Title |
In silico identification of EGFR-T790M inhibitors with novel scaffolds: start with extraction of common features
|
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Published in |
Drug Design, Development and Therapy, August 2013
|
DOI | 10.2147/dddt.s41305 |
Pubmed ID | |
Authors |
Mingli Xiang, Kai Lei, Wenjie Fan, Yuchun Lin, Gu He, Mingli Yang, Lijuan Chen, Yirong Mo |
Abstract |
Epidermal growth factor receptor (EGFR) is an attractive therapeutic target for a number of human tumors including non-small cell lung cancer (NSCLC). Most patients with NSCLC and somatic mutations have shown a dramatic initial clinical response to reversible EGFR inhibitors. The clinical efficacy of reversible inhibitors is, however, ultimately limited due to the emergence of drug resistance, which is usually conferred by the EGFR T790M mutation. Importantly, irreversible, synthetic small molecule inhibitors are currently evaluated and some of them have been shown to overcome the acquired resistance that is oftentimes observed in these patients. Thus far, irreversible EGFR inhibitors as a drug class have not received regulatory approval due in part to their poor effectiveness at clinically achievable concentrations. Therefore, there is an urgent need to discover and develop novel, potent irreversible inhibitors against the EGFR T790M mutation. |
X Demographics
Geographical breakdown
Country | Count | As % |
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Unknown | 1 | 100% |
Demographic breakdown
Type | Count | As % |
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Members of the public | 1 | 100% |
Mendeley readers
Geographical breakdown
Country | Count | As % |
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Spain | 1 | 3% |
Germany | 1 | 3% |
Unknown | 31 | 94% |
Demographic breakdown
Readers by professional status | Count | As % |
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Student > Ph. D. Student | 6 | 18% |
Researcher | 5 | 15% |
Student > Master | 4 | 12% |
Professor | 4 | 12% |
Other | 3 | 9% |
Other | 6 | 18% |
Unknown | 5 | 15% |
Readers by discipline | Count | As % |
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Chemistry | 11 | 33% |
Biochemistry, Genetics and Molecular Biology | 4 | 12% |
Pharmacology, Toxicology and Pharmaceutical Science | 3 | 9% |
Agricultural and Biological Sciences | 3 | 9% |
Mathematics | 1 | 3% |
Other | 4 | 12% |
Unknown | 7 | 21% |