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3cuk
From Proteopedia
| 3cuk, resolution 2.49Å () | |||||||||
|---|---|---|---|---|---|---|---|---|---|
| Sites: | , , , , , , and | ||||||||
| Ligands: | , | ||||||||
| Gene: | DAO, DAMOX (Homo sapiens) | ||||||||
| Activity: | D-amino-acid oxidase, with EC number 1.4.3.3 | ||||||||
| |||||||||
| Resources: | FirstGlance, OCA, PDBsum, RCSB | ||||||||
| Coordinates: | save as pdb, mmCIF, xml | ||||||||
Crystal structure of human D-amino acid oxidase: bound to an inhibitor
The 'NMDA hypofunction hypothesis of schizophrenia' can be tested in a number of ways. DAO is the enzyme primarily responsible for the metabolism of d-serine, a co-agonist for the NMDA receptor. We identified novel DAO inhibitors, in particular, acid 1, which demonstrated moderate potency for DAO in vitro and ex vivo, and raised plasma d-serine levels after dosing ip to rats. In parallel, analogues were prepared to survey the SARs of 1.
The discovery of fused pyrrole carboxylic acids as novel, potent D-amino acid oxidase (DAO) inhibitors., Sparey T, Abeywickrema P, Almond S, Brandon N, Byrne N, Campbell A, Hutson PH, Jacobson M, Jones B, Munshi S, Pascarella D, Pike A, Prasad GS, Sachs N, Sakatis M, Sardana V, Venkatraman S, Young MB, Bioorg Med Chem Lett. 2008 Jun 1;18(11):3386-91. Epub 2008 Apr 13. PMID:18455394
From MEDLINE®/PubMed®, a database of the U.S. National Library of Medicine.
About this Structure
3CUK is a 4 chains structure of sequences from Homo sapiens. Full crystallographic information is available from OCA.
Reference
- Sparey T, Abeywickrema P, Almond S, Brandon N, Byrne N, Campbell A, Hutson PH, Jacobson M, Jones B, Munshi S, Pascarella D, Pike A, Prasad GS, Sachs N, Sakatis M, Sardana V, Venkatraman S, Young MB. The discovery of fused pyrrole carboxylic acids as novel, potent D-amino acid oxidase (DAO) inhibitors. Bioorg Med Chem Lett. 2008 Jun 1;18(11):3386-91. Epub 2008 Apr 13. PMID:18455394 doi:10.1016/j.bmcl.2008.04.020
Page seeded by OCA on Tue Feb 17 10:12:00 2009
