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Literature summary for 1.1.1.86 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
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Cloned(Commentary)

Cloned (Comment) Organism
-
 Mycobacterium tuberculosis

Crystallization (Commentary)

Crystallization (Comment) Organism
hanging drop method Mycobacterium tuberculosis

Inhibitors

Inhibitors Comment Organism Structure
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

Organism UniProt Comment Textmining
Mycobacterium tuberculosis A5U713
-
-
Mycobacterium tuberculosis P9WKJ7
-
-
Mycobacterium tuberculosis H37Rv P9WKJ7
-
-

Purification (Commentary)

Purification (Comment) Organism
-
 Mycobacterium tuberculosis

Substrates and Products (Substrate)

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

Synonyms

Synonyms Comment Organism
KARI
-
 Mycobacterium tuberculosis

Cofactor

Cofactor Comment Organism Structure
NADPH
-
 Mycobacterium tuberculosis

General Information

General Information Comment Organism
drug target the enzyme is a TB drug target Mycobacterium tuberculosis
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
metabolism second enzyme in the branched chain amino acid biosynthesis pathway Mycobacterium tuberculosis