Nicotinic acids: Liver-targeted SCD inhibitors with preclinical anti-diabetic efficacy
2011
Abstract An in vitro screening protocol was used to transform a systemically-distributed SCD inhibitor into a liver-targeted compound. Incorporation of a key nicotinic acid moiety enables molecular recognition by OATP transporters, as demonstrated by uptake studies in transfected cell lines, and likely serves as a critical component of the observed liver-targeted tissue distribution profile. Preclinical anti-diabetic oGTT efficacy is demonstrated with nicotinic acid-based, liver-targeting SCD inhibitor 10 , and studies with a close-structural analog devoid of SCD1 activity, suggest this efficacy is a result of on-target activity.
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