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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 …
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 …
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
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 …
structures or functions that are difficult to interfere with using conventional drug design …
EGFR signaling pathway as therapeutic target in human cancers
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 …
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 …
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
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 …
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
Epidermal growth factor receptor (EGFR) therapy using small-molecule tyrosine kinase
inhibitors (TKIs) is initially efficacious in patients with EGFR-mutant lung cancer, although …
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 …
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
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 …
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 …
factor family, regulates cell proliferation and signal transduction; moreover, EGFR is related …