Challenges and opportunities in cancer drug resistance

RA Ward, S Fawell, N Floc'h, V Flemington… - Chemical …, 2020 - ACS Publications
There has been huge progress in the discovery of targeted cancer therapies in recent years.
However, even for the most successful and impactful cancer drugs which have been …

Rational, biologically based treatment of EGFR-mutant non-small-cell lung cancer

W Pao, J Chmielecki - Nature Reviews Cancer, 2010 - nature.com
Epidermal growth factor receptor (EGFR)-mutant non-small-cell lung cancer (NSCLC) was
first recognized in 2004 as a distinct, clinically relevant molecular subset of lung cancer. The …

The allelic context of the C797S mutation acquired upon treatment with third-generation EGFR inhibitors impacts sensitivity to subsequent treatment strategies

MJ Niederst, H Hu, HE Mulvey, EL Lockerman… - Clinical Cancer …, 2015 - AACR
Purpose: A secondary EGFR mutation, T790M, is the most common resistance mechanism
in EGFR-mutant adenocarcinomas that have progressed on erlotinib. Third-generation …

Heterogeneity Underlies the Emergence of EGFRT790 Wild-Type Clones Following Treatment of T790M-Positive Cancers with a Third-Generation EGFR Inhibitor

Z Piotrowska, MJ Niederst, CA Karlovich, HA Wakelee… - Cancer discovery, 2015 - AACR
Rociletinib is a third-generation EGFR inhibitor active in lung cancers with T790M, the
gatekeeper mutation underlying most first-generation EGFR drug resistance. We biopsied …

Acquired EGFR C797S mutation mediates resistance to AZD9291 in non–small cell lung cancer harboring EGFR T790M

KS Thress, CP Paweletz, E Felip, BC Cho, D Stetson… - Nature medicine, 2015 - nature.com
Here we studied cell-free plasma DNA (cfDNA) collected from subjects with advanced lung
cancer whose tumors had developed resistance to the epidermal growth factor receptor …

Molecular hybrids: A five-year survey on structures of multiple targeted hybrids of protein kinase inhibitors for cancer therapy

OM Soltan, ME Shoman, SA Abdel-Aziz… - European Journal of …, 2021 - Elsevier
Protein kinases have grown over the past few years as a crucial target for different cancer
types. With the multifactorial nature of cancer, and the fast development of drug resistance …

Emerging paradigms in the development of resistance to tyrosine kinase inhibitors in lung cancer

JF Gainor, AT Shaw - Journal of clinical oncology, 2013 - ascopubs.org
The success of tyrosine kinase inhibitors (TKIs) in select patients with non–small-cell lung
cancer (NSCLC) has transformed management of the disease, placing new emphasis on …

Structural insight and development of EGFR tyrosine kinase inhibitors

T Amelia, RE Kartasasmita, T Ohwada, DH Tjahjono - Molecules, 2022 - mdpi.com
Lung cancer has a high prevalence, with a growing number of new cases and mortality
every year. Furthermore, the survival rate of patients with non-small-cell lung carcinoma …

The significance of epidermal growth factor receptor uncommon mutations in non-small cell lung cancer: A systematic review and critical appraisal

V Gristina, U Malapelle, A Galvano, P Pisapia… - Cancer Treatment …, 2020 - Elsevier
Uncommon epidermal growth factor receptor (EGFR) mutations collectively account for 10%
of EGFR mutations, harboring heterogeneous molecular alterations within exons 18–21 with …

Acquired resistance to epidermal growth factor receptor tyrosine kinase inhibitors in non–small-cell lung cancers dependent on the epidermal growth factor receptor …

KSH Nguyen, S Kobayashi, DB Costa - Clinical lung cancer, 2009 - Elsevier
Abstract Most advanced Non–Small-cell lung cancers (NSCLCs) with activating epidermal
growth factor receptor (EGFR) mutations (exon 19 deletions or L858R) initially respond to …