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    Insights into Current Tropomyosin Receptor Kinase (TRK) inhibitors: development and clinical application

    Yan, W. and Lakkaniga, N.R. and Gunaganti, N. and Lv, F. and Carlomagno, F. and Santoro, M. and McDonald, Neil Q. and Frett, B. and Li, H.-Y. (2018) Insights into Current Tropomyosin Receptor Kinase (TRK) inhibitors: development and clinical application. Journal of Medicinal Chemistry 62 (4), pp. 1731-1760. ISSN 0022-2623.

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    Abstract

    The use of kinase-directed precision medicine has been heavily pursued since the discovery and development of imatinib. Annually, it is estimated that around ∼20 000 new cases of tropomyosin receptor kinase (TRK) cancers are diagnosed, with the majority of cases exhibiting a TRK genomic rearrangement. In this Perspective, we discuss current development and clinical applications for TRK precision medicine by providing the following: (1) the biological background and significance of the TRK kinase family, (2) a compilation of known TRK inhibitors and analysis of their cocrystal structures, (3) an overview of TRK clinical trials, and (4) future perspectives for drug discovery and development of TRK inhibitors.

    Metadata

    Item Type: Article
    School: Birkbeck Schools and Departments > School of Science > Biological Sciences
    Depositing User: Neil Mcdonald
    Date Deposited: 29 Mar 2019 14:41
    Last Modified: 08 Sep 2019 09:46
    URI: http://eprints.bbk.ac.uk/id/eprint/24751

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