Journal Article

A Review of HER4 (ErbB4) Kinase, Its Impact on Cancer, and Its Inhibitors

Tarazi, Hamadeh, Sbenati, Rawan M., Shahin, Afnan I., Mewafi, Nada H., Zaraei, Seyed-Omar, Emara, Minnatullah A., El-Gamal, Mohammed I., Madkour, Moustafa M., Anbar, Hanan S., Abdelmotteleb, Nada E.

2021

Overview

HER4 is a receptor tyrosine kinase that is required for the evolution of normal body systems such as cardiovascular, nervous, and endocrine systems, especially the mammary glands. It is activated through ligand binding and activates MAPKs and PI3K/AKT pathways. HER4 is commonly expressed in many human tissues, both adult and fetal. It is important to understand the role of HER4 in the treatment of many disorders. Many studies were also conducted on the role of HER4 in tumors and its tumor suppressor function. Mostly, overexpression of HER4 kinase results in cancer development. In the present article, we reviewed the structure, location, ligands, physiological functions of HER4, and its relationship to different cancer types. HER4 inhibitors reported mainly from 2016 to the present were reviewed as well.

• Publisher: MDPI AG,MDPI
• Subject: Amino acids / Animals / Binding sites / Cancer / Cell division / Cloning / Epidermal growth factor / ErbB4 / HER4 / Humans / kinase inhibitors / Kinases / Ligands / Mutation / Neoplasms - drug therapy / Neoplasms - metabolism / Neoplasms - pathology / Phosphatidylinositol 3-Kinases - metabolism / Phosphorylation / Protein Kinase Inhibitors - pharmacology / Protein Kinase Inhibitors - therapeutic use / Proteins / Proto-Oncogene Proteins c-akt - metabolism / Receptor, ErbB-4 - analysis / Receptor, ErbB-4 - antagonists & inhibitors / Receptor, ErbB-4 - metabolism / Review / Signal transduction / Signal Transduction - drug effects / structure-activity relationship