2q5g

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Image:2q5g.jpg

Template:STRUCTURE 2q5g

Ligand binding domain of PPAR delta receptor in complex with a partial agonist


Overview

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.

About this Structure

2Q5G is a Single protein structure of sequence from Homo sapiens. Full crystallographic information is available from OCA.

Reference

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 Page seeded by OCA on Wed Jun 4 09:51:38 2008

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