Literature DB >> 23400472

Maximizing the benefits of off-target kinase inhibitor activity.

Monica Red Brewer1, William Pao.   

Abstract

Investigators report the identification of novel mutant-specific inhibition of EGF receptor (EGFR) T790M by bis-indole-based inhibitors of protein kinase C using a small-molecule cancer cell line-based screening platform. This study shows the power of high-throughput drug screening in cancer cell lines and provides new lead scaffolds for optimization against resistant EGFR mutants in lung cancer.

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Year:  2013        PMID: 23400472     DOI: 10.1158/2159-8290.CD-12-0581

Source DB:  PubMed          Journal:  Cancer Discov        ISSN: 2159-8274            Impact factor:   39.397


  3 in total

Review 1.  The quest to overcome resistance to EGFR-targeted therapies in cancer.

Authors:  Curtis R Chong; Pasi A Jänne
Journal:  Nat Med       Date:  2013-11-07       Impact factor: 53.440

2.  Linking off-target kinase pharmacology to the differential cellular effects observed among PARP inhibitors.

Authors:  Albert A Antolín; Jordi Mestres
Journal:  Oncotarget       Date:  2014-05-30

Review 3.  Polypharmacology in Precision Oncology: Current Applications and Future Prospects.

Authors:  Albert A Antolin; Paul Workman; Jordi Mestres; Bissan Al-Lazikani
Journal:  Curr Pharm Des       Date:  2016       Impact factor: 3.116

  3 in total

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