Endoxifen is a new potent inhibitor of PKC: A potential therapeutic agent for bipolar disorder |
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Authors: | Shoukath M Ali Ateeq Ahmad Syed Shahabuddin Moghis U Ahmad Saifuddin Sheikh Imran Ahmad |
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Institution: | Jina Pharmaceuticals, Inc. 28100 N. Ashley Circle, Suite 103, Libertyville, IL 60048, USA |
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Abstract: | 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. |
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