Pyrazolo[1,5-a]pyrimidine as a Prominent Framework for Tropomyosin Receptor Kinase (Trk) Inhibitors—Synthetic Strategies and SAR Insights [PDF]
MoleculesTropomyosin receptor kinases (Trks) are transmembrane receptor tyrosine kinases named TrkA, TrkB, and TrkC and encoded by the NTRK1, NTRK2, and NTRK3 genes, respectively.
Amol T. Mahajan +5 more
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The Research Progress of Neurotrophic Tyrosine Receptor Kinase (NTRK) Gene Fusions and Tropomyosin Receptor Kinase (TRK) Inhibitors: A Narrative Review [PDF]
Iran J Public HealthNTRK gene is responsible for encoding TRK, which consists of three family members: NTRK1, NTRK2, and NTRK3. These family members encode different proteins known as TRKA, TRKB, and TRKC, respectively. NTRK fusion genes are the clearest driving factor for carcinogenesis.
Li J, Liang Y.
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Development of small-molecule tropomyosin receptor kinase (TRK) inhibitors for NTRK fusion cancers [PDF]
Acta Pharmaceutica Sinica B, 2021 Tropomyosin receptor kinase A, B and C (TRKA, TRKB and TRKC), which are well-known members of the cell surface receptor tyrosine kinase (RTK) family, are encoded by the neurotrophic receptor tyrosine kinase 1, 2 and 3 (NTRK1, NTRK2 and NTRK3) genes ...
Tingting Jiang +7 more
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Induction of resistance to neurotrophic tropomyosin‐receptor kinase inhibitors by HMGCS2 via a mevalonate pathway [PDF]
Cancer MedicineIntroduction A neurotrophic tropomyosin receptor kinase (NTRK)‐tyrosine kinase inhibitor (TKI) has shown dramatic efficacy against malignant tumors harboring an NTRK fusion gene.
Yasuhiro Kato +12 more
doaj +5 more sources
Tropomyosin receptor kinase B (TrkB) signalling: targeted therapy in neurogenic tumours [PDF]
The Journal of Pathology: Clinical Research, 2023 Tropomyosin receptor kinase B (TrkB), a transmembrane receptor protein, has been found to play a pivotal role in neural development. This protein is encoded by the neurotrophic receptor tyrosine kinase 2 (NTRK2) gene, and its abnormal activation caused ...
Yuehua Li +4 more
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Identification and characterization of the Cucurbitacins, a novel class of small-molecule inhibitors of Tropomyosin receptor kinase a [PDF]
BMC Complementary and Alternative Medicine, 2019 Background NGF-TrkA is well known to play a key role in propagating and sustaining pruritogenic signals, which form the pathology of chronic pruritus. Inhibition of NGF-TrkA is a known strategy for the treatment of pruritus.
Yueling Zhong +9 more
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Tropomyosin receptor kinase: a novel target in screened neuroendocrine tumors [PDF]
Endocrine-Related Cancer, 2018 Tropomyosin receptor kinase (Trk) inhibitors are investigated as a novel targeted therapy in various cancers. We investigated thein vitroeffects of the pan-Trk inhibitor GNF-5837 in human neuroendocrine tumor (NET) cells. The human neuroendocrine pancreatic BON1, bronchopulmonary NCI-H727 and ileal GOT1 cell lines were treated with GNF-5837 alone and ...
Elke Tatjana Aristizabal Prada +13 more
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Downstream of tyrosine kinase/docking protein 6, as a novel substrate of tropomyosin-related kinase C receptor, is involved in neurotrophin 3-mediated neurite outgrowth in mouse cortex neurons [PDF]
BMC Biology, 2010 Background The downstream of tyrosine kinase/docking protein (Dok) adaptor protein family has seven members, Dok1 to Dok7, that act as substrates of multiple receptor tyrosine kinase and non-receptor tyrosine kinase.
Yuan Jian +6 more
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Unlocking the potential of approved drugs for the allosteric inhibition of tropomyosin-receptor kinase A using molecular docking and molecular dynamics studies [PDF]
Frontiers in Chemistry, 2023 Tropomyosin-receptor kinase A (TrkA) is the primary isoform among the tropomyosin-receptor kinases that have been associated with human cancer development, contributing to approximately 7.4% of all cancer cases.
Rua M. Mukhtar +20 more
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Larotrectinib: A Novel Tumor-Agnostic Neurotrophic Tropomyosin Receptor Kinase (NTRK) Inhibitor in Advanced Solid Tumors [PDF]
Indian Journal of Medical and Paediatric Oncology, 2021 AbstractLarotrectinib and entrectinib are highly selective, potent tropomyosin receptor kinase fusion inhibitors. It is U.S. Food and Drug Administration approved for the treatment of adult and pediatric advanced solid tumors with neurotrophic tropomyosin receptor kinase fusion genes who are refractory to standard systemic therapy.
Manikandan Dhanushkodi, Jyoti Bajpai
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