TY - JOUR
T1 - Insights into Current Tropomyosin Receptor Kinase (TRK) Inhibitors
T2 - Development and Clinical Application
AU - Yan, Wei
AU - Lakkaniga, Naga Rajiv
AU - Carlomagno, Francesca
AU - Santoro, Massimo
AU - McDonald, Neil Q.
AU - Lv, Fengping
AU - Gunaganti, Naresh
AU - Frett, Brendan
AU - Li, Hong Yu
N1 - Funding Information:
H.L. was supported by the grants (NIH 1R01CA194094-010 and 1R01CA197178-01A1).
Publisher Copyright:
© 2018 American Chemical Society.
PY - 2019/2/28
Y1 - 2019/2/28
N2 - The use of kinase-directed precision medicine has been heavily pursued since the discovery and development of imatinib. Annually, it is estimated that around 20000 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.
AB - The use of kinase-directed precision medicine has been heavily pursued since the discovery and development of imatinib. Annually, it is estimated that around 20000 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.
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U2 - 10.1021/acs.jmedchem.8b01092
DO - 10.1021/acs.jmedchem.8b01092
M3 - Review article
C2 - 30188734
AN - SCOPUS:85053832680
VL - 62
SP - 1731
EP - 1760
JO - Journal of Medicinal Chemistry
JF - Journal of Medicinal Chemistry
SN - 0022-2623
IS - 4
ER -