Third-generation EGFR and ALK inhibitors: mechanisms of resistance and management

AJ Cooper, LV Sequist, JJ Lin - Nature Reviews Clinical Oncology, 2022 - nature.com
The discoveries of EGFR mutations and ALK rearrangements as actionable oncogenic
drivers in non-small-cell lung cancer (NSCLC) has propelled a biomarker-directed treatment …

Kinase drug discovery 20 years after imatinib: progress and future directions

P Cohen, D Cross, PA Jänne - Nature reviews drug discovery, 2021 - nature.com
Protein kinases regulate nearly all aspects of cell life, and alterations in their expression, or
mutations in their genes, cause cancer and other diseases. Here, we review the remarkable …

Amivantamab in EGFR exon 20 insertion–mutated non–small-cell lung cancer progressing on platinum chemotherapy: initial results from the CHRYSALIS phase I …

K Park, EB Haura, NB Leighl, P Mitchell… - Journal of Clinical …, 2021 - ascopubs.org
PURPOSE Non–small-cell lung cancer (NSCLC) with epidermal growth factor receptor
(EGFR) exon 20 insertion (Exon20ins) mutations exhibits inherent resistance to approved …

RAS-targeted therapies: is the undruggable drugged?

AR Moore, SC Rosenberg, F McCormick… - Nature reviews Drug …, 2020 - nature.com
Abstract RAS (KRAS, NRAS and HRAS) is the most frequently mutated gene family in
cancers, and, consequently, investigators have sought an effective RAS inhibitor for more …

Small molecule kinase inhibitor drugs (1995–2021): medical indication, pharmacology, and synthesis

CC Ayala-Aguilera, T Valero… - Journal of Medicinal …, 2021 - ACS Publications
The central role of dysregulated kinase activity in the etiology of progressive disorders,
including cancer, has fostered incremental efforts on drug discovery programs over the past …

EGFR in cancer: Signaling mechanisms, drugs, and acquired resistance

ML Uribe, I Marrocco, Y Yarden - Cancers, 2021 - mdpi.com
Simple Summary Growth factors are hormone-like molecules able to promote division and
migration of normal cells, but cancer captured the underlying mechanisms to unleash tumor …

Recent advances in targeting the “undruggable” proteins: from drug discovery to clinical trials

X Xie, T Yu, X Li, N Zhang, LJ Foster, C Peng… - Signal transduction and …, 2023 - nature.com
Undruggable proteins are a class of proteins that are often characterized by large, complex
structures or functions that are difficult to interfere with using conventional drug design …

EGFR signaling pathway as therapeutic target in human cancers

E Levantini, G Maroni, M Del Re, DG Tenen - Seminars in cancer biology, 2022 - Elsevier
Abstract Epidermal Growth Factor Receptor (EGFR) enacts major roles in the maintenance
of epithelial tissues. However, when EGFR signaling is altered, it becomes the grand …

The emerging treatment landscape of targeted therapy in non-small-cell lung cancer

M Yuan, LL Huang, JH Chen, J Wu, Q Xu - Signal transduction and …, 2019 - nature.com
Lung cancer is one of the most common cancer in the world. In 2018, there were over 2
million new cases of lung cancer and over 1.7 million deaths were attributed to lung cancer …

Current approaches to the management of brain metastases

JH Suh, R Kotecha, ST Chao, MS Ahluwalia… - Nature reviews Clinical …, 2020 - nature.com
Brain metastases are a very common manifestation of cancer that have historically been
approached as a single disease entity given the uniform association with poor clinical …