1q9m

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{{Seed}}
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{{STRUCTURE_1q9m| PDB=1q9m | SCENE= }}
{{STRUCTURE_1q9m| PDB=1q9m | SCENE= }}
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'''Three dimensional structures of PDE4D in complex with roliprams and implication on inhibitor selectivity'''
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===Three dimensional structures of PDE4D in complex with roliprams and implication on inhibitor selectivity===
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==Overview==
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Selective inhibitors against the 11 families of cyclic nucleotide phosphodiesterases (PDEs) are used to treat various human diseases. How the inhibitors selectively bind the conserved PDE catalytic domains is unknown. The crystal structures of the PDE4D2 catalytic domain in complex with (R)- or (R,S)-rolipram suggest that inhibitor selectivity is determined by the chemical nature of amino acids and subtle conformational changes of the binding pockets. The conformational states of Gln369 in PDE4D2 may play a key role in inhibitor recognition. The corresponding Y329S mutation in PDE7 may lead to loss of the hydrogen bonds between rolipram and Gln369 and is thus a possible reason explaining PDE7's insensitivity to rolipram inhibition. Docking of the PDE5 inhibitor sildenafil into the PDE4 catalytic pocket further helps understand inhibitor selectivity.
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(as it appears on PubMed at http://www.pubmed.gov), where 12842049 is the PubMed ID number.
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{{ABSTRACT_PUBMED_12842049}}
==About this Structure==
==About this Structure==
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[[Category: Rolipram]]
[[Category: Rolipram]]
[[Category: Specific inhibitor]]
[[Category: Specific inhibitor]]
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''Page seeded by [http://oca.weizmann.ac.il/oca OCA ] on Sat May 3 06:02:30 2008''
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''Page seeded by [http://oca.weizmann.ac.il/oca OCA ] on Tue Jul 29 08:25:19 2008''

Revision as of 05:25, 29 July 2008

Image:1q9m.png

Template:STRUCTURE 1q9m

Three dimensional structures of PDE4D in complex with roliprams and implication on inhibitor selectivity

Template:ABSTRACT PUBMED 12842049

About this Structure

1Q9M is a Single protein structure of sequence from Homo sapiens. This structure supersedes the now removed PDB entry 1oym. Full crystallographic information is available from OCA.

Reference

Three-dimensional structures of PDE4D in complex with roliprams and implication on inhibitor selectivity., Huai Q, Wang H, Sun Y, Kim HY, Liu Y, Ke H, Structure. 2003 Jul;11(7):865-73. PMID:12842049

Page seeded by OCA on Tue Jul 29 08:25:19 2008

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