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Literature summary extracted from

  • Rudraraju, R.S.; Daher, S.S.; Gallardo-Macias, R.; Wang, X.; Neiditch, M.B.; Freundlich, J.S.
    Mycobacterium tuberculosis KasA as a drug target structure-based inhibitor design (2022), Front. Cell. Infect. Microbiol., 12, 1008213.
    View publication on PubMed

Protein Variants

EC Number Protein Variants Comment Organism
2.3.1.293 C171Q site-directed mutagenesis, the mutant mimics acylated wild-type KasA Mycobacterium tuberculosis

Inhibitors

EC Number Inhibitors Comment Organism Structure
2.3.1.293 3-acetyl thiolactomycin
-
 Mycobacterium tuberculosis
2.3.1.293 3-ethyl thiolactomycin
-
 Mycobacterium tuberculosis
2.3.1.293 3-propyl thiolactomycin
-
 Mycobacterium tuberculosis
2.3.1.293 3-trifluoroacetyl thiolactomycin
-
 Mycobacterium tuberculosis
2.3.1.293 4,4,4-trifluoro-N-(isoquinolin-6-yl)butane-1-sulfonamide
-
 Mycobacterium tuberculosis
2.3.1.293 5-fluoro-N-(3-methyl-1H-indazol-6-yl)pentane-1-sulfonamide
-
 Mycobacterium tuberculosis
2.3.1.293 N-(1-methyl-1H-indazol-6-yl)butane-1-sulfonamide i.e. DG167 Mycobacterium tuberculosis
2.3.1.293 N-(1H-indazol-6-yl)butane-1-sulfonamide
-
 Mycobacterium tuberculosis
2.3.1.293 N-(2,3-dihydro-1H-inden-5-yl)butane-1-sulfonamide MIC value is 0.0163 mM Mycobacterium tuberculosis
2.3.1.293 N-(2-cyano-3-methyl-1H-indol-6-yl)hexane-1-sulfonamide
-
 Mycobacterium tuberculosis
2.3.1.293 N-(2-cyano-3-methyl-1H-indol-6-yl)pentane-1-sulfonamide
-
 Mycobacterium tuberculosis
2.3.1.293 N-(3-methyl-1H-indazol-6-yl)butane-1-sulfonamide
-
 Mycobacterium tuberculosis
2.3.1.293 thiolactomycin TLM, thiolactomycin chemotype as a malonyl binding site inhibitor, binding structure of KasA mutant C171Q bound to the following TLM analogues. TLM inhibits all three annotated Mycobacterum tuberculosis beta-ketoacyl synthases, in descending order KasA > KasB > FabH. Binding structure and inhibition mechanism, interaction profiles for wild-type KasA with inhibitory componds, overview Mycobacterium tuberculosis

Organism

EC Number Organism UniProt Comment Textmining
2.3.1.293 Mycobacterium tuberculosis P9WQD9
-
-
2.3.1.293 Mycobacterium tuberculosis ATCC 25618 P9WQD9
-
-
2.3.1.293 Mycobacterium tuberculosis H37Rv P9WQD9
-
-

Synonyms

EC Number Synonyms Comment Organism
2.3.1.293 3-oxoacyl-[acyl-carrier-protein] synthase 1 SwissProt Mycobacterium tuberculosis
2.3.1.293 beta-ketoacyl acyl carrier protein
-
 Mycobacterium tuberculosis
2.3.1.293 KasA
-
 Mycobacterium tuberculosis