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 …

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 …

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 …

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 …

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 …

[HTML][HTML] Rare epidermal growth factor receptor (EGFR) mutations in non-small cell lung cancer

PT Harrison, S Vyse, PH Huang - Seminars in cancer biology, 2020 - Elsevier
Epidermal growth factor receptor (EGFR) mutations are the second most common oncogenic
driver event in non-small cell lung cancer (NSCLC). Classical activating mutations (exon 19 …

An allosteric inhibitor against the therapy-resistant mutant forms of EGFR in non-small cell lung cancer

C To, TS Beyett, J Jang, WW Feng, M Bahcall… - Nature cancer, 2022 - nature.com
Epidermal growth factor receptor (EGFR) therapy using small-molecule tyrosine kinase
inhibitors (TKIs) is initially efficacious in patients with EGFR-mutant lung cancer, although …

The ascension of targeted covalent inhibitors

J Singh - Journal of Medicinal Chemistry, 2022 - ACS Publications
Covalent drugs have made a major impact on human health but until recently were shunned
by the pharmaceutical industry over concerns about the potential for toxicity. A resurgence …

[PDF][PDF] Review on epidermal growth factor receptor (EGFR) structure, signaling pathways, interactions, and recent updates of EGFR inhibitors

DA Sabbah, R Hajjo, K Sweidan - Current topics in medicinal …, 2020 - researchgate.net
The epidermal growth factor receptor (EGFR) belongs to the ERBB family of tyrosine kinase
receptors. EGFR signaling cascade is a key regulator in cell proliferation, differentiation …

Emerging strategies to overcome resistance to third-generation EGFR inhibitors

K Shi, G Wang, J Pei, J Zhang, J Wang… - Journal of Hematology & …, 2022 - Springer
Epidermal growth factor receptor (EGFR), the receptor for members of the epidermal growth
factor family, regulates cell proliferation and signal transduction; moreover, EGFR is related …