ArticleScientific reports2015
Design, Synthesis and Inhibitory Activity of Photoswitchable RET Kinase Inhibitors.
Article in Scientific reports, 2015. The graph could read no effect estimate from its abstract, so it casts no vote on the map. Cited by 19 papers.
What it found
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The abstract states no effect estimate the extractor could read, or names no intervention and outcome on the map, so this paper lights no cell and moves no belief. It is still indexed, cited and linked below.
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Trials whose registry record cites this paper, or whose number appears in the abstract. A trial that started after this paper was published is citing it as background, not reporting it.
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Who cites it
19 citing papers in PubMed, 76 citations in OpenAlex.
- Photoswitchable Inhibitors to Optically Control Specific Kinase Activity.ACS chemical biology · 2023Article
- Light-Control over Casein Kinase 1δ Activity with Photopharmacology: A Clear Case for Arylazopyrazole-Based Inhibitors.International journal of molecular sciences · 2022Article
- Optical Control of Mitosis with a Photoswitchable Eg5 Inhibitor.Angewandte Chemie (International ed. in English) · 2022Article
- Molecular photoswitches in aqueous environments.Chemical Society reviews · 2021Review
- Controlling the Covalent Reactivity of a Kinase Inhibitor with Light.Angewandte Chemie (International ed. in English) · 2021Article
- Photopharmacological Applications for Cherenkov Radiation Generated by Clinically Used Radionuclides.International journal of molecular sciences · 2021Article
- Review
- Chemoproteomics-Enabled De Novo Discovery of Photoswitchable Carboxylesterase Inhibitors for Optically Controlled Drug Metabolism.Angewandte Chemie (International ed. in English) · 2021Article
- Photoswitchable Azo- and Diazocine-Functionalized Derivatives of the VEGFR-2 Inhibitor Axitinib.International journal of molecular sciences · 2020Article
- Base-Promoted Radical Azofluoromethylation of Unactivated Alkenes.Organic letters · 2020Article
- Reversible Photocontrolled Nanopore Assembly.Journal of the American Chemical Society · 2019Article
- Expression of BMP-4 and Smad1 in patients with Hirschsprung disease and its clinical significance.Experimental and therapeutic medicine · 2019Article
- Mapping the Azolog Space Enables the Optical Control of New Biological Targets.ACS central science · 2019Article
- Molecular Motors in Aqueous Environment.The Journal of organic chemistry · 2018Article
- Two-Step, One-Pot Synthesis of Visible-Light-Responsive 6-Azopurines.Organic letters · 2017Article
- Photo-enhanced Aqueous Solubilization of an Azo-compound.Scientific reports · 2017Article
- The molecular basis for RET tyrosine-kinase inhibitors in thyroid cancer.Best practice & research. Clinical endocrinology & metabolism · 2017Review
- Cyclic and Macrocyclic Peptides as Chemical Tools To Recognise Protein Surfaces and Probe Protein-Protein Interactions.ChemMedChem · 2016Review
- The role of alkyl substituents in deazaadenine-based diarylethene photoswitches.Beilstein journal of organic chemistry · 2016Article
Corrections and comments
PubMed lists nothing against this paper. Absence here is not a guarantee, only a check that was made.
Authors and funding
5 authors at 2 institutions in 1 country.
Funding
No grant is acknowledged in the PubMed record.
Abstract
REarranged during Transfection (RET) is a transmembrane receptor tyrosine kinase required for normal development and maintenance of neurons of the central and peripheral nervous systems. Deregulation of RET and hyperactivity of the RET kinase is intimately connected to several types of human cancers, most notably thyroid cancers, making it an attractive therapeutic target for small-molecule kinase inhibitors. Novel approaches, allowing external control of the activity of RET, would be key additions to the signal transduction toolbox. In this work, photoswitchable RET kinase inhibitors based on azo-functionalized pyrazolopyrimidines were developed, enabling photonic control of RET activity. The most promising compound displays excellent switching properties and stability with good inhibitory effect towards RET in cell-free as well as live-cell assays and a significant difference in inhibitory activity between its two photoisomeric forms. As the first reported photoswitchable small-molecule kinase inhibitor, we consider the herein presented effector to be a significant step forward in the development of tools for kinase signal transduction studies with spatiotemporal control over inhibitor concentration in situ.
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Registered trials
Read under generation 80e0d062 · epoch 390. Bibliography from PubMed, PubMed Central and OpenAlex; grants from NIH RePORTER; trial links from ClinicalTrials.gov; estimates, votes and beliefs from the OpenQuestion graph.