Targeted inhibitors of EGFR: structure, biology, biomarkers, and clinical applications

N Shaban, D Kamashev, A Emelianova, A Buzdin - Cells, 2023 - mdpi.com
Members of the EGFR family of tyrosine kinase receptors are major regulators of cellular
proliferation, differentiation, and survival. In humans, abnormal activation of EGFR is …

Understanding resistance to EGFR inhibitors—impact on future treatment strategies

DL Wheeler, EF Dunn, PM Harari - Nature reviews Clinical oncology, 2010 - nature.com
EGFR is a tyrosine kinase that participates in the regulation of cellular homeostasis.
Following ligand binding, EGFR stimulates downstream cell signaling cascades that …

Mechanisms of resistance to EGFR targeted therapies

G Hrustanovic, BJ Lee, TG Bivona - Cancer biology & therapy, 2013 - Taylor & Francis
EGFR is a validated therapeutic target in many human cancers. EGFR targeted therapies
are in widespread clinical use in patients with non-small cell lung cancer and other tumor …

Heterogeneous mechanisms of primary and acquired resistance to third-generation EGFR inhibitors

S Ortiz-Cuaran, M Scheffler, D Plenker, L Dahmen… - Clinical Cancer …, 2016 - AACR
Purpose: To identify novel mechanisms of resistance to third-generation EGFR inhibitors in
patients with lung adenocarcinoma that progressed under therapy with either AZD9291 or …

Targeting the EGFR signaling pathway in cancer therapy

P Seshacharyulu, MP Ponnusamy… - Expert opinion on …, 2012 - Taylor & Francis
Introduction: Cancer is a devastating disease; however, several therapeutic advances have
recently been made, wherein EGFR and its family members have emerged as useful …

Strategies to overcome acquired resistances conferred by mutations in the kinase domain of EGFR

SM Lim, Y Jeong, S Hong - Future Medicinal Chemistry, 2016 - Taylor & Francis
Deregulation of EGFR is involved in the development of many cancers. The inhibition of
EGFR kinase activity has been clinically validated as a promising approach for the treatment …

Rethink of EGFR in cancer with its kinase independent function on board

R Thomas, Z Weihua - Frontiers in oncology, 2019 - frontiersin.org
The epidermal growth factor receptor (EGFR) is one of most potent oncogenes that are
commonly altered in cancers. As a receptor tyrosine kinase, EGFR's kinase activity has been …

Mechanisms of tumor resistance to EGFR-targeted therapies

EA Hopper-Borge, RE Nasto, V Ratushny… - Expert opinion on …, 2009 - Taylor & Francis
Background: Much effort has been devoted to development of cancer therapies targeting
EGFR, based on its role in regulating cell growth. Small-molecule and antibody EGFR …

Mechanisms of resistance to EGFR inhibitors

R Bianco, T Gelardi, V Damiano, F Ciardiello… - Targeted Oncology, 2007 - Springer
The epidermal growth factor receptor (EGFR) autocrine pathway plays a crucial role in
human cancer, contributing to a number of highly relevant processes in tumor development …

A third shot at EGFR: new opportunities in cancer therapy

S Guardiola, M Varese, M Sanchez-Navarro… - Trends in …, 2019 - cell.com
Epidermal growth factor receptor (EGFR) inhibitors were among the first type of targeted
agents discovered in cancer and currently constitute the standard of care for a wide range of …