6 research outputs found

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

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    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

    (Z)-N-tert-Butyl-2-(4-methoxyanilino)-N′-(4-methoxyphenyl)-2-phenylacetimidamide

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    In the crystal of the title compound, C26H31N3O2, pairs of N—H...O hydrogen bonds link molecules, forming inversion dimers, which enclose an R22(20) ring motif. One N atom does not form hydrogen bonds and lies in a hydrophobic pocket with closest intermolecular contacts of 4.196 (2) and 4.262 (2) Å

    Targeting Mutant KRAS for Anticancer Therapeutics: A Review of Novel Small Molecule Modulators

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