Minireview: The effects of species ortholog and SNP variation on receptors for free fatty acids.

Although both series have been successfully used to block FFA1 responses in rodent insulinoma cell lines ( 25 , 51 ), we find that, at least in a Ca 2+ mobilization assay, although GW1100 has similar activity at human and rodent orthologs, the Pfizer compounds are significantly human selective ( Figure 1 ), suggesting that there are likely to be significant species ortholog issues to be considered when using these FFA1 antagonists in nonhuman systems.

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One study examining this polymorphism found no difference in pharmacology between it and wild-type FFA4 and only a weak trend toward an association between the polymorphism and obesity in humans [odds ratio 1.16] ( 22 ).

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