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Design and synthesis of novel selective estrogen receptor degradation inducers based on the diphenylheptane skeleton.

ABSTRACT: Estrogen receptors (ERs) are a family of nuclear receptors (NRs) that regulate physiological effects such as reproduction and bone homeostasis. It has been reported that approximately 70% of human breast cancers are hormone-dependent and ER?-positive. Recently, novel anti-breast cancer drugs based on different mechanisms of action have received significant attention. In this article, we have designed and synthesized a selective ER degradation inducer based on the diphenylheptane skeleton. Western blotting analysis revealed that PBP-NC10 degraded ER? through the ubiquitin-proteasome system. We also performed computational docking analysis to predict the binding mode of PBP-NC10 to ER?.

SUBMITTER: Misawa T

PROVIDER: S-EPMC6072319 | biostudies-literature | 2017 Jan

REPOSITORIES: biostudies-literature

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Design and synthesis of novel selective estrogen receptor degradation inducers based on the diphenylheptane skeleton.

Misawa Takashi T Fujisato Takuma T Kanda Yasunari Y Ohoka Nobumichi N Shoda Takuji T Yorioka Momoko M Makishima Makoto M Sekino Yuko Y Naito Mikihiko M Demizu Yosuke Y Kurihara Masaaki M

MedChemComm 20161208 1

Estrogen receptors (ERs) are a family of nuclear receptors (NRs) that regulate physiological effects such as reproduction and bone homeostasis. It has been reported that approximately 70% of human breast cancers are hormone-dependent and ERα-positive. Recently, novel anti-breast cancer drugs based on different mechanisms of action have received significant attention. In this article, we have designed and synthesized a selective ER degradation inducer based on the diphenylheptane skeleton. Wester ...[more]

PMID: 30108709

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