Exploiting receptor tyrosine kinase co-activation for cancer therapy

Aik Choon Tan, Simon Vyse, Paul H. Huang

    Research output: Contribution to journalReview articlepeer-review

    28 Citations (Scopus)

    Abstract

    Studies over the past decade have shown that many cancers have evolved receptor tyrosine kinase (RTK) co-activation as a mechanism to drive tumour progression and limit the lethal effects of therapy. This review summarises the general principles of RTK co-activation and discusses approaches to exploit this phenomenon in cancer therapy and drug discovery. Computational strategies to predict kinase co-dependencies by integrating drug screening data and kinase inhibitor selectivity profiles will also be described. We offer a perspective on the implications of RTK co-activation on tumour heterogeneity and cancer evolution and conclude by surveying emerging computational and experimental approaches that will provide insights into RTK co-activation biology and deliver new developments in effective cancer therapies.

    Original languageEnglish
    Pages (from-to)72-84
    Number of pages13
    JournalDrug Discovery Today
    Volume22
    Issue number1
    DOIs
    Publication statusPublished - 2017 Jan 1

    Bibliographical note

    Publisher Copyright:
    © 2016 Elsevier Ltd

    ASJC Scopus subject areas

    • Pharmacology
    • Drug Discovery

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