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Literature summary for 2.6.1.36 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
Search for more literature for 2.6.1.36

Inhibitors

Inhibitors Comment Organism Structure
(E)-2-(2-(2-(benzo[d]thiazol-2-yl)-2-cyanovinyl)phenoxy)acetic acid
-
 Mycobacterium tuberculosis
(E)-2-(4-(2-(benzo[d]thiazol-2-yl)-2-cyanovinyl)phenoxy)acetic acid
-
 Mycobacterium tuberculosis
(E)-2-(benzo[d]thiazol-2-yl)-3-(1H-indol-3-yl)acrylonitrile
-
 Mycobacterium tuberculosis
(E)-2-(benzo[d]thiazol-2-yl)-3-(1H-pyrrol -2-yl)acrylonitrile
-
 Mycobacterium tuberculosis
(E)-2-(benzo[d]thiazol-2-yl)-3-(2,4-dihydroxyphenyl)acrylonitrile
-
 Mycobacterium tuberculosis
(E)-2-(benzo[d]thiazol-2-yl)-3-(3,4,5-trimethoxyphenyl)acrylonitrile
-
 Mycobacterium tuberculosis
(E)-2-(benzo[d]thiazol-2-yl)-3-(3,4-dimethoxyphenyl)acrylonitrile
-
 Mycobacterium tuberculosis
(E)-2-(benzo[d]thiazol-2-yl)-3-(4-benzyloxyphenyl)acrylonitrile
-
 Mycobacterium tuberculosis
(E)-2-(benzo[d]thiazol-2-yl)-3-(4-fluorophenyl)acrylonitrile
-
 Mycobacterium tuberculosis
(E)-2-(benzo[d]thiazol-2-yl)-3-(4-hydroxy-3-methoxyphenyl)acrylonitrile
-
 Mycobacterium tuberculosis
(E)-2-(benzo[d]thiazol-2-yl)-3-(4-hydroxyphenyl)acrylonitrile
-
 Mycobacterium tuberculosis
(E)-2-(benzo[d]thiazol-2-yl)-3-(5-nitrofuran-2-yl)acrylonitrile
-
 Mycobacterium tuberculosis
(E)-2-(benzo[d]thiazol-2-yl)-3-(5-nitrothiophen-2-yl)acrylonitrile
-
 Mycobacterium tuberculosis
(E)-2-(benzo[d]thiazol-2-yl)-3-(furan-2-yl)acrylonitrile
-
 Mycobacterium tuberculosis
(E)-2-(benzo[d]thiazol-2-yl)-3-(thiophen-2-yl)acrylonitrile
-
 Mycobacterium tuberculosis
(E)-3-(5-(2-(benzo[d]thiazol-2-yl)-2-cyanovinyl)furan-2-yl)benzoic acid
-
 Mycobacterium tuberculosis
(E)-3-(5-(2-(benzo[d]thiazol-2-yl)-2-cyanovinyl)thiophen-2-yl)benzoic acid
-
 Mycobacterium tuberculosis
(E)-3-(benzo[d][1,3]dioxol-5-yl)-2-(benzo[d]thiazol-2-yl)acrylonitrile
-
 Mycobacterium tuberculosis
(E)-4-(5-(2-(benzo[d]thiazol-2-yl)-2-cyanovinyl)furan-2-yl)benzoic acid
-
 Mycobacterium tuberculosis
(E)-4-(5-(2-(benzo[d]thiazol-2-yl)-2-cyanovinyl)thiophen-2-yl)benzoic acid
-
 Mycobacterium tuberculosis
(E)-4-(5-(2-(benzo[d]thiazol-2-yl)-2-cyanovinyl)thiophen-2-yl)isophthalic acid
-
 Mycobacterium tuberculosis
(E)-5-(5-(2-(benzo[d]thiazol-2-yl)-2-cyanovinyl)furan-2-yl)isophthalic acid
-
 Mycobacterium tuberculosis
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)

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

Organism

Organism UniProt Comment Textmining
Mycobacterium tuberculosis P9WQ77
-
-
Mycobacterium tuberculosis ATCC 25618 P9WQ77
-
-
Mycobacterium tuberculosis H37Rv P9WQ77
-
-

Substrates and Products (Substrate)

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

Synonyms

Synonyms Comment Organism
LAT
-
 Mycobacterium tuberculosis
lysine-epsilon-aminotransferase
-
 Mycobacterium tuberculosis

Temperature Optimum [°C]

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

pH Optimum

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

Cofactor

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

IC50 Value

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

General Information

General Information Comment Organism
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