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Identification and structural analysis of a selective tropomyosin receptor kinase C (TRKC) inhibitor

European Journal of Medicinal Chemistry, 2022
Tropomyosin 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
openaire   +2 more sources

Transplantation of bone marrow stromal stem cells overexpressing tropomyosin receptor kinase A for peripheral nerve repair.

Cytotherapy, 2017
Previously we reported that overexpression of tropomyosin receptor kinase A (TrkA) could improve the survival and Schwann-like cell differentiation of bone marrow stromal stem cells (BMSCs) in nerve grafts for bridging rat sciatic nerve defects.
Meige Zheng   +8 more
semanticscholar   +3 more sources

Type I inhibitors of tropomyosin receptor kinase (Trk): a 2020–2022 patent update

Expert Opinion on Therapeutic Patents, 2023
Trk inhibitors are significant in the realm of personalized medicine as they target specific genetic alterations, such as NTRK gene fusions, leading to improved treatment outcomes for cancer patients. By tailoring the treatment to the genetic characteristics of the tumor rather than the tumor type, Trk inhibitors offer the potential for more effective ...
Carolin Jaworski   +6 more
openaire   +2 more sources

Tropomyosin receptor kinase inhibitors: a patent update 2009 – 2013

Expert Opinion on Therapeutic Patents, 2014
Tropomyosin receptor kinases (Trks) are a family of three similar tyrosine kinases activated by peptide hormones of the neurotrophin family. The nerve growth factor antibody tanezumab has provided clinical proof of concept for inhibition of the TrkA pathway in pain.
Clive, McCarthy, Edward, Walker
openaire   +2 more sources

Recent advances in the discovery of tropomyosin receptor kinases TRKs inhibitors: A mini review

European Journal of Medicinal Chemistry, 2023
The 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
openaire   +2 more sources

An isoform-selective inhibitor of tropomyosin receptor kinase A behaves as molecular glue

Bioorganic & Medicinal Chemistry Letters, 2020
The production of TrkA-selective inhibitors is considerably difficult because the kinase domains of TrkA and its isoforms TrkB/C have highly homologous amino acid sequences. Here we describe the structural basis for the acquisition of selectivity for a isoform-selective TrkA inhibitor, namely compound V1.
Noritaka Furuya   +8 more
openaire   +2 more sources

Real-world Experience With Neurotrophic Tyrosine Receptor Kinase Fusion–positive Tumors and Tropomyosin Receptor Kinase Inhibitors in Veterans

JCO Precision Oncology, 2023
PURPOSE Neurotrophic tyrosine receptor kinase 1-3 (NTRK1-3) gene fusions are found in a broad range of tumor types. Clinical trials demonstrated high response rates to tropomyosin receptor kinase (TRK) inhibitors in NTRK fusion–positive cancers, but few ...
K. I. Zhou   +4 more
semanticscholar   +1 more source

Identification of potential inhibitors of tropomyosin receptor kinase B targeting CNS-related disorders and cancers

Journal of Biomolecular Structure and Dynamics, 2023
Tropomyosin receptor kinase B (TrkB), also known as neurotrophic tyrosine kinase receptor type 2 (NTRK2), is a protein that belongs to the family of receptor tyrosine kinases (RTKs). NTRK2 plays a crucial role in regulating the development and maturation
M. A. Hakami   +6 more
semanticscholar   +1 more source

Real‐world experience of tropomyosin receptor kinase inhibition with entrectinib in ETV6‐NTRK3 positive metastatic salivary secretory carcinoma: A case series

Head and Neck, 2023
The efficacy of entrectinib, a potent inhibitor of tropomyosin receptor kinases, c‐ros oncogene 1, and anaplastic lymphoma kinase has been demonstrated in neurotrophic receptor tyrosine kinase fusion‐positive pediatric and adult solid tumors.
T. Yokota   +3 more
semanticscholar   +1 more source

Discovery of Next-Generation Tropomyosin Receptor Kinase Inhibitors for Combating Multiple Resistance Associated with Protein Mutation.

Journal of Medicinal Chemistry, 2021
Tropomyosin receptor kinase (TRK) inhibition is an effective therapeutic approach for treatment of a variety of cancers. Despite the use of first-generation TRK inhibitor (TRKI) larotrectinib (1) resulting in significant therapeutic response in patients,
L. Zhuo   +10 more
semanticscholar   +1 more source

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