Related Experiment Video

Updated: Feb 25, 2026

Systems Biology of Metabolic Regulation by Estrogen Receptor Signaling in Breast Cancer
10:36

Systems Biology of Metabolic Regulation by Estrogen Receptor Signaling in Breast Cancer

Published on: March 17, 2016

11.0K

Estrogen receptor coregulator binding modulators (ERXs) effectively target estrogen receptor positive human breast

Ganesh V Raj1, Gangadhara Reddy Sareddy2,3, Shihong Ma1

  • 1Departments of Urology and Pharmacology, University of Texas Southwestern Medical Center at Dallas, Dallas, United States.

Elife
|August 9, 2017
PubMed

Insights

A new drug, ERX-11, targets estrogen receptor alpha (ER) in breast cancer. It effectively blocks cancer cell growth in both sensitive and resistant tumors, offering a promising new therapy.

Area of Science:

  • Oncology
  • Molecular Biology
  • Pharmacology

Background:

  • Estrogen receptor alpha (ER)-positive breast cancer is common.
  • Anti-estrogen therapies are initially effective but often lead to drug resistance.
  • Therapy-resistant tumors frequently maintain ER signaling through coregulator interactions.

Purpose of the Study:

  • To develop a novel therapeutic agent targeting ER coregulator interactions.
  • To investigate the efficacy of ERX-11 in preclinical breast cancer models.

Main Methods:

  • Development of ERX-11, a novel ER coregulator binding modulator.
  • Assessment of ERX-11's ability to block coregulator-ER interactions.
  • Evaluation of ERX-11's anti-proliferative activity in vitro and in vivo.

Main Results:

  • ERX-11 directly interacts with ER, inhibiting critical coregulator binding.
  • ERX-11 demonstrates potent anti-proliferative effects against therapy-sensitive and resistant breast cancer cells.
  • ERX-11 is orally bioavailable, well-tolerated, and effective in xenograft and patient-derived tumor models.

Conclusions:

  • ERX-11 represents a first-in-class agent with a novel mechanism of action.
  • This agent overcomes limitations of current breast cancer therapies by disrupting protein-protein interactions.
  • ERX-11 shows significant clinical potential for treating both therapy-sensitive and resistant breast cancers.
Keywords:
E. colibreast cancercancer biologycoagulator binding modulatorcoregulatorsendocrine therapyestrogen receptormouse

More Related Videos

Profiling of Estrogen-regulated MicroRNAs in Breast Cancer Cells16:24

Profiling of Estrogen-regulated MicroRNAs in Breast Cancer Cells

Published on: February 21, 2014

20.8K
Detecting the Ligand-binding Domain Dimerization Activity of Estrogen Receptor Alpha Using the Mammalian Two-Hybrid Assay09:07

Detecting the Ligand-binding Domain Dimerization Activity of Estrogen Receptor Alpha Using the Mammalian Two-Hybrid Assay

Published on: December 19, 2018

6.8K

Related Concept Videos

Transducer Mechanism: Nuclear Receptors01:31

Transducer Mechanism: Nuclear Receptors

Nuclear receptors, or NRs, are unique transcription factors that regulate gene transcription and affect the cellular pathways involved in reproduction, development, or metabolism. Their ability to be stimulated by small lipophilic ligands and control vital cellular processes makes them ideal drug targets. Nearly 10-15% of currently prescribed drugs target these receptors.
About 48 different soluble family members of nuclear receptors are identified that can be divided into two main classes:
3.3K
Targeted Cancer Therapies02:57

Targeted Cancer Therapies

The targeted cancer therapies, also known as “molecular targeted therapies,” take advantage of the molecular and genetic differences between the cancer cells and the normal cells. It needs a thorough understanding of the cancer cells to develop drugs that can target specific molecular aspects that drive the growth, progression, and spread of cancer cells without affecting the growth and survival of other normal cells in the body.
There are several types of targeted therapies against...
9.0K
Mitogens and the Cell Cycle02:38

Mitogens and the Cell Cycle

Mitogens and their receptors play a crucial role in controlling the progression of the cell cycle. However, the loss of mitogenic control over cell division leads to tumor formation. Therefore, mitogens and mitogen receptors play an important role in cancer research. For instance, the epidermal growth factor (EGF) - a type of mitogen and its transmembrane receptor (EGFR), decides the fate of the cell's proliferation. When EGF binds to EGFR, a member of the ErbB family of tyrosine kinase...
8.2K
Receptor Downregulation in MVBs01:15

Receptor Downregulation in MVBs

Multivesicular bodies (MVBs) are mature endosomes that sort ubiquitinated proteins and then fuse with lysosomes to degrade the sorted proteins. Epidermal growth factor (EGF) and its receptor (EGFR) form a complex that can be internalized through endocytosis, sorted into an MVB, and later degraded.
The EGFR can initiate signaling pathways that  lead to cell proliferation, migration, and differentiation. Overexpression of EGFR  stimulates cells to proliferate. Excessive  EGFR...
2.9K
Treatment Resistant Cancers02:56

Treatment Resistant Cancers

Cancer is the second leading cause of death in the United States. A cancer cell is genetically unstable and hence can mutate faster. They can also modify their microenvironment and escape immune surveillance. The difficulties in treating cancer are further compounded by the emergence of rapid resistance to anticancer drugs. The most common ways to attain resistance in cancer cells include alteration in drug transport and metabolism, modification of drug target, elevated DNA damage response, or...
3.8K
Transducer Mechanism: Enzyme-Linked Receptors01:27

Transducer Mechanism: Enzyme-Linked Receptors

Enzyme-linked receptors are cell-surface receptors acting as an enzyme or associating with an enzyme intracellularly. They make excellent drug targets. Drugs can bind to the extracellular ligand-binding domain or directly affect their enzymatic domain and alter their activity.
Major types that are helpful drug targets include:
4.5K