Advances in covalent drug discovery

L Boike, NJ Henning, DK Nomura - Nature Reviews Drug Discovery, 2022 - nature.com
Covalent drugs have been used to treat diseases for more than a century, but tools that
facilitate the rational design of covalent drugs have emerged more recently. The purposeful …

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 …

Therapeutic strategies for EGFR-mutated non-small cell lung cancer patients with osimertinib resistance

K Fu, F **e, F Wang, L Fu - Journal of Hematology & Oncology, 2022 - Springer
Epidermal growth factor receptor tyrosine kinase inhibitors (EGFR-TKIs) are the preferential
options for advanced non-small cell lung cancer (NSCLC) patients harboring EGFR …

Small-molecule inhibitors, immune checkpoint inhibitors, and more: FDA-approved novel therapeutic drugs for solid tumors from 1991 to 2021

Q Wu, W Qian, X Sun, S Jiang - Journal of hematology & oncology, 2022 - Springer
Abstract The United States Food and Drug Administration (US FDA) has always been a
forerunner in drug evaluation and supervision. Over the past 31 years, 1050 drugs …

Overcoming therapy resistance in EGFR-mutant lung cancer

A Passaro, PA Jänne, T Mok, S Peters - Nature Cancer, 2021 - nature.com
Tyrosine kinase inhibitors (TKIs) have dramatically changed the clinical prospects of patients
with non-small cell lung cancer harboring epidermal growth factor receptor (EGFR) …

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

X **e, 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 …

Proteogenomic characterization reveals therapeutic vulnerabilities in lung adenocarcinoma

MA Gillette, S Satpathy, S Cao, SM Dhanasekaran… - Cell, 2020 - cell.com
To explore the biology of lung adenocarcinoma (LUAD) and identify new therapeutic
opportunities, we performed comprehensive proteogenomic characterization of 110 tumors …

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 …