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 …

ERBB receptors: from oncogene discovery to basic science to mechanism-based cancer therapeutics

CL Arteaga, JA Engelman - Cancer cell, 2014 - cell.com
ERBB receptors were linked to human cancer pathogenesis approximately three decades
ago. Biomedical investigators have since developed substantial understanding of the …

Antitumour immunity regulated by aberrant ERBB family signalling

S Kumagai, S Koyama, H Nishikawa - Nature Reviews Cancer, 2021 - nature.com
Aberrant signalling of ERBB family members plays an important role in tumorigenesis and in
the escape from antitumour immunity in multiple malignancies. Molecular-targeted agents …

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 …

Perturbation-response genes reveal signaling footprints in cancer gene expression

M Schubert, B Klinger, M Klünemann, A Sieber… - Nature …, 2018 - nature.com
Aberrant cell signaling can cause cancer and other diseases and is a focal point of drug
research. A common approach is to infer signaling activity of pathways from gene …

Mechanisms of resistance to trastuzumab emtansine (T-DM1) in HER2-positive breast cancer

FW Hunter, HR Barker, B Lipert, F Rothé… - British journal of …, 2020 - nature.com
The HER2-targeted antibody–drug conjugate trastuzumab emtansine (T-DM1) is approved
for the treatment of metastatic, HER2-positive breast cancer after prior trastuzumab and …

Designed ankyrin repeat proteins (DARPins): binding proteins for research, diagnostics, and therapy

A Plückthun - Annual review of pharmacology and toxicology, 2015 - annualreviews.org
Designed ankyrin repeat proteins (DARPins) can recognize targets with specificities and
affinities that equal or surpass those of antibodies, but because of their robustness and …

Preclinical activity of HER2-selective tyrosine kinase inhibitor tucatinib as a single agent or in combination with trastuzumab or docetaxel in solid tumor models

A Kulukian, P Lee, J Taylor, R Rosler, P de Vries… - Molecular Cancer …, 2020 - AACR
HER2 is a transmembrane tyrosine kinase receptor that mediates cell growth, differentiation,
and survival. HER2 is overexpressed in approximately 20% of breast cancers and in subsets …

Trastuzumab mechanism of action; 20 years of research to unravel a dilemma

H Maadi, MH Soheilifar, WS Choi, A Moshtaghian… - Cancers, 2021 - mdpi.com
Simple Summary Overexpression of HER2 receptors have been identified in various types of
cancer including breast cancer and ovarian cancer. HER2 overexpression is generally …

Resistance mechanisms to anti-HER2 therapies in HER2-positive breast cancer: Current knowledge, new research directions and therapeutic perspectives

C Vernieri, M Milano, M Brambilla, A Mennitto… - Critical reviews in …, 2019 - Elsevier
HER2-positive breast cancer (HER2+ BC) represents 15–20% of all BCs. In the last two
decades, the introduction of monoclonal antibodies (MoAbs), tyrosine kinase inhibitors …