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Updated: Jul 9, 2026

Biosynthesis of a Flavonol from a Flavanone by Establishing a One-pot Bienzymatic Cascade
Published on: August 14, 2019
Flavonoids as RTK inhibitors and potential anticancer agents
Florence Teillet1, Ahcene Boumendjel, Jean Boutonnat
1Laboratoire de Dynamique Cellulaire, EPHE, Laboratoire TIMC-IMAG, UMR-CNRS 5525, Université Joseph Fourier, Pavillon Taillefer, 38706 La Tronche Cedex, France.
Abstract:
Tyrosine kinase receptors (RTKs) play a crucial role in the regulation of the cell division cycle. Currently more than 50 RTKs divided into several subfamilies have been described. The inhibition of these enzymes has emerged as an important research-area. Compounds able to inhibit the activity of these enzymes are expected to display antiproliferative properties. Flavonoids are representative of various small molecules acting as RTK inhibitors. These naturally occurring compounds are able to bind to the ATP-binding site of several kinases. The most plausible current hypothesis explaining the action of these substances on kinases is that the chromenone moiety of the flavonoid acts as a mimetic of the adenine moiety of ATP, the receptor co-factor. In this review, we report recent results on the activity of natural and synthetic derivatives of flavonoids as inhibitors of RTKs. Mechanistic aspects, the therapeutic usefulness, and the potential clinical use are discussed.
Insights
Flavonoids, natural compounds, inhibit tyrosine kinase receptors (RTKs) by binding to their ATP-binding site. This review explores their antiproliferative potential and clinical applications as RTK inhibitors.
Area of Science:
- Biochemistry
- Molecular Biology
- Pharmacology
Background:
- Tyrosine kinase receptors (RTKs) are critical regulators of cell division.
- Over 50 RTKs are known, grouped into distinct subfamilies.
- Inhibiting RTK activity is a key area of research for therapeutic intervention.
Purpose of the Study:
- To review recent findings on natural and synthetic flavonoid derivatives as RTK inhibitors.
- To discuss the mechanisms of action, therapeutic utility, and clinical potential of these compounds.
- To highlight flavonoids as promising small molecules targeting RTKs.
Main Methods:
- Literature review of studies on flavonoid RTK inhibition.
- Analysis of mechanistic data regarding flavonoid-ATP-binding site interactions.
- Evaluation of reported antiproliferative activities and therapeutic potential.
Main Results:
- Flavonoids act as RTK inhibitors by binding to the ATP-binding site.
- The chromenone moiety of flavonoids mimics ATP's adenine, explaining their kinase inhibitory action.
- Both natural and synthetic flavonoid derivatives show significant RTK inhibitory activity.
Conclusions:
- Flavonoids are effective inhibitors of tyrosine kinase receptors.
- Their ability to target RTKs suggests potential as antiproliferative agents.
- Further research into their therapeutic and clinical applications is warranted.
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