Neurotrophic tropomyosin or tyrosine receptor kinase (NTRK) genes
Journal of Clinical Pathology, 2019The neurotrophic tropomyosin or tyrosine receptor kinase (NTRK) genes (1-3) are proto-oncogenes that when activated are encountered in a wide array of tumours. The recent advent of very specific and selective inhibitors of their gene fusions makes the NRTK gene fusions actionable.
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Conformational adjustment overcomes multiple drug-resistance mutants of tropomyosin receptor kinase
European Journal of Medicinal Chemistry, 2022Mutation-induced resistance to targeted drug treatment poses a serious threat to successful chemotherapy. Multiple mutations underlying drug resistance remain a largely unsolved scientific issue. Tropomyosin receptor kinases (TRKs) are promising therapeutic targets for several malignant human cancers, but they have become less effective due to multiple
Long-Can, Mei+5 more
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Identification and structural analysis of a selective tropomyosin receptor kinase C (TRKC) inhibitor
European Journal of Medicinal Chemistry, 2022Tropomyosin receptor kinases (TRKs) are a family of TRKA, TRKB and TRKC isoforms. It has been widely reported that TRKs are implicated in a variety of tumors with several Pan-TRK inhibitors currently being used or evaluated in clinical treatment. However, off-target adverse events frequently occur in the clinical use of Pan-TRK inhibitors, which result
Zhijie Wang+18 more
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Type 2 inhibitor leads of human tropomyosin receptor kinase (hTrkA)
Bioorganic & Medicinal Chemistry Letters, 2019In silico virtual screening using the ligand-based ROCS approach and the commercially purchasable compound collection from the ZINC database resulted in the identification of distinctly different and novel acetamide core frameworks with series representatives 1a and 2a exhibiting nanomolar affinity in the kinase domain only hTrkA HTRF biochemical assay.
Nicole Roush+8 more
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Recent advances in the discovery of tropomyosin receptor kinases TRKs inhibitors: A mini review
European Journal of Medicinal Chemistry, 2023The tropomyosin receptor tyrosine kinases (TRKs) control the cell proliferation mainly in the nervous system and are encoded by NTRK genes. Fusion and mutation of NTRK genes were detected in various types of cancers. Many small molecules TRK inhibitors have been discovered during the last two decades and some of them have entered clinical trials ...
Hala B. El-Nassan, Mustafa A. Al-Qadhi
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Primary sensory neurons expressing tropomyosin receptor kinase A in the rat trigeminal ganglion
Neuroscience Letters, 2019Tropomyosin receptor kinase A (trkA), a high affinity receptor for nerve growth factor (NGF), has been implicated in neuronal survival, neurite outgrowth and inflammatory pain. So far, the characterization of the primary sensory neurons that express trkA, and are thus potentially affected by NGF, has remained incomplete.
Hye Min Han+3 more
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Toward Imaging Tropomyosin Receptor Kinase (Trk) with Positron Emission Tomography
2020The three tropomyosin receptor kinases (TrkA, B, and C) fulfill important roles within the central nervous system facilitating neuronal growth, neuronal survival, and neuronal differentiation during cell development at all ages of neuronal development.
Carmen Wängler+5 more
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Sexual motivation in male rats is modulated by tropomyosin receptor kinase B (TrkB).
Behavioral Neuroscience, 2019The expression of brain derived neurotrophic factor (BDNF) and tropomyosin receptor kinase B (TrkB) are regulated by gonadal hormone signaling and are expressed in brain areas that are important for sexual behaviors. Accordingly, BDNF and TrkB signaling have been shown to be important for the expression of consummatory sexual behaviors.
Deandra E. Mosura, Wayne R. Hawley
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Discovery of Tropomyosin Receptor Kinase Inhibitors as New Generation Anticancer Agents: A Review
Current Topics in Medicinal ChemistryBackground:: The tropomyosin receptor kinases (TRKs) are crucial for many cellular functions, such as growth, motility, differentiation, and metabolism. Abnormal TRK signalling contributes to a variety of human disorders, most evidently cancer. Comprehensive genomic stud-ies have found numerous changes in the genes that code for TRKs like MET, HER2 ...
Ishan Panchal+3 more
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