| Structural highlights
2w4i is a 4 chain structure with sequence from Helicobacter pylori. Full crystallographic information is available from OCA. For a guided tour on the structure components use FirstGlance.
| | Ligands: | ,
| | Related: | 2jfz, 2jfx, 2jfy |
| Activity: | Glutamate racemase, with EC number 5.1.1.3 |
| Resources: | FirstGlance, OCA, RCSB, PDBsum |
Evolutionary Conservation
Check, as determined by ConSurfDB. You may read the explanation of the method and the full data available from ConSurf.
Publication Abstract from PubMed
An SAR study of an HTS screening hit generated a series of pyridodiazepine amines as potent inhibitors of Helicobacter pylori glutamate racemase (MurI) showing highly selective anti-H. pylori activity, marked improved solubility, and reduced plasma protein binding. X-ray co-crystal E-I structures were obtained. These uncompetitive inhibitors bind at the MurI dimer interface.
Potent and selective inhibitors of Helicobacter pylori glutamate racemase (MurI): pyridodiazepine amines.,Geng B, Basarab G, Comita-Prevoir J, Gowravaram M, Hill P, Kiely A, Loch J, MacPherson L, Morningstar M, Mullen G, Osimboni E, Satz A, Eyermann C, Lundqvist T Bioorg Med Chem Lett. 2009 Feb 1;19(3):930-6. Epub 2008 Dec 6. PMID:19097892[1]
From MEDLINE®/PubMed®, a database of the U.S. National Library of Medicine.
See Also
References
- ↑ Geng B, Basarab G, Comita-Prevoir J, Gowravaram M, Hill P, Kiely A, Loch J, MacPherson L, Morningstar M, Mullen G, Osimboni E, Satz A, Eyermann C, Lundqvist T. Potent and selective inhibitors of Helicobacter pylori glutamate racemase (MurI): pyridodiazepine amines. Bioorg Med Chem Lett. 2009 Feb 1;19(3):930-6. Epub 2008 Dec 6. PMID:19097892 doi:S0960-894X(08)01490-X
|
