Related Experiment Video

Updated: Jul 14, 2025

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

10.5K

Optimization of small molecule degraders and antagonists for targeting estrogen receptor based on breast cancer:

Jiaqi Yao1,2, Yiran Tao3, Zelin Hu1,2

  • 1General Practice Ward/International Medical Center, General Practice Medical Center, West China Hospital, Sichuan University, Chengdu, Sichuan, China.

Frontiers in Pharmacology
|October 9, 2023
PubMed

Insights

Novel drugs targeting the estrogen receptor (ER) show promise for treating ER-positive breast cancer. Selective estrogen receptor degraders (SERDs) and covalent antagonists (SERCAs) offer new therapeutic avenues beyond traditional SERMs.

Area of Science:

  • Endocrinology
  • Oncology
  • Medicinal Chemistry

Background:

  • The estrogen receptor (ER) is vital in physiological processes and ER-positive (ER+) breast cancer.
  • ER-targeting therapies like Tamoxifen (a SERM) are established but face challenges like drug resistance and side effects.
  • Novel ER-targeting agents, SERDs and SERCAs, are emerging to overcome these limitations.

Purpose of the Study:

  • To review the structural functions of the estrogen receptor.
  • To highlight advancements in SERD and SERCA small molecule drugs.
  • To discuss therapeutic potential and future directions for ER-targeted therapies in breast cancer and other ER-related diseases.

Main Methods:

  • Comprehensive literature review of ER structure-function relationships.
  • Analysis of recent developments in SERD and SERCA small molecule drug design.
  • Discussion of clinical applications and challenges of novel ER-targeted agents.

Main Results:

  • ER plays a critical role in various tissues, including breast cancer.
  • SERDs and SERCAs demonstrate potential in overcoming resistance and side effects associated with SERMs.
  • Structural optimization strategies for SERDs and SERCAs are crucial for enhancing efficacy.

Conclusions:

  • Novel SERDs and SERCAs represent a significant advancement in ER-targeted therapy for breast cancer.
  • Further research into structural optimization and therapeutic applications is warranted.
  • These agents hold promise for treating various ER-related diseases beyond breast cancer.
Keywords:
estrogen receptorselective estrogen receptor covalent antagonistselective estrogen receptor degradersmall molecule drugsstructural optimization

More Related Videos

Polymalic Acid-based Nano Biopolymers for Targeting of Multiple Tumor Markers: An Opportunity for Personalized Medicine?14:20

Polymalic Acid-based Nano Biopolymers for Targeting of Multiple Tumor Markers: An Opportunity for Personalized Medicine?

Published on: June 13, 2014

16.8K
Author Spotlight: Exploring Salidroside's Molecular Mechanisms in Breast Cancer Treatment11:13

Author Spotlight: Exploring Salidroside's Molecular Mechanisms in Breast Cancer Treatment

Published on: June 9, 2023

1.6K

Related Concept Videos

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...
7.7K
Structure-Activity Relationships and Drug Design01:28

Structure-Activity Relationships and Drug Design

Drug design is a dynamic field that involves discovering and developing new medications based on specific biological targets. This process heavily relies on structure-activity relationships (SAR) and quantitative structure-activity relationships (QSAR) to guide the design and optimization of efficient drugs.
SAR studies the intricate relationship between a drug's chemical structure and biological activity. It focuses on understanding how modifications to a drug's structure can influence...
742
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:
1.4K
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...
6.5K
Targets for Drug Action: Overview01:26

Targets for Drug Action: Overview

Drugs target macromolecules to modify ongoing cellular processes. Primary drug targets include receptors, ion channels, transporters, and enzymes.
Receptors are either membrane-spanning or intracellular proteins, which upon binding a ligand, get activated and transmit the signal downstream to elicit a response. Drugs bind receptors, either mimicking the action of endogenous ligands or blocking the receptor activity to bring about a modified response. Nearly 35% of approved drugs target the G...
6.3K
Drug Discovery: Overview01:26

Drug Discovery: Overview

Drug discovery is a multifaceted process involving extensive screening, testing, and optimization of lead compounds to identify potential new drugs for therapeutic use. It combines several approaches, including screening large numbers of natural products, chemical modification of known active molecules, identification of new drug targets, and rational design based on biological mechanisms and drug-receptor structure. These approaches are carried out in both academic research laboratories and...
8.0K