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

By Carlos L. Arteaga, J. Engelman. 2014

952 citations recorded by the source corpus.

Summary ERBB receptors were linked to human cancer pathogenesis approximately three decades ago. Biomedical investigators have since developed substantial understanding of the biology underlying the dependence of cancers on aberrant ERBB receptor signaling. An array of cancer-associated genetic alterations in ERBB receptors has also been identified. These findings have led to the discovery and development of mechanism-based therapies targeting ERBB receptors that have improved outcome for many cancer patients. In this Perspective, we discuss current paradigms of targeting ERBB receptors with cancer therapeutics and our understanding of mechanisms of action and resistance to these drugs. As current strategies still have limitations, we also discuss challenges and opportunities that lie ahead as basic scientists and clinical investigators work toward more breakthroughs.

Subfields: Molecular Biology, Radiology, Nuclear Medicine and Imaging

How researchers see this paper

The researchers whose trusted networks rank it highest, strongest advocate first. Every researcher gets a different order.

In Molecular Biology

1. A. Hanker
2. D. Sudhan
3. Jens Timmer
4. Carlos L. Arteaga
5. Birgit Schoeberl
6. G. MacBeath

In Radiology, Nuclear Medicine and Imaging

1. A. Hanker
2. D. Sudhan
3. Carlos L. Arteaga
4. Birgit Schoeberl

Citations in the corpus

• Predicting ligand-dependent tumors from multi-dimensional signaling features (2017, background): “This coincides with prior biological knowledge that ErbB receptors induce proliferation.(13) It can be observed that EGF, HGF or HRG stimulation induce very specific homo and heterodimerization patterns of EGFR and EGFR/ HER2 respectively.”
• Overcoming Endocrine Resistance in Breast Cancer (2020, positive): “, 2016), 2) target-independent activation of downstream or bypass signaling pathways (ie, RTK, PI3K, and MAPK pathway deregulation) (Arteaga and Engelman, 2014; Cocco et al., 2019; Hazar-Rethinam et al., 2018; Shi et al., 2014), and 3) microenvironmental components that affect drug sensitivity (Hira”
• Breast cancer development and progression: Risk factors, cancer stem cells, signaling pathways, genomics, and molecular pathogenesis (2018, background): “Novel mechanisms underlying the relationship between HER2 and breast cancer have been uncovered recently.(105,116) While the interplay of HER2 and ERs has long been recognized,(102) it was recently discovered that a new intermediary factor MED1 has significant impact on HER2-driven tumorigenesis.”