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Docking of competitive inhibitors to the P2X7 receptor family reveals key differences responsible for changes in response between rat and human.

Caseley EA, Muench SP, Baldwin SA, Simmons K, Fishwick CW, Jiang LH - Bioorg. Med. Chem. Lett. (2015)

Bottom Line: Importantly this residue is replaced by Leu in the rat P2X7 receptor resulting in a significantly reduced binding affinity.This work provides new insights into binding of P2X7 inhibitors and shows the structural difference in human and rat P2X7 receptors which results in a difference in affinity.Such information is useful both for the rational design of inhibitors based on these scaffolds and also the way in which these compounds are tested in animal models.

View Article: PubMed Central - PubMed

Affiliation: School of Biomedical Sciences, University of Leeds, Leeds, UK. Electronic address: bs09e2c@leeds.ac.uk.

No MeSH data available.


Related in: MedlinePlus

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Docking of competitive inhibitors to the P2X7 receptor family reveals key differences responsible for changes in response between rat and human.

Caseley EA, Muench SP, Baldwin SA, Simmons K, Fishwick CW, Jiang LH - Bioorg. Med. Chem. Lett. (2015)

© Copyright Policy - CC BY
Related In: Results  -  Collection

License
Show All Figures
getmorefigures.php?uid=PMC4508345&req=5

Bottom Line: Importantly this residue is replaced by Leu in the rat P2X7 receptor resulting in a significantly reduced binding affinity.This work provides new insights into binding of P2X7 inhibitors and shows the structural difference in human and rat P2X7 receptors which results in a difference in affinity.Such information is useful both for the rational design of inhibitors based on these scaffolds and also the way in which these compounds are tested in animal models.

View Article: PubMed Central - PubMed

Affiliation: School of Biomedical Sciences, University of Leeds, Leeds, UK. Electronic address: bs09e2c@leeds.ac.uk.

No MeSH data available.


Related in: MedlinePlus