molecules of the month

compound 10

oral PPARg phosphorylation inhibitor, partial agonist

efficacy in diabetic mouse model

from structure-based virtual screen

ACS Med. Chem. Lett.

AstraZeneca, Gothenburg, SE

oral PPARg phosphorylation inhibitor, partial agonist - AstraZeneca, Gothenburg, SE
3 mins read

Context. “Compound 10” (AstraZeneca) is an oral CDK5-mediated PPARγ phosphorylation inhibitor and partial PPARγ agonist being developed as an antidiabetic drug. Although widely used PPARγ agonists such as rosiglitazone and pioglitazone are effective antidiabetics, they are limited by their side effects which have been attributed to PPARγ agonism. AstraZeneca researchers therefore sought compounds with only negligible PPARγ agonism but demonstrating potent binding and subsequent inhibition of CDK5-mediated Ser273 phosphorylation PPARγ which is thought to mediate the positive antidiabetic effects of PPARγ agonists. Preclinical data revealed that the molecule only has moderate plasma glucose and insulin lowering effects, making further development and improvement necessary if the compound is to have a future in antidiabetic therapy. The molecule was nominated by Dr.…

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