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Literature summary extracted from

  • Reshma, R.; Jeankumar, V.; Kapoor, N.; Saxena, S.; Bobesh, K.; Vachaspathy, A.; Kolattukudy, P.; Sriram, D.
    Mycobacterium tuberculosis lysine-epsilon-aminotransferase a potential target in dormancy Benzothiazole based inhibitors (2017), Bioorg. Med. Chem., 25, 2761-2771.
    View publication on PubMed

Inhibitors

EC Number Inhibitors Comment Organism Structure
2.6.1.36 (E)-2-(2-(2-(benzo[d]thiazol-2-yl)-2-cyanovinyl)phenoxy)acetic acid
-
 Mycobacterium tuberculosis
2.6.1.36 (E)-2-(4-(2-(benzo[d]thiazol-2-yl)-2-cyanovinyl)phenoxy)acetic acid
-
 Mycobacterium tuberculosis
2.6.1.36 (E)-2-(benzo[d]thiazol-2-yl)-3-(1H-indol-3-yl)acrylonitrile
-
 Mycobacterium tuberculosis
2.6.1.36 (E)-2-(benzo[d]thiazol-2-yl)-3-(1H-pyrrol -2-yl)acrylonitrile
-
 Mycobacterium tuberculosis
2.6.1.36 (E)-2-(benzo[d]thiazol-2-yl)-3-(2,4-dihydroxyphenyl)acrylonitrile
-
 Mycobacterium tuberculosis
2.6.1.36 (E)-2-(benzo[d]thiazol-2-yl)-3-(3,4,5-trimethoxyphenyl)acrylonitrile
-
 Mycobacterium tuberculosis
2.6.1.36 (E)-2-(benzo[d]thiazol-2-yl)-3-(3,4-dimethoxyphenyl)acrylonitrile
-
 Mycobacterium tuberculosis
2.6.1.36 (E)-2-(benzo[d]thiazol-2-yl)-3-(4-benzyloxyphenyl)acrylonitrile
-
 Mycobacterium tuberculosis
2.6.1.36 (E)-2-(benzo[d]thiazol-2-yl)-3-(4-fluorophenyl)acrylonitrile
-
 Mycobacterium tuberculosis
2.6.1.36 (E)-2-(benzo[d]thiazol-2-yl)-3-(4-hydroxy-3-methoxyphenyl)acrylonitrile
-
 Mycobacterium tuberculosis
2.6.1.36 (E)-2-(benzo[d]thiazol-2-yl)-3-(4-hydroxyphenyl)acrylonitrile
-
 Mycobacterium tuberculosis
2.6.1.36 (E)-2-(benzo[d]thiazol-2-yl)-3-(5-nitrofuran-2-yl)acrylonitrile
-
 Mycobacterium tuberculosis
2.6.1.36 (E)-2-(benzo[d]thiazol-2-yl)-3-(5-nitrothiophen-2-yl)acrylonitrile
-
 Mycobacterium tuberculosis
2.6.1.36 (E)-2-(benzo[d]thiazol-2-yl)-3-(furan-2-yl)acrylonitrile
-
 Mycobacterium tuberculosis
2.6.1.36 (E)-2-(benzo[d]thiazol-2-yl)-3-(thiophen-2-yl)acrylonitrile
-
 Mycobacterium tuberculosis
2.6.1.36 (E)-3-(5-(2-(benzo[d]thiazol-2-yl)-2-cyanovinyl)furan-2-yl)benzoic acid
-
 Mycobacterium tuberculosis
2.6.1.36 (E)-3-(5-(2-(benzo[d]thiazol-2-yl)-2-cyanovinyl)thiophen-2-yl)benzoic acid
-
 Mycobacterium tuberculosis
2.6.1.36 (E)-3-(benzo[d][1,3]dioxol-5-yl)-2-(benzo[d]thiazol-2-yl)acrylonitrile
-
 Mycobacterium tuberculosis
2.6.1.36 (E)-4-(5-(2-(benzo[d]thiazol-2-yl)-2-cyanovinyl)furan-2-yl)benzoic acid
-
 Mycobacterium tuberculosis
2.6.1.36 (E)-4-(5-(2-(benzo[d]thiazol-2-yl)-2-cyanovinyl)thiophen-2-yl)benzoic acid
-
 Mycobacterium tuberculosis
2.6.1.36 (E)-4-(5-(2-(benzo[d]thiazol-2-yl)-2-cyanovinyl)thiophen-2-yl)isophthalic acid
-
 Mycobacterium tuberculosis
2.6.1.36 (E)-5-(5-(2-(benzo[d]thiazol-2-yl)-2-cyanovinyl)furan-2-yl)isophthalic acid
-
 Mycobacterium tuberculosis
2.6.1.36 additional information identification of inhibitors by high throughput virtual database screening for active derivatives using a benzothiazole lead as template, structure-activity relationship analysis of potentials inhibitors, docking study, overview Mycobacterium tuberculosis

Natural Substrates/ Products (Substrates)

EC Number Natural Substrates Organism Comment (Nat. Sub.) Natural Products Comment (Nat. Pro.) Rev. Reac.
2.6.1.36 L-lysine + 2-oxoglutarate Mycobacterium tuberculosis
-
 (S)-2-amino-6-oxohexanoate + L-glutamate
-
 ?
2.6.1.36 L-lysine + 2-oxoglutarate Mycobacterium tuberculosis H37Rv
-
 (S)-2-amino-6-oxohexanoate + L-glutamate
-
 ?
2.6.1.36 L-lysine + 2-oxoglutarate Mycobacterium tuberculosis ATCC 25618
-
 (S)-2-amino-6-oxohexanoate + L-glutamate
-
 ?

Organism

EC Number Organism UniProt Comment Textmining
2.6.1.36 Mycobacterium tuberculosis P9WQ77
-
-
2.6.1.36 Mycobacterium tuberculosis ATCC 25618 P9WQ77
-
-
2.6.1.36 Mycobacterium tuberculosis H37Rv P9WQ77
-
-

Substrates and Products (Substrate)

EC Number Substrates Comment Substrates Organism Products Comment (Products) Rev. Reac.
2.6.1.36 L-lysine + 2-oxoglutarate
-
 Mycobacterium tuberculosis (S)-2-amino-6-oxohexanoate + L-glutamate
-
 ?
2.6.1.36 L-lysine + 2-oxoglutarate
-
 Mycobacterium tuberculosis H37Rv (S)-2-amino-6-oxohexanoate + L-glutamate
-
 ?
2.6.1.36 L-lysine + 2-oxoglutarate
-
 Mycobacterium tuberculosis ATCC 25618 (S)-2-amino-6-oxohexanoate + L-glutamate
-
 ?

Synonyms

EC Number Synonyms Comment Organism
2.6.1.36 LAT
-
 Mycobacterium tuberculosis
2.6.1.36 lysine-epsilon-aminotransferase
-
 Mycobacterium tuberculosis

Temperature Optimum [°C]

EC Number Temperature Optimum [°C] Temperature Optimum Maximum [°C] Comment Organism
2.6.1.36 37
-
 assay at Mycobacterium tuberculosis

pH Optimum

EC Number pH Optimum Minimum pH Optimum Maximum Comment Organism
2.6.1.36 7.2
-
 assay at Mycobacterium tuberculosis

Cofactor

EC Number Cofactor Comment Organism Structure
2.6.1.36 pyridoxal 5'-phosphate at 0.015 mM Mycobacterium tuberculosis

IC50 Value

EC Number IC50 Value IC50 Value Maximum Comment Organism Inhibitor Structure
2.6.1.36 0.00115
-
 pH 7.2, 37°C Mycobacterium tuberculosis (E)-5-(5-(2-(benzo[d]thiazol-2-yl)-2-cyanovinyl)furan-2-yl)isophthalic acid
2.6.1.36 0.00262
-
 pH 7.2, 37°C Mycobacterium tuberculosis (E)-4-(5-(2-(benzo[d]thiazol-2-yl)-2-cyanovinyl)thiophen-2-yl)isophthalic acid
2.6.1.36 0.00308
-
 pH 7.2, 37°C Mycobacterium tuberculosis (E)-2-(4-(2-(benzo[d]thiazol-2-yl)-2-cyanovinyl)phenoxy)acetic acid
2.6.1.36 0.00374
-
 pH 7.2, 37°C Mycobacterium tuberculosis (E)-3-(5-(2-(benzo[d]thiazol-2-yl)-2-cyanovinyl)furan-2-yl)benzoic acid
2.6.1.36 0.00411
-
 pH 7.2, 37°C Mycobacterium tuberculosis (E)-2-(benzo[d]thiazol-2-yl)-3-(4-fluorophenyl)acrylonitrile
2.6.1.36 0.00573
-
 pH 7.2, 37°C Mycobacterium tuberculosis (E)-3-(5-(2-(benzo[d]thiazol-2-yl)-2-cyanovinyl)thiophen-2-yl)benzoic acid
2.6.1.36 0.00672
-
 pH 7.2, 37°C Mycobacterium tuberculosis (E)-4-(5-(2-(benzo[d]thiazol-2-yl)-2-cyanovinyl)thiophen-2-yl)benzoic acid
2.6.1.36 0.00783
-
 pH 7.2, 37°C Mycobacterium tuberculosis (E)-2-(benzo[d]thiazol-2-yl)-3-(4-hydroxy-3-methoxyphenyl)acrylonitrile
2.6.1.36 0.01038
-
 pH 7.2, 37°C Mycobacterium tuberculosis (E)-2-(benzo[d]thiazol-2-yl)-3-(4-hydroxyphenyl)acrylonitrile
2.6.1.36 0.01406
-
 pH 7.2, 37°C Mycobacterium tuberculosis (E)-4-(5-(2-(benzo[d]thiazol-2-yl)-2-cyanovinyl)furan-2-yl)benzoic acid
2.6.1.36 0.01623
-
 pH 7.2, 37°C Mycobacterium tuberculosis (E)-2-(benzo[d]thiazol-2-yl)-3-(furan-2-yl)acrylonitrile
2.6.1.36 0.01705
-
 pH 7.2, 37°C Mycobacterium tuberculosis (E)-2-(benzo[d]thiazol-2-yl)-3-(1H-pyrrol -2-yl)acrylonitrile
2.6.1.36 0.01959
-
 pH 7.2, 37°C Mycobacterium tuberculosis (E)-2-(benzo[d]thiazol-2-yl)-3-(5-nitrofuran-2-yl)acrylonitrile
2.6.1.36 0.02319
-
 pH 7.2, 37°C Mycobacterium tuberculosis (E)-2-(benzo[d]thiazol-2-yl)-3-(2,4-dihydroxyphenyl)acrylonitrile
2.6.1.36 0.03791
-
 pH 7.2, 37°C Mycobacterium tuberculosis (E)-2-(benzo[d]thiazol-2-yl)-3-(1H-indol-3-yl)acrylonitrile
2.6.1.36 0.04793
-
 pH 7.2, 37°C Mycobacterium tuberculosis (E)-2-(benzo[d]thiazol-2-yl)-3-(4-benzyloxyphenyl)acrylonitrile
2.6.1.36 0.05378
-
 pH 7.2, 37°C Mycobacterium tuberculosis (E)-2-(2-(2-(benzo[d]thiazol-2-yl)-2-cyanovinyl)phenoxy)acetic acid
2.6.1.36 0.05476
-
 pH 7.2, 37°C Mycobacterium tuberculosis (E)-2-(benzo[d]thiazol-2-yl)-3-(5-nitrothiophen-2-yl)acrylonitrile
2.6.1.36 0.06141
-
 pH 7.2, 37°C Mycobacterium tuberculosis (E)-2-(benzo[d]thiazol-2-yl)-3-(3,4-dimethoxyphenyl)acrylonitrile
2.6.1.36 0.06489
-
 pH 7.2, 37°C Mycobacterium tuberculosis (E)-2-(benzo[d]thiazol-2-yl)-3-(3,4,5-trimethoxyphenyl)acrylonitrile
2.6.1.36 0.06598
-
 pH 7.2, 37°C Mycobacterium tuberculosis (E)-3-(benzo[d][1,3]dioxol-5-yl)-2-(benzo[d]thiazol-2-yl)acrylonitrile
2.6.1.36 0.09257
-
 pH 7.2, 37°C Mycobacterium tuberculosis (E)-2-(benzo[d]thiazol-2-yl)-3-(thiophen-2-yl)acrylonitrile

General Information

EC Number General Information Comment Organism
2.6.1.36 physiological function Mycobacterium tuberculosis lysine-epsilon-aminotransferase (LAT) plays a crucial role in persistence and antibiotic tolerance. LAT serves as a potential target in the management of latent tuberculosis Mycobacterium tuberculosis