Proteolysis Targeting Chimeras (PROTACs) of Anaplastic Lymphoma Kinase (ALK).

ABSTRACT: Anaplastic lymphoma kinase (ALK) activation has been associated with many types of human cancer. Significant efforts have been devoted to the development of ALK inhibitors to antagonize the kinase activity of ALK. Four ALK inhibitors have been approved by the FDA to date for treating patients with ALK-positive non-small cell lung cancers (NSCLC). However, drug resistance has been observed in the majority of patients treated with these inhibitors. New therapeutic strategies (e.g., compounds with novel mechanisms of action) are needed to overcome the drug resistance issue. The emerging PROTAC (Proteolysis Targeting Chimera) technology has been successfully applied to selective degradation of multiple protein targets, but not ALK. Since ALK protein levels are not important for viability in ma

SUBMITTER: Zhang C 

PROVIDER: S-EPMC5924614 | biostudies-literature | 2018 May

REPOSITORIES: biostudies-literature