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 …
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 …
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
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 …
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
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+ …
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 …
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 …
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 …
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 …
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 …
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 …
only a few activating ERBB4 mutations have been characterized, primarily due to lack of …