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Literature summary extracted from

  • Makafe, G.G.; Hussain, M.; Surineni, G.; Tan, Y.; Wong, N.K.; Julius, M.; Liu, L.; Gift, C.; Jiang, H.; Tang, Y.; Liu, J.; Tan, S.; Yu, Z.; Liu, Z.; Lu, Z.; Fang, C.; Zhou, Y.; Zhang, J.; Zhu, Q.; Liu, J.; Zhang, T.
    Quinoline derivatives kill Mycobacterium tuberculosis by activating glutamate kinase (2019), Cell Chem. Biol., 26, 1187-1194 .
    View publication on PubMed

Activating Compound

EC Number Activating Compound Comment Organism Structure
2.7.2.11 4-(11H-indolo[3,2-c]quinolin-6-yl)aniline Z0933M Mycobacterium tuberculosis
2.7.2.11 6-(4-(pyrrolidin-1-yl)phenyl)-11H-pyrido[2',3':4,5]pyrrolo[3,2-c]quinoline Z0930 Mycobacterium tuberculosis
2.7.2.11 tert-butyl(4-(11H-indolo[3,2-c]quinolin-6-yl)phenyl)carbamate Z0933 Mycobacterium tuberculosis

Cloned(Commentary)

EC Number Cloned (Comment) Organism
2.7.2.11 expressed in Escherichia coli BL21 (lambdaDE3) cells Mycobacterium tuberculosis

Protein Variants

EC Number Protein Variants Comment Organism
2.7.2.11 A226S the mutant has 1.2fold increased activity and higher thermostability compared to the wild type enzyme Mycobacterium tuberculosis

Inhibitors

EC Number Inhibitors Comment Organism Structure
2.7.2.11 L-proline feedback inhibitor Mycobacterium tuberculosis

KM Value [mM]

EC Number KM Value [mM] KM Value Maximum [mM] Substrate Comment Organism Structure
2.7.2.11 92.8
-
 L-glutamate at pH 7.2 and 37°C Mycobacterium tuberculosis

Metals/Ions

EC Number Metals/Ions Comment Organism Structure
2.7.2.11 Mg2+ 80 mM used in assay conditions Mycobacterium tuberculosis

Natural Substrates/ Products (Substrates)

EC Number Natural Substrates Organism Comment (Nat. Sub.) Natural Products Comment (Nat. Pro.) Rev. Reac.
2.7.2.11 ATP + L-glutamate Mycobacterium tuberculosis
-
 ADP + L-glutamate 5-phosphate
-
 ?
2.7.2.11 ATP + L-glutamate Mycobacterium tuberculosis H37Rv
-
 ADP + L-glutamate 5-phosphate
-
 ?

Organism

EC Number Organism UniProt Comment Textmining
2.7.2.11 Mycobacterium tuberculosis P9WHU9
-
-
2.7.2.11 Mycobacterium tuberculosis H37Rv P9WHU9
-
-

Purification (Commentary)

EC Number Purification (Comment) Organism
2.7.2.11 HisTrap column chromatography Mycobacterium tuberculosis

Substrates and Products (Substrate)

EC Number Substrates Comment Substrates Organism Products Comment (Products) Rev. Reac.
2.7.2.11 ATP + L-glutamate
-
 Mycobacterium tuberculosis ADP + L-glutamate 5-phosphate
-
 ?
2.7.2.11 ATP + L-glutamate
-
 Mycobacterium tuberculosis H37Rv ADP + L-glutamate 5-phosphate
-
 ?

Temperature Optimum [°C]

EC Number Temperature Optimum [°C] Temperature Optimum Maximum [°C] Comment Organism
2.7.2.11 25
-
-
 Mycobacterium tuberculosis

General Information

EC Number General Information Comment Organism
2.7.2.11 physiological function enzyme activation kills Mycobacterium tuberculosis via induction of proline and reactive oxygen species overproduction Mycobacterium tuberculosis