Bioorganic and Medicinal Chemistry Letters 2010-Apr
Endoxifen is a new potent inhibitor of PKC: a potential therapeutic agent for bipolar disorder.
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Линкът е запазен в клипборда
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Резюме
Protein kinase C (PKC) plays a major role in regulation of both pre and postsynaptic neurotransmission. Excessive activation of PKC results in symptoms related to bipolar disorder. Tamoxifen, a widely used breast cancer drug is known to inhibit PKC and demonstrate antimanic properties in human. We describe herein the synthesis of endoxifen, a tamoxifen active metabolite and compared its PKC inhibitory activity with that of tamoxifen. Endoxifen exhibited fourfold higher potency compared to tamoxifen.