Yan, W;
Lakkaniga, NR;
Carlomagno, F;
Santoro, M;
McDonald, NQ;
Lv, F;
Gunaganti, N;
... Li, H-Y; + view all
(2019)
Insights into Current Tropomyosin Receptor Kinase (TRK) Inhibitors: Development and Clinical Application.
Journal of Medicinal Chemistry
, 62
(4)
pp. 1731-1760.
10.1021/acs.jmedchem.8b01092.
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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.
| Type: | Article |
|---|---|
| Title: | Insights into Current Tropomyosin Receptor Kinase (TRK) Inhibitors: Development and Clinical Application |
| Open access status: | An open access version is available from UCL Discovery |
| DOI: | 10.1021/acs.jmedchem.8b01092 |
| Publisher version: | https://doi.org/10.1021/acs.jmedchem.8b01092 |
| Language: | English |
| Additional information: | This version is the author accepted manuscript. For information on re-use, please refer to the publisher’s terms and conditions. |
| UCL classification: | UCL UCL > Provost and Vice Provost Offices > School of Life and Medical Sciences UCL > Provost and Vice Provost Offices > School of Life and Medical Sciences > Faculty of Life Sciences |
| URI: | https://discovery-pp.ucl.ac.uk/id/eprint/10093065 |
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