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Strategies to overcome acquired resistances conferred by mutations in the kinase domain of EGFR

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Title
Strategies to overcome acquired resistances conferred by mutations in the kinase domain of EGFR
Author(s)
Sang Min Lim; Yujeong Jeong; Sungwoo Hong
Publication Date
2016-05
Journal
FUTURE MEDICINAL CHEMISTRY, v.8, no.8, pp.853 - 878
Publisher
FUTURE SCI LTD
Abstract
Deregulation of EGFR is involved in the development of many cancers. The inhibition of EGFR kinase activity has been clinically validated as a promising approach for the treatment of non-small-cell lung cancer (NSCLC). However, all NSCLC patients who initially benefited from first-generation EGFR inhibitors eventually develop drug resistance. A point mutation at the gatekeeper position, T790M in EGFR kinase domain accounts for more than 50% of acquired resistance. Therefore, second- and third-generation EGFR inhibitors have been developed to overcome the resistance conferred by the gatekeeper mutation. This review has highlighted recent advances in overcoming acquired resistance for the development of each generation of EGFR inhibitors along with their potential issues, and urgent quest for the development of new generation of EGFR inhibitors. © 2016 Future Science Ltd
URI
https://pr.ibs.re.kr/handle/8788114/2662
ISSN
1756-8919
Appears in Collections:
Center for Catalytic Hydrocarbon Functionalizations(분자활성 촉매반응 연구단) > Journal Papers (저널논문)
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