ArticleJournal of medicinal chemistry2025
Tetrahydropyrazolopyridinones as a Novel Class of Potent and Highly Selective LIMK Inhibitors.
Article in Journal of medicinal chemistry, 2025. The graph could read no effect estimate from its abstract, so it casts no vote on the map. Cited by 3 papers.
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The trial behind it
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
3 citing papers in PubMed.
- Probing Allosteric Kinase Modulators as Next Game-Changers in Fighting Neurodegeneration.Journal of medicinal chemistry · 2026Review
- Rational design and structural Bioinformatics-Driven discovery of tetrapeptide inhibitors for LIMK-Targeted cancer therapy.Medical oncology (Northwood, London, England) · 2025Article
- Exploring diarylheptanoid derivatives to target LIMK1 as potential agents against colorectal cancer.Journal of enzyme inhibition and medicinal chemistry · 2025Article
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Authors and funding
15 authors.
Funding
No grant is acknowledged in the PubMed record.
Abstract
LIMKs are serine/threonine and tyrosine kinases that play critical roles in regulating actin filament turnover, affecting key cellular processes such as cytoskeletal remodeling, proliferation and migration. Aberrant LIMK overactivation has been implicated in several diseases, including cancers and neurodegenerative disorders. Understanding the precise molecular mechanisms by which LIMKs modulate actin cytoskeletal dynamics necessitates highly potent and selective LIMK pharmacological inhibitors. We report the discovery of a novel class of allosteric dual-LIMK1/2 inhibitors based on the tetrahydropyrazolopyridinone scaffold. Using structure-based drug design, we identified MDI-117740 (
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