhibits the growth of Mycobacterium tuberculosis H37Rv strain with MIC50 value of 0.00606 mM Mycobacterium tuberculosis

Organism

EC Number Organism UniProt Comment Textmining
1.1.1.86 Mycobacterium tuberculosis A5U713
-
-
1.1.1.86 Mycobacterium tuberculosis P9WKJ7
-
-
1.1.1.86 Mycobacterium tuberculosis H37Rv P9WKJ7
-
-

Purification (Commentary)

EC Number Purification (Comment) Organism
1.1.1.86
-
Mycobacterium tuberculosis

Substrates and Products (Substrate)

EC Number Substrates Comment Substrates Organism Products Comment (Products) Rev. Reac.
1.1.1.86 (2S)-2-acetolactate + NADPH + H+
-
Mycobacterium tuberculosis (2R)-2,3-dihydroxyisovalerate + NADP+
-
?

Synonyms

EC Number Synonyms Comment Organism
1.1.1.86 KARI
-
Mycobacterium tuberculosis

Cofactor

EC Number Cofactor Comment Organism Structure
1.1.1.86 NADPH
-
Mycobacterium tuberculosis

General Information

EC Number General Information Comment Organism
1.1.1.86 drug target the enzyme is a TB drug target Mycobacterium tuberculosis
1.1.1.86 drug target the enzyme is a TB drug target and 6-hydroxy-2-methylthiazolo[4,5-d]pyrimidine-5,7(4H,6H)-dione (NSC116565) is a promising lead for anti-TB drug development Mycobacterium tuberculosis
1.1.1.86 metabolism second enzyme in the branched chain amino acid biosynthesis pathway Mycobacterium tuberculosis