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Endovascular Stem Cell Therapy Post Stroke Rescues Neurons from Endoplasmic Reticulum Stress-Induced Apoptosis by Modulating Brain-Derived Neurotrophic Factor/Tropomyosin Receptor Kinase B Signaling.

ACS Chemical Neuroscience, 2021
Ischemic stroke is devastating, with serious long-term disabilities affecting millions of people worldwide. Growing evidence has shown that mesenchymal stem cells (MSCs) administration after stroke provides neuroprotection and enhances the quality of ...
Harpreet Kaur   +7 more
semanticscholar   +1 more source

Discovery of Tropomyosin Receptor Kinase Inhibitors as New Generation Anticancer Agents: A Review

Current Topics in Medicinal Chemistry
Background:: 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
openaire   +2 more sources

Overexpressions of Nerve Growth Factor and Its Tropomyosin-Related Kinase A Receptor on Chordoma Cells

Spine, 2007
Immunohistochemistry and in situ apoptosis detection assay were performed on chordoma and notochordal cells.To investigate the expression levels of nerve growth factor (NGF) and its 2 receptors, tropomyosin-related kinase A (TrkA) and p75, as well as proliferation potential and apoptosis indexes in chordoma and notochordal cells.Chordomas arise from ...
Jong-Beom, Park   +5 more
openaire   +2 more sources

Discovery of First-In-Class Potent and Selective Tropomyosin Receptor Kinase Degraders.

Journal of Medicinal Chemistry, 2020
We report compounds 5 (CG416) and 6 (CG428) as two first-in-class tropomyosin receptor kinase (TRK) degraders that target the intracellular kinase domain of TRK.
Liqun Chen   +16 more
semanticscholar   +1 more source

First-in-Human Brain Imaging of [18F]TRACK, a PET tracer for Tropomyosin Receptor Kinases

ACS Chemical Neuroscience, 2019
The tropomyosin receptor kinase TrkA/B/C family is responsible for human neuronal growth, survival, and differentiation from early nervous system development stages onward. Downregulation of TrkA/B/C receptors characterizes numerous neurological disorders including Alzheimer's disease (AD).
Justin J. Bailey   +14 more
openaire   +2 more sources

A peptide encoded by upstream open reading frame of MYC binds to tropomyosin receptor kinase B and promotes glioblastoma growth in mice

Science Translational Medicine
MYC promotes tumor growth through multiple mechanisms. Here, we show that, in human glioblastomas, the variant MYC transcript encodes a 114–amino acid peptide, MYC pre-mRNA encoded protein (MPEP), from the upstream open reading frame (uORF) MPEP ...
Fanying Li   +18 more
semanticscholar   +1 more source

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

Expert Opinion on Therapeutic Patents
The Trk family proteins are membrane-bound kinases predominantly expressed in neuronal tissues. Activated by neurotrophins, they regulate critical cellular processes through downstream signaling pathways. Dysregulation of Trk signaling can drive a range of diseases, making the design and study of Trk inhibitors a vital area of research.
Petar, Iliev   +6 more
openaire   +2 more sources

Identification of [18F]TRACK, a Fluorine-18-Labeled Tropomyosin Receptor Kinase (Trk) Inhibitor for PET Imaging

Journal of Medicinal Chemistry, 2018
Changes in expression and dysfunctional signaling of TrkA/B/C receptors and oncogenic Trk fusion proteins are found in neurological diseases and cancers. Here, we describe the development of a first 18F-labeled optimized lead suitable for in vivo imaging of Trk, [18F]TRACK, which is radiosynthesized with ease from a nonactivated aryl precursor ...
Vadim Bernard-Gauthier   +19 more
openaire   +2 more sources

Discovery and Hit to Lead Optimization of Macrocyclic Peptides as Novel Tropomyosin Receptor Kinase A Antagonists

Journal of Medicinal Chemistry
Tropomyosin receptor kinases (Trks) are receptor tyrosine kinases activated by neurotrophic factors, called neurotrophins. Among them, TrkA interacts with the nerve growth factor (NGF), which leads to pain induction. mRNA-display screening was carried out to discover a hit compound 2, which inhibits protein-protein interactions between TrkA and NGF ...
Toru Yamada   +8 more
openaire   +2 more sources

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