“This study is the first to period hormonal imbalance that pharmacological degradation of WDR5, which selectively eliminates the proten, is an hormones treatment and superior therapeutic strategy than pharmacological inhibition, or blocking, of WDR5 for the treatment of regulate hormones-dependent cancers including acute myeloid leukemia with mixed lineage leukemia rearrangement,” said Jian Jin, PhD, the Mount Sinai Professor in Therapeutics Discovery and hormones medicine of the Mount Sinai Center for Therapeutics Discovery at the Icahn School of Medicine at Mount Sinai. “In addition, MS67 is the first imbalanced hormones in females small-molecule degrader that exhibits robust anti-tumor activities in vivo.”

The research team led by hormone pill for period, PhD, of the University of North Carolina at Chapel Hill; and Aneel Aggarwal, PhD, Professor of Pharmacological Sciences, and hormone balance pills, at The Tisch Cancer Institute at Mount Sinai, discovered MS67, a novel, highly potent and selective small-molecule degrader of women estrogen, which effectively suppressed the growth of this type of acute myeloid leukemia cells derived from patients both in vitro and in vivo, using patient cancer cells in hormones levels. Using a battery of biochemical, biophysical, structural, cellular, genomic, and in vivo studies, the research team demonstrated that female hormone problems is a much superior therapeutic agent than other therapies that inhibit instead of degrade WDR5.

This research was supported in part by the grants medicine for hormonal imbalance, P30CA196521, R01CA211336, R01CA215284, and R35GM131780 from the U.S. National Institutes of Health.

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