| Structural highlights
4kp7 is a 2 chain structure with sequence from Plafx. Full crystallographic information is available from OCA. For a guided tour on the structure components use FirstGlance.
| | Ligands: | , , |
| Related: | 3au8, 3au9 |
| Gene: | codon optimized form, DXR, synthetic (PLAFX) |
| Activity: | 1-deoxy-D-xylulose-5-phosphate reductoisomerase, with EC number 1.1.1.267 |
| Resources: | FirstGlance, OCA, PDBe, RCSB, PDBsum, ProSAT |
Function
[DXR_PLAFX] Catalyzes the NADP-dependent rearrangement and reduction of 1-deoxy-D-xylulose-5-phosphate (DXP) to 2-C-methyl-D-erythritol 4-phosphate (MEP).[1]
Publication Abstract from PubMed
The emergence and spread of multidrug-resistant pathogens is widely believed to endanger human health. New drug targets and lead compounds exempt from cross-resistance with existing drugs are urgently needed. We report on the synthesis and properties of "reverse" thia-analogs of fosmidomycin, which inhibit the first committed enzyme of a metabolic pathway that is essential for the causative agents of tuberculosis and malaria but is absent in the human host. Notably, IspC displays a high level of enantioselectivity for an alpha-susbtituted fosmidomycin derivative.
IspC as target for antiinfective drug discovery: Synthesis, enantiomeric separation and structural biology of fosmidomycin thia-isosters.,Kunfermann A, Lienau C, Illarionov B, Held J, Grawert T, Behrendt CT, Werner P, Hahn S, Eisenreich W, Riederer U, Mordmuller B, Bacher A, Fischer M, Groll M, Kurz T J Med Chem. 2013 Sep 13. PMID:24032981[2]
From MEDLINE®/PubMed®, a database of the U.S. National Library of Medicine.
See Also
References
- ↑ Jomaa H, Wiesner J, Sanderbrand S, Altincicek B, Weidemeyer C, Hintz M, Turbachova I, Eberl M, Zeidler J, Lichtenthaler HK, Soldati D, Beck E. Inhibitors of the nonmevalonate pathway of isoprenoid biosynthesis as antimalarial drugs. Science. 1999 Sep 3;285(5433):1573-6. PMID:10477522
- ↑ Kunfermann A, Lienau C, Illarionov B, Held J, Grawert T, Behrendt CT, Werner P, Hahn S, Eisenreich W, Riederer U, Mordmuller B, Bacher A, Fischer M, Groll M, Kurz T. IspC as target for antiinfective drug discovery: Synthesis, enantiomeric separation and structural biology of fosmidomycin thia-isosters. J Med Chem. 2013 Sep 13. PMID:24032981 doi:10.1021/jm4012559
|
