靶向EGFR蛋白降解剂及其在非小细胞肺癌中的应用

doi:10.3969/j.issn.0253-9608.2021.06.002

Abstract

Abstract: Activating mutations in the kinase domains of EGFR (epidermal growth factor receptor) lead into the occurrence of non-small cell lung cancer. Currently, the standard care for such diseases is to use EGFR-specific tyrosine kinase inhibitor drugs. However,
drug resistance inevitably occurs after the treatment with these drugs. Novel strategies are needed to solve these issues to extend
patients survival time. Due to the dependency of EGFR mutant lung cancer on EGFR proteins and the critical roles of EGFR protein
in drug resistance, targeted degradation of EGFR protein provides a promising strategy to treat such patients. Several novel strategies have been developed lately to target EGFR for degradation in non-small cell lung cancer. The strategies include proteolysis targeting chimeras (PROTACs), lysosome-targeting chimaera (LYTAC) and stapled-peptide. The latest development of these strategies were reviewed and their potential uses in lung cancer treatment were assessed.

Key words: proteolysis targeting chimera (PROTAC), EGFR mutation, non-small cell lung cancer, targeted degradation, drug , resistance, lysosome-targeting chimaera (LYTAC)

SONG Xiaoling , QU Xiaojuan , QU Siqi , JIANG Biao. Novel strategies to target EGFR proteins for degradation and their applications in non-small cell lung cancer[J]. Chinese Journal of Nature, 2021, 43(6): 400-407.

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Novel strategies to target EGFR proteins for degradation and their applications in non-small cell lung cancer

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