ErbB/HER protein-tyrosine kinases: Structures and small molecule inhibitors

R Roskoski Jr - Pharmacological research, 2014 - Elsevier
The epidermal growth factor receptor (EGFR) family consists of four members that belong to
the ErbB lineage of proteins (ErbB1–4). These receptors consist of an extracellular domain …

The ErbB/HER family of protein-tyrosine kinases and cancer

R Roskoski Jr - Pharmacological research, 2014 - Elsevier
The human epidermal growth factor receptor (EGFR) family consists of four members that
belong to the ErbB lineage of proteins (ErbB1–4). These receptors consist of a glycosylated …

The ErbB/HER receptor protein-tyrosine kinases and cancer

R Roskoski Jr - Biochemical and biophysical research communications, 2004 - Elsevier
The ErbB/HER protein-tyrosine kinases, which include the epidermal growth factor receptor,
consist of a growth-factor-binding ectodomain, a single transmembrane segment, an …

Small molecule inhibitors targeting the EGFR/ErbB family of protein-tyrosine kinases in human cancers

R Roskoski Jr - Pharmacological research, 2019 - Elsevier
The EGFR family is among the most investigated receptor protein-tyrosine kinase groups
owing to its general role in signal transduction and in oncogenesis. This family consists of …

Structure-based design of a potent, selective, and irreversible inhibitor of the catalytic domain of the erbB receptor subfamily of protein tyrosine kinases

J Singh, EM Dobrusin, DW Fry, T Haske… - Journal of medicinal …, 1997 - ACS Publications
We report the use of structure-based drug design to create a selective erbB-1 (aka
epidermal growth factor receptor) and erbB-2 (aka neu/her2 growth factor receptor) tyrosine …

Targeting EGFR and HER‐2 receptor tyrosine kinases for cancer drug discovery and development

S Kamath, JK Buolamwini - Medicinal research reviews, 2006 - Wiley Online Library
Conventional anticancer therapy using cytotoxic drugs lacks selectivity and is prone to
toxicity and drug resistance. Anticancer therapies targeting aberrant growth factor receptor …

Epidermal growth factor receptor: mechanisms of activation and signalling

RN Jorissen, F Walker, N Pouliot, TPJ Garrett… - The EGF receptor …, 2003 - Elsevier
Publisher Summary This chapter discusses the structure and function of the epidermal
growth factor (EGF) receptor (EGFR), from ligand binding to the initiation of intracellular …

All EGF (ErbB) receptors have preformed homo-and heterodimeric structures in living cells

RH Tao, IN Maruyama - Journal of cell science, 2008 - journals.biologists.com
The epidermal growth factor receptor (EGFR) family of receptor tyrosine kinases, also known
as ErbB or HER, plays crucial roles in the development of multicellular organisms. Mutations …

An open-and-shut case? Recent insights into the activation of EGF/ErbB receptors

AW Burgess, HS Cho, C Eigenbrot, KM Ferguson… - Molecular cell, 2003 - cell.com
Recent crystallographic studies have provided significant new insight into how receptor
tyrosine kinases from the EGF receptor or ErbB family are regulated by their growth factor …

[HTML][HTML] The ErbB signaling network: receptor heterodimerization in development and cancer

MA Olayioye, RM Neve, HA Lane, NE Hynes - The EMBO journal, 2000 - embopress.org
Cells are continuously exposed to diverse stimuli ranging from soluble endocrine and
paracrine factors, to signaling molecules on neighboring cells. It is of great importance that …