ArticleAngewandte Chemie (International ed. in English)2021
Controlling the Covalent Reactivity of a Kinase Inhibitor with Light.
Article in Angewandte Chemie (International ed. in English), 2021. The graph could read no effect estimate from its abstract, so it casts no vote on the map. Cited by 17 papers.
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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
17 citing papers in PubMed.
- Advances in the design and discovery of small-molecule tyrosine kinase inhibitors for breast cancer.RSC advances · 2026Review
- Advances in JNK inhibitor development: therapeutic prospects in neurodegenerative diseases and fibrosis.Archives of pharmacal research · 2025Review
- Synthesis and Properties of Cyclic Imide Extended Diazocines: Tweezer-Like, Rigid Photoswitches with Large Switching Amplitudes.Chemistry (Weinheim an der Bergstrasse, Germany) · 2025Article
- A Urease-Based pH Photoswitch: A General Route to Light-to-pH Transduction.Angewandte Chemie (International ed. in English) · 2025Article
- Tilting the Scales toward EGFR Mutant Selectivity: Expanding the Scope of Bivalent "Type V" Kinase Inhibitors.Journal of medicinal chemistry · 2024Article
- Recent Progress in Regulating the Activity of Enzymes with Photoswitchable Inhibitors.Molecules (Basel, Switzerland) · 2024Review
- All-photonic kinase inhibitors: light-controlled release-and-report inhibition.Chemical science · 2024Article
- Visible Light Control over the Cytolytic Activity of a Toxic Pore-Forming Protein.ACS chemical biology · 2024Article
- Triplet sensitization enables bidirectional isomerization of diazocine with 130 nm redshift in excitation wavelengths.Chemical science · 2023Article
- Photoswitchable Inhibitors to Optically Control Specific Kinase Activity.ACS chemical biology · 2023Article
- StilleRSC advances · 2023Article
- Photocaging of Pyridinylimidazole-Based Covalent JNK3 Inhibitors Affords Spatiotemporal Control of the Binding Affinity in Live Cells.Pharmaceuticals (Basel, Switzerland) · 2023Article
- Design and Synthesis of Visible-Light-Responsive Azobenzene Building Blocks for Chemical Biology.The Journal of organic chemistry · 2022Article
- Photoresponsive Small Molecule Inhibitors for the Remote Control of Enzyme Activity.Chemistry, an Asian journal · 2022Review
- Light-Control over Casein Kinase 1δ Activity with Photopharmacology: A Clear Case for Arylazopyrazole-Based Inhibitors.International journal of molecular sciences · 2022Article
- Hypothesis-Driven, Structure-Based Design in Photopharmacology: The Case of eDHFR Inhibitors.Journal of medicinal chemistry · 2022Article
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Authors and funding
8 authors.
Funding
Abstract
Covalent kinase inhibitors account for some of the most successful drugs that have recently entered the clinic and many others are in preclinical development. A common strategy is to target cysteines in the vicinity of the ATP binding site using an acrylamide electrophile. To increase the tissue selectivity of kinase inhibitors, it could be advantageous to control the reactivity of these electrophiles with light. Here, we introduce covalent inhibitors of the kinase JNK3 that function as photoswitchable affinity labels (PALs). Our lead compounds contain a diazocine photoswitch, are poor non-covalent inhibitors in the dark, and become effective covalent inhibitors after irradiation with visible light. Our proposed mode of action is supported by X-ray structures that explain why these compounds are unreactive in the dark and undergo proximity-based covalent attachment following exposure to light.
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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.