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2q5g
From Proteopedia
| 2q5g, resolution 2.70Å () | |||||||||
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| Ligands: | |||||||||
| Gene: | PPARD, NR1C2, PPARB (Homo sapiens) | ||||||||
| Related: | 2gwx
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| Resources: | FirstGlance, OCA, PDBsum, RCSB | ||||||||
| Coordinates: | save as pdb, mmCIF, xml | ||||||||
Contents |
Ligand binding domain of PPAR delta receptor in complex with a partial agonist
Structure based ligand design was used in order to design a partial agonist for the PPARdelta receptor. The maximum activation in the transactivation assay was reduced from 87% to 39%. The crystal structure of the ligand binding domain of the PPARdelta receptor in complex with compound 2 was determined in order to understand the structural changes which gave rise to the decrease in maximum activation.
Design of a partial PPARdelta agonist., Pettersson I, Ebdrup S, Havranek M, Pihera P, Korinek M, Mogensen JP, Jeppesen CB, Johansson E, Sauerberg P, Bioorg Med Chem Lett. 2007 Aug 15;17(16):4625-9. Epub 2007 May 27. PMID:17560785
From MEDLINE®/PubMed®, a database of the U.S. National Library of Medicine.
About this Structure
2q5g is a 2 chain structure with sequence from Homo sapiens. Full crystallographic information is available from OCA.
See Also
Reference
- Pettersson I, Ebdrup S, Havranek M, Pihera P, Korinek M, Mogensen JP, Jeppesen CB, Johansson E, Sauerberg P. Design of a partial PPARdelta agonist. Bioorg Med Chem Lett. 2007 Aug 15;17(16):4625-9. Epub 2007 May 27. PMID:17560785 doi:10.1016/j.bmcl.2007.05.079
