Comprehensive mutational scanning of EGFR reveals TKI sensitivities of extracellular domain mutants

TK Hayes, E Aquilanti, NS Persky, X Yang… - nature …, 2024 - nature.com
The epidermal growth factor receptor, EGFR, is frequently activated in lung cancer and
glioblastoma by genomic alterations including missense mutations. The different mutation …

[HTML][HTML] Defining the sensitivity landscape of EGFR variants to tyrosine kinase inhibitors

LEI An, Y Wang, G Wu, Z Wang, Z Shi, C Liu… - Translational …, 2023 - Elsevier
Tyrosine kinase inhibitor (TKI) is a standard treatment for patients with NSCLC harboring
constitutively active epidermal growth factor receptor (EGFR) mutations. However, most rare …

Drug-resistant EGFR mutations promote lung cancer by stabilizing interfaces in ligand-free kinase-active EGFR oligomers

RS Iyer, SR Needham, I Galdadas, BM Davis… - Nature …, 2024 - nature.com
Abstract The Epidermal Growth Factor Receptor (EGFR) is frequently found to be mutated in
non-small cell lung cancer. Oncogenic EGFR has been successfully targeted by tyrosine …

DUSP6 inhibition overcomes neuregulin/HER3-driven therapy tolerance in HER2+ breast cancer

M Momeny, M Tienhaara, M Sharma… - EMBO Molecular …, 2024 - embopress.org
Despite clinical benefits of tyrosine kinase inhibitors (TKIs) in cancer, most tumors can
reactivate proliferation under TKI therapy. Here we present transcriptional profiling of HER2+ …

Trans-activating mutations of the pseudokinase ERBB3

MKA Koivu, D Chakroborty, TT Airenne, MS Johnson… - Oncogene, 2024 - nature.com
Genetic changes in the ERBB family of receptor tyrosine kinases serve as oncogenic driver
events and predictive biomarkers for ERBB inhibitor drugs. ERBB3 is a pseudokinase …

Mutational screens highlight glycosylation as a modulator of colony-stimulating factor 3 receptor (CSF3R) activity

MJ Hollander, SA Malaker, NM Riley, I Perez… - Journal of Biological …, 2023 - ASBMB
The colony-stimulating factor 3 receptor (CSF3R) controls the growth of neutrophils, the most
abundant type of white blood cell. In healthy neutrophils, signaling is dependent on CSF3R …

Saturation resistance profiling of EGFR variants against tyrosine kinase inhibitors using prime editing

Y Kim, HC Oh, S Lee, HH Kim - bioRxiv, 2023 - biorxiv.org
Variants of uncertain significance (VUS) hamper the clinical application of genetic
information. For example, in treating lung cancer with tyrosine kinase inhibitors (TKIs), many …

Identification of Predictive ERBB Mutations by Leveraging Publicly Available Cell Line Databases

MKA Koivu, D Chakroborty, MZ Tamirat… - Molecular cancer …, 2021 - AACR
Although targeted therapies can be effective for a subgroup of patients, identification of
individuals who benefit from the treatments is challenging. At the same time, the predictive …

[PDF][PDF] The T766M-EGFR lung cancer mutation promotes tumor growth by exploiting newfound assembly mechanisms in ligand-free EGFR oligomers

RS Iyer, SR Needham, I Galdadas, BM Davis… - bioRxiv, 2023 - academia.edu
Epidermal growth factor receptor (EGFR) is central to cell growth in physiology and
pathophysiologies, including non-small cell lung cancer (NSCLC). EGFR has been …

An unbiased functional genetics screen identifies rare activating ERBB4 mutations

D Chakroborty, VK Ojala, AM Knittle, J Drexler… - Cancer Research …, 2022 - AACR
Despite the relatively high frequency of somatic ERBB4 mutations in various cancer types,
only a few activating ERBB4 mutations have been characterized, primarily due to lack of …