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 …

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 EGFR inhibitors as anti-cancer agents: discovery, mechanisms of action, and opportunities

T Zubair, D Bandyopadhyay - International Journal of Molecular Sciences, 2023‏ - mdpi.com
Epidermal growth factor receptors (EGFRs) are a class of receptor tyrosine kinase that are
also called ErbB1 and HER1. EGFR tyrosine kinase activity inhibition is considered a …

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 …

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 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 …

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 - benthamdirect.com
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 …

Glioblastoma therapy: Past, present and future

E Obrador, P Moreno-Murciano… - International journal of …, 2024‏ - mdpi.com
Glioblastoma (GB) stands out as the most prevalent and lethal form of brain cancer.
Although great efforts have been made by clinicians and researchers, no significant …

[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 …

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 …