2ntn
From Proteopedia
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| , resolution 2.30Å | |||||||
|---|---|---|---|---|---|---|---|
| Gene: | fabG, fabG1 (Mycobacterium tuberculosis) | ||||||
| Activity: | [acyl-carrier-protein_reductase 3-oxoacyl-[acyl-carrier-protein] reductase], with EC number 1.1.1.100 | ||||||
| Coordinates: | save as pdb, mmCIF, xml | ||||||
Crystal structure of MabA-C60V/G139A/S144L
Overview
The MabA protein from Mycobacterium tuberculosis is a validated drug target. Previous structural studies of this protein showed dynamic behaviour in the catalytic site and described motion between an open 'active' holo form (with NADP) and a closed 'inactive' apo form (without NADP). Here, a mutation (G139A) is reported that leads to complete protein inactivation and freezes the catalytic site into its closed form, even in the presence of the cofactor. This observation suggests a new way to develop anti-MabA drugs via protein stabilization of the 'inactive' form.
About this Structure
2NTN is a Single protein structure of sequence from Mycobacterium tuberculosis. Full crystallographic information is available from OCA.
Reference
Lack of dynamics in the MabA active site kills the enzyme activity: practical consequences for drug-design studies., Poncet-Montange G, Ducasse-Cabanot S, Quemard A, Labesse G, Cohen-Gonsaud M, Acta Crystallogr D Biol Crystallogr. 2007 Aug;63(Pt 8):923-5. Epub 2007, Jul 17. PMID:17642518 [[Category: 3-oxoacyl-[acyl-carrier-protein] reductase]]
Page seeded by OCA on Thu Mar 20 17:50:58 2008
