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Development of a Novel Separase Inhibitor, Sepin 1, for Breast Cancer Therapy

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Technical Report,15 May 2015,14 May 2016

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Baylor College of Medicine Houston United States

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Currently there is no good therapy for two subtypes of human breast cancers BCwhich have aggressive disease phenotype, often resulting in high mortality. They include the triple negative BC TNBC, and the endocrine resistant Luminal B subtypes. Our goal in this project is to develop a new class of drugs targeted for these hard-to-treat tumors which is safe and effective. Towards that goal we have identified a novel target called Separase, anenzyme important for cell division. Separase is an oncogene which is overexpressed in 60 ofBC, 50 of TNBC, and 65 of Luminal-B tumors, and its over expression strongly correlates withhigh incidence of relapse, metastasis, and a lower 5-year overall survival rate. We hypothesize that modulation of Separase enzymatic activity constitutes a new therapeutic strategy for targeting resistant, Separase-overexpressing tumors, particularly the hard-to treatTNBC. Using a high through put screen, we have identified a novel small molecular inhibitor of Separase, named Sepin-1. The goal of this project has been, 1 to examine ephramocokinetics, pharmacodynamics, and the efficacy of Sepin-1 in animal models, and 2 to characterize the mechanisms of Sepin-1 action at the molecular level. This is the 1st annual progress report for this project.

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