Drug intelligence / Profile preview

MA-6

Development stage
Preclinical
Lead developer
Johns Hopkins University
Modality
Small Molecules
01

Overview

MA-6 is a synthetic, structurally modified genistein derivative developed by researchers at Johns Hopkins University. It is designed as a selective estrogen receptor modulator (SERM) for the potential treatment and chemoprevention of estrogen receptor-alpha (ERα)-positive breast cancer. By linking the parent soy isoflavone genistein to aliphatic side-chains or heterocyclic triazole moieties, MA-6 is engineered to preclude standard agonist-induced conformational changes in the ERα pocket. In preclinical studies, MA-6 demonstrated potent antiproliferative and apoptotic activity in ER-positive breast cancer cell lines (such as MCF-7, 21PT, and T47D) at concentrations 10- to 15-fold lower than parent genistein. This growth inhibition is accompanied by a downregulation of ERα expression and an upregulation of estrogen receptor-beta (ERβ) levels, thereby increasing the protective ERβ/ERα ratio.

Other names
MA6MA-6MA 6modified genistein derivative MA-6
02

Targets

ESR1 (ERα)ESR2 (ERβ)

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