Related Experiment Video

Updated: Feb 9, 2026

Assessing Cellular Target Engagement by SHP2 PTPN11 Phosphatase Inhibitors
08:45

Assessing Cellular Target Engagement by SHP2 PTPN11 Phosphatase Inhibitors

Published on: July 17, 2020

6.6K

Targeting phosphatases of regenerating liver (PRLs) in cancer

Min Wei1, Konstantin V Korotkov1, Jessica S Blackburn1

  • 1Department of Molecular and Cellular Biochemistry, University of Kentucky, Lexington, KY, United States.

Pharmacology & Therapeutics
|June 3, 2018
PubMed

Insights

Phosphatase of regenerating liver (PRL) proteins are oncogenic and highly expressed in advanced cancers. Developing specific PRL inhibitors for cancer therapy is challenging but crucial for future drug development.

Area of Science:

  • Biochemistry
  • Molecular Biology
  • Oncology

Background:

  • The phosphatase of regenerating liver (PRL) family, also known as protein tyrosine phosphatase 4A (PTP4A), are dual-specificity phosphatases.
  • Accumulating evidence indicates that PRLs are oncogenic across a broad variety of human cancers, with high expression correlating with poor prognosis.

Purpose of the Study:

  • To review current PRL inhibitors, including strategies for their identification.
  • To discuss their biological efficacy, potency, and selectivity.
  • To highlight how PRL structure can inform future inhibitor development.

Main Methods:

  • Literature review of current PRL inhibitors.
  • Analysis of strategies for inhibitor identification.
  • Evaluation of biological efficacy, potency, and selectivity data.

Main Results:

  • PRLs are highly expressed in advanced tumors and metastases.
  • Targeting PRLs with small molecules is challenging due to conserved active sites and sequence similarity.
  • Current PRL inhibitors vary in efficacy, potency, and selectivity.

Conclusions:

  • PRLs are promising therapeutic targets in cancer due to their oncogenic roles.
  • Overcoming challenges in developing specific PRL inhibitors is essential for cancer drug development.
  • Understanding PRL structure is key to designing more effective and selective inhibitors.
Keywords:
MetastasisProtein tyrosine phosphataseStructureTheinopyridone

More Related Videos

A Hepatocellular Cancer Patient-Derived Organoid Xenograft Model to Investigate Impact of Liver Regeneration on Tumor Growth08:15

A Hepatocellular Cancer Patient-Derived Organoid Xenograft Model to Investigate Impact of Liver Regeneration on Tumor Growth

Published on: February 2, 2024

1.5K
Three-Dimensional Collagen Matrix Scaffold Implantation as a Liver Regeneration Strategy05:20

Three-Dimensional Collagen Matrix Scaffold Implantation as a Liver Regeneration Strategy

Published on: June 29, 2021

3.5K

Related Concept Videos

Liver Regeneration01:24

Liver Regeneration

The liver is an important organ in vertebrates that plays an essential role in metabolism. It is also responsible for storing and redistributing nutrients such as carbohydrates, fats, and vitamins in the body. Additionally, the liver releases bile salts which are critical for digesting food and eliminating toxic metabolites from the body.
Cells of Liver
The liver comprises four major types of cells— hepatocytes, stellate, Kupffer, and sinusoidal endothelial cells. The hepatocytes are...
4.4K
Protein Kinases and Phosphatases02:54

Protein Kinases and Phosphatases

Proteins undergo chemical modifications that trigger changes in the charge, structure, and conformation of the proteins. Phosphorylation, acetylation, glycosylation, nitrosylation, ubiquitination, lipidation, methylation, and proteolysis are various protein modifications that regulate protein activity. Such modifications are usually enzyme-driven.
Protein kinases
Many proteins in the cell are regulated by phosphorylation, the addition of a phosphate group. A family of enzymes called kinases...
15.2K
Protein Kinases and Phosphatases02:54

Protein Kinases and Phosphatases

4.5K
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
Whole Body Regeneration01:33

Whole Body Regeneration

Regeneration is the process of restoring injured or lost tissues, organs, or body parts. While simpler organisms generally show greater ability to regenerate their whole body, few complex animals show similarly exceptional regeneration. For example, planarian flatworms have a unique regenerative potential making them a popular study organism among biologists to understand the mechanisms of whole body regeneration. Other organisms, such as hydra, also show extreme regeneration potential;...
4.2K
Overview of Regeneration and Repair01:19

Overview of Regeneration and Repair

Regeneration and repair processes are critical in healing damages caused by injury, disease, and aging. In regeneration, the damaged tissue is entirely replaced with new growth that restores the original architecture and function. In contrast, tissue repair usually results in a fixed tissue architecture involving scar formation. Scars generally do not reestablish tissue function and may also exhibit structural abnormalities at the injury site.
Regeneration
All animals have varying degrees of...
5.2K