Thirty years of HER3: from basic biology to therapeutic interventions

HM Haikala, PA Jänne - Clinical Cancer Research, 2021 - AACR
HER3 is a pseudokinase member of the EGFR family having a role in both tumor
progression and drug resistance. Although HER3 was discovered more than 30 years ago …

Prospects for pharmacological targeting of pseudokinases

JE Kung, N Jura - Nature Reviews Drug Discovery, 2019 - nature.com
Pseudokinases are members of the protein kinase superfamily but signal primarily through
noncatalytic mechanisms. Many pseudokinases contribute to the pathologies of human …

There's more to death than life: Noncatalytic functions in kinase and pseudokinase signaling

PD Mace, JM Murphy - Journal of Biological Chemistry, 2021 - ASBMB
Protein kinases are present in all domains of life and play diverse roles in cellular signaling.
Whereas the impact of substrate phosphorylation by protein kinases has long been …

[HTML][HTML] Direct and indirect cholesterol effects on membrane proteins with special focus on potassium channels

F Zakany, T Kovacs, G Panyi, Z Varga - … BBA)-Molecular and Cell Biology of …, 2020 - Elsevier
As described in the literature the interaction between cholesterol and membrane proteins
can occur via direct, ligand-like and indirect mechanisms, in which cholesterol effects are …

Effects of HER family–targeting tyrosine kinase inhibitors on antibody-dependent cell-mediated cytotoxicity in HER2-expressing breast cancer

DM Collins, SF Madden, N Gaynor, D AlSultan… - Clinical Cancer …, 2021 - AACR
Purpose: Antibody-dependent cell-mediated cytotoxicity (ADCC) is one mechanism of action
of the monoclonal antibody (mAb) therapies trastuzumab and pertuzumab. Tyrosine kinase …

The root cause of drug resistance in HER2-positive breast cancer and the therapeutic approaches to overcoming the resistance

Y Zhang - Pharmacology & therapeutics, 2021 - Elsevier
HER2 is a well-known oncogenic receptor tyrosine kinase. HER2 gene amplification occurs
in about 20% of breast cancer (BC), which leads to overexpression of HER2 protein, known …

The architecture of EGFR's basal complexes reveals autoinhibition mechanisms in dimers and oligomers

LC Zanetti-Domingues, D Korovesis… - Nature …, 2018 - nature.com
Our current understanding of epidermal growth factor receptor (EGFR) autoinhibition is
based on X-ray structural data of monomer and dimer receptor fragments and does not …

Tracing the origin and evolution of pseudokinases across the tree of life

A Kwon, S Scott, R Taujale, W Yeung, KJ Kochut… - Science …, 2019 - science.org
Protein phosphorylation by eukaryotic protein kinases (ePKs) is a fundamental mechanism
of cell signaling in all organisms. In model vertebrates,~ 10% of ePKs are classified as …

Preclinical Characteristics of the Irreversible Pan-HER Kinase Inhibitor Neratinib Compared with Lapatinib: Implications for the Treatment of HER2-Positive and HER2 …

DM Collins, NT Conlon, S Kannan, CS Verma, LD Eli… - Cancers, 2019 - mdpi.com
An estimated 15–20% of breast cancers overexpress human epidermal growth factor
receptor 2 (HER2/ERBB2/neu). Two small-molecule tyrosine kinase inhibitors (TKIs) …

It takes more than two to tango: Complex, hierarchal, and membrane-modulated interactions in the regulation of receptor tyrosine kinases

T Kovacs, F Zakany, P Nagy - Cancers, 2022 - mdpi.com
Simple Summary Receptor tyrosine kinases probably constitute the most important
subfamily of transmembrane receptors with respect to their role in regulating the balance …