Related Experiment Video
Updated: May 20, 2026

Reverse Yeast Two-hybrid System to Identify Mammalian Nuclear Receptor Residues that Interact with Ligands and/or Antagonists
Published on: November 15, 2013
Exploration of a new drug that targets YAP
1Division of Molecular Oncology, Aichi Cancer Center Research Institute, 1-1 Kanokoden, Chikusa-ku, Nagoya, Aichi 464-8681, Japan. fujiim@aichi-cc.jp
Abstract:
Yes-associated protein (YAP) has been shown to play a critical role in the growth of various tumours. Phosphorylation of Ser127 of YAP leads to the inhibition of YAP translocation into nucleus and subsequent failure to regulate the expression of target genes that induce cell proliferation. Chemical manipulation of YAP localization or expression may provide an efficient method for cancer treatment. In a recent work published by Bao et al. (J. Biochem. 2011;150:199-208), various compounds were screened in human osteosarcoma cells that stably express Green Fluorescent Protein-labeled YAP by monitoring subcellular localization of GFP-YAP. Using this cell-based assay, they found that dobutamine, a β-adrenergic receptor agonist, attenuated YAP-dependent transcription by inhibiting its nuclear translocation. The authors suggest dobutamine as a possible drug for cancer treatment.
Insights
Dobutamine, a drug, was found to inhibit the growth of tumors by blocking the Yes-associated protein (YAP) from entering the cell nucleus. This discovery offers a potential new cancer treatment strategy.
Area of Science:
- Oncology
- Molecular Biology
- Pharmacology
Background:
- Yes-associated protein (YAP) is crucial for tumor growth.
- YAP nuclear translocation regulates genes for cell proliferation.
- Inhibiting YAP nuclear entry is a potential cancer therapy.
Purpose of the Study:
- To identify compounds that modulate YAP localization.
- To explore novel cancer treatment strategies targeting YAP.
Main Methods:
- Screening of compounds using human osteosarcoma cells expressing Green Fluorescent Protein-labeled YAP (GFP-YAP).
- Monitoring subcellular localization of GFP-YAP to assess compound effects.
- Utilizing a cell-based assay to evaluate YAP-dependent transcription.
Main Results:
- Dobutamine, a beta-adrenergic receptor agonist, was identified as an inhibitor of YAP.
- Dobutamine attenuated YAP-dependent transcription by preventing nuclear translocation.
- The study demonstrated dobutamine's effect on YAP in a cellular model.
Conclusions:
- Dobutamine shows potential as a therapeutic agent for cancer treatment.
- Targeting YAP nuclear translocation is a viable strategy for inhibiting tumor growth.
- Further research into dobutamine's anti-cancer properties is warranted.
Related Concept Videos
Drug Discovery: Overview
Pharmacogenomics: Identification of New Drug Targets
Targets for Drug Action: Overview
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...
Structure-Activity Relationships and Drug Design
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 its...
Drug Regulation
Drug-Receptor Interaction: Agonist
Agonists can bind to receptors in different ways. Some agonists bind directly to the receptor's active site, mimicking the endogenous ligand's action.
