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2fm5

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{{STRUCTURE_2fm5| PDB=2fm5 | SCENE= }}
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'''Crystal structure of PDE4D2 in complex with inhibitor L-869299'''
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===Crystal structure of PDE4D2 in complex with inhibitor L-869299===
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==Overview==
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Type 4 phosphodiesterase (PDE4) inhibitors are emerging as new treatments for a number of disorders including asthma and chronic obstructive pulmonary disease. Here we report the biochemical characterization on the second generation inhibitor (+)-1 (L-, IC50=0.4 nM) and its enantiomer (-)-1 (L-, IC50=43 nM) and their cocrystal structures with PDE4D at 2.0 A resolution. Despite the 107-fold affinity difference, both enantiomers interact with the same sets of residues in the rigid active site. The weaker (-)-1 adopts an unfavorable conformation to preserve the pivotal interactions between the Mg-bound waters and the N-oxide of pyridine. These structures support a model in which inhibitors are anchored by the invariant glutamine at one end and the metal-pocket residues at another end. This model provides explanations for most of the observed structure-activity relationship and the metal ion dependency of the catechol-ether based inhibitors and should facilitate their further design.
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==About this Structure==
==About this Structure==
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[[Category: L-869299]]
[[Category: L-869299]]
[[Category: Pde4]]
[[Category: Pde4]]
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''Page seeded by [http://oca.weizmann.ac.il/oca OCA ] on Sun May 4 04:03:35 2008''
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''Page seeded by [http://oca.weizmann.ac.il/oca OCA ] on Tue Jul 29 12:33:35 2008''

Revision as of 09:33, 29 July 2008

Image:2fm5.png

Template:STRUCTURE 2fm5

Crystal structure of PDE4D2 in complex with inhibitor L-869299

Template:ABSTRACT PUBMED 16539372

About this Structure

2FM5 is a Single protein structure of sequence from Homo sapiens. Full crystallographic information is available from OCA.

Reference

Enantiomer discrimination illustrated by the high resolution crystal structures of type 4 phosphodiesterase., Huai Q, Sun Y, Wang H, Macdonald D, Aspiotis R, Robinson H, Huang Z, Ke H, J Med Chem. 2006 Mar 23;49(6):1867-73. PMID:16539372

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