Noncovalent Mutant Selective Epidermal Growth Factor Receptor Inhibitors: A Lead Optimization Case Study.

doi:10.1021/acs.jmedchem.5b01412

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Article

Noncovalent Mutant Selective Epidermal Growth Factor Receptor Inhibitors: A Lead Optimization Case Study.

Journal of medicinal chemistry - 25 Nov 2015

Heald Robert, Bowman Krista K, Bryan Marian C, Burdick Daniel, Chan Bryan, Chan Emily, Chen Yuan, Clausen Saundra, Dominguez-Fernandez Belen, Eigenbrot Charles, Elliott Richard, Hanan Emily J, Jackson Philip, Knight Jamie, La Hank, Lainchbury Michael, Malek Shiva, Mann Sam, Merchant Mark, Mortara Kyle, Purkey Hans, Schaefer Gabriele, Schmidt Stephen, Seward Eileen, Sideris Steve, Shao Lily, Wang Shumei, Yeap Kuen, Yen Ivana, Yu Christine, Heffron Timothy P

Abstract excerpt

Because of their increased activity against activating mutants, first-generation epidermal growth factor receptor (EGFR) kinase inhibitors have had remarkable success in treating non-small-cell lung cancer (NSCLC) patients, but acquired resistance, through a secondary mutation of the gatekeeper residue, means that clinical responses only last for 8-14 months. Addressing this unmet medical need requires agents...

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PMID: 26455919
DOI: 10.1021/acs.jmedchem.5b01412

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