Related Experiment Video

Updated: Aug 6, 2026

Inducible and Reversible Dominant-negative (DN) Protein Inhibition
08:35

Inducible and Reversible Dominant-negative (DN) Protein Inhibition

Published on: January 7, 2019

A new class of retinoids with selective inhibition of AP-1 inhibits proliferation

A Fanjul1, M I Dawson, P D Hobbs

  • 1Cancer Center, La Jolla Cancer Research Foundation, La Jolla, California 92037.

Nature
|November 3, 1994
PubMed

Insights

New retinoids selectively inhibit AP-1 activity without transcriptional activation. These compounds reduce tumor cell proliferation, offering potential as therapeutic agents with fewer side effects.

Area of Science:

  • Molecular Biology
  • Cell Biology
  • Pharmacology

Background:

  • Retinoids are crucial for biological processes like cell differentiation and proliferation.
  • Their therapeutic use is limited by significant side effects.
  • Retinoid action is mediated by nuclear receptors (RARs and RXRs) and AP-1 inhibition.

Purpose of the Study:

  • To identify conformationally restricted retinoids with selective receptor actions.
  • To develop novel retinoid agents with a potentially improved side effect profile.

Main Methods:

  • Investigated the distinct mechanisms of retinoid receptor actions.
  • Developed and characterized a new class of retinoids.
  • Assessed retinoid effects on AP-1 activity, transcriptional activation, F9 cell differentiation, and tumor cell proliferation.

Main Results:

  • Identified novel retinoids that selectively inhibit AP-1 activity.
  • These retinoids do not activate transcription.
  • Demonstrated inhibition of tumor cell proliferation without inducing F9 cell differentiation.

Conclusions:

  • A new class of retinoids selectively targets AP-1 signaling.
  • These compounds show promise for cancer therapy with potentially reduced side effects.
  • Further development could lead to novel therapeutic agents for various conditions.

More Related Videos

Y-27632 Enriches the Yield of Human Melanocytes from Adult Skin Tissues08:06

Y-27632 Enriches the Yield of Human Melanocytes from Adult Skin Tissues

Published on: July 8, 2020

Quantitative Analysis of Dietary Vitamin A Metabolites in Murine Ocular and Non-Ocular Tissues Using High-Performance Liquid Chromatography05:03

Quantitative Analysis of Dietary Vitamin A Metabolites in Murine Ocular and Non-Ocular Tissues Using High-Performance Liquid Chromatography

Published on: December 27, 2024

Related Concept Videos

Negative Regulator Molecules01:23

Negative Regulator Molecules

Positive regulators allow a cell to advance through cell cycle checkpoints. Negative regulators have an equally important role as they terminate a cell’s progression through the cell cycle—or pause it—until the cell meets specific criteria.
Inhibition of Cdk Activity02:34

Inhibition of Cdk Activity

The orderly progression of the cell cycle depends on the activation of Cdk protein by binding to its cyclin partner. However, the cell cycle must be restricted when undergoing abnormal changes. Most cancers correlate to the deregulated cell cycle, and since Cdks are a central component of the cell cycle, Cdk inhibitors are extensively studied to develop anticancer agents. For instance, cyclin D associates with several Cdks, such as Cdk 4/6, to form an active complex. The cyclin D-Cdk4/6 complex...
Abnormal Proliferation02:23

Abnormal Proliferation

Under normal conditions, most adult cells remain in a non-proliferative state unless stimulated by internal or external factors to replace lost cells. Abnormal cell proliferation is a condition in which the cell's growth exceeds and is uncoordinated with normal cells. In such situations, cell division persists in the same excessive manner even after cessation of the stimuli, leading to persistent tumors. The tumor arises from the damaged cells that replicate to pass the damage to the daughter...
The Retinoblastoma Gene01:20

The Retinoblastoma Gene

Tumor suppressor genes are normal genes that can slow down cell division, repair DNA mistakes, or program the cells for apoptosis in case of irreparable damage. Hence, they play an essential role in preventing the proliferation of damaged cells.
The first-ever tumor suppressor gene called Rb was identified in retinoblastoma - a rare eye tumor in children. In inherited forms of the disease, a child inherits one defective copy of the Rb gene, which predisposes them to retinoblastoma. However,...
Inhibition of CDK Activity02:34

Inhibition of CDK Activity

The orderly progression of the cell cycle depends on the activation of Cdk protein by binding to its cyclin partner. However, the cell cycle must be restricted when undergoing abnormal changes. Most cancers correlate to the deregulated cell cycle, and since Cdks are a central component of the cell cycle, Cdk inhibitors are extensively studied to develop anticancer agents. For instance, cyclin D associates with several Cdks, such as Cdk 4/6, to form an active complex. The cyclin D-Cdk4/6 complex...
The Retinoblastoma Gene01:20

The Retinoblastoma Gene

Tumor suppressor genes are normal genes that can slow down cell division, repair DNA mistakes, or program the cells for apoptosis in case of irreparable damage. Hence, they play an essential role in preventing the proliferation of damaged cells.
The first-ever tumor suppressor gene called Rb was identified in retinoblastoma - a rare eye tumor in children. In inherited forms of the disease, a child inherits one defective copy of the Rb gene, which predisposes them to retinoblastoma. However,...