Application | Comment | Organism |
---|---|---|
pharmacology | the enzyme is a target for the development of new anti-tubercular drugs | Mycobacterium tuberculosis |
Crystallization (Comment) | Organism |
---|---|
overview of 80 available crystal structures of wild-type and mutant InhA, in its apo form, in complex with its cofactor, with an analogue of its natural ligands (C16 fatty acid and/or NADH) or with inhibitor | Mycobacterium tuberculosis |
Protein Variants | Comment | Organism |
---|---|---|
K165A | mutation prevents NADH from binding | Mycobacterium tuberculosis |
K165M | mutation prevents NADH from binding | Mycobacterium tuberculosis |
K165Q | mutation has no effect on NADH binding | Mycobacterium tuberculosis |
K165R | mutation has no effect on NADH binding | Mycobacterium tuberculosis |
Y158A | mutation improves the KM for the cofactor by a factor of 13 | Mycobacterium tuberculosis |
Y158F | mutation improves the KM for the cofactor by a factor of 33 | Mycobacterium tuberculosis |
Y158S | mutation has no effect on NADH binding | Mycobacterium tuberculosis |
Inhibitors | Comment | Organism | Structure |
---|---|---|---|
Ethionamide | the indirect inhibitor forms a covalent adduct with the cofactor | Mycobacterium tuberculosis | |
Genz10850 | - |
Mycobacterium tuberculosis | |
GENZ8575 | - |
Mycobacterium tuberculosis | |
isoniazid | the indirect inhibitor forms a covalent adduct with the cofactor, leading compound for antitubercular drug therapy | Mycobacterium tuberculosis | |
additional information | overview of 80 available crystal structures of wild-type and mutant InhA, in its apo form, in complex with its cofactor, with an analogue of its natural ligands (C16 fatty acid and/or NADH) or with inhibitors | Mycobacterium tuberculosis |
Organism | UniProt | Comment | Textmining |
---|---|---|---|
Mycobacterium tuberculosis | P9WGR1 | - |
- |
Mycobacterium tuberculosis ATCC 25618 | P9WGR1 | - |
- |
Synonyms | Comment | Organism |
---|---|---|
enoyl-ACP reductase InhA | - |
Mycobacterium tuberculosis |
IC50 Value | IC50 Value Maximum | Comment | Organism | Inhibitor | Structure |
---|---|---|---|---|---|
0.00016 | - |
pH and temperature not specified in the publication | Mycobacterium tuberculosis | Genz10850 | |
0.0024 | - |
pH and temperature not specified in the publication | Mycobacterium tuberculosis | GENZ8575 |
General Information | Comment | Organism |
---|---|---|
metabolism | the enzyme is involved in the mycobacterial fatty acid biosynthesis pathway. It is essential for the survival of Mycobacterium tuberculosis | Mycobacterium tuberculosis |
physiological function | the enzyme is the causative agent of tuberculosis | Mycobacterium tuberculosis |