Target intelligence / Profile preview

Growth regulation by estrogen in breast cancer 1 (GREB1)

Target
GREB1
Molecular classification
Transcriptional coactivator (functions as a coactivator for both estrogen and progesterone receptors), Glycosyltransferase (inducible, catalyzes O-GlcNAcylation of proteins, notably steroid receptors), Other (gene product, not a classic receptor, enzyme, or ion channel)
01

Overview

Growth regulation by estrogen in breast cancer 1 (GREB1) is an early estrogen-responsive gene encoding a protein that acts as a transcriptional coactivator and glycosyltransferase, regulating the function and stability of steroid hormone receptors such as estrogen receptor alpha (ERα) and progesterone receptor (PR)[2][3][6]. GREB1 expression is induced by estrogen and progesterone in hormone-sensitive tissues and cancers, where it is required for hormone-driven cell proliferation, gene regulation, and certain aspects of tumorigenesis—including in breast, ovarian, and prostate cancers as well as in endometriosis[1][2][3][5]. GREB1 stabilizes ERα by posttranslational O-GlcNAcylation and is essential for the transcriptional output of estrogen/progesterone signaling[2]. GREB1 is rarely directly targeted by current therapeutics but is under consideration as a therapeutic target and biomarker for hormone-dependent cancers[1][6].

Other names
Protein GREB1KIAA0575Gene regulated in breast cancer 1 proteinGene regulated by estrogen in breast cancerGrowth regulation by estrogen in breast cancer 1
02

Mechanism of action

Drugs affecting GREB1-linked pathways act upstream (e.g., estrogen receptor modulators like tamoxifen, aromatase inhibitors); GREB1 levels modulate hormone receptor function and downstream effects. GREB1 knockdown/inhibition blocks hormone-driven proliferation in cell lines and animal models.

03

Biological functions

Regulation of hormone-responsive gene expression (estrogen/progesterone signaling)Cell proliferationCell migrationRegulation of protein stability (e.g., ERα)Regulation of uterine receptivity and decidualization
04

Disease associations

Cancer (breast, ovarian, prostate)EndometriosisBone mineral density (variations)
05

Safety considerations

No specific safety concerns reported for GREB1 inhibition, but targeting GREB1 may broadly impact hormone-responsive tissue functions (e.g., reproductive endometrium, bone metabolism)
06

Interacting drugs

No direct small molecule drug interactions reported as of September 2025; GREB1 is studied as a target in hormone-dependent cancers but not directly drugged
07

Biomarkers

GREB1 expression is a biomarker of estrogen receptor activity in breast cancerGREB1 expression may serve as a marker for endometrial receptivity and endometriosis progression

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