ArticlePharmacology research & perspectives2021
ZINC40099027 activates human focal adhesion kinase by accelerating the enzymatic activity of the FAK kinase domain.
Article in Pharmacology research & perspectives, 2021. The graph could read no effect estimate from its abstract, so it casts no vote on the map. Cited by 18 papers.
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Who cites it
18 citing papers in PubMed, 19 citations in OpenAlex.
- CD98hc controls CNS angiogenesis and blood-brain barrier integrity through localized regulation of the systemic integrin-FAK pathway.Nature cardiovascular research · 2026Article
- [Ziyuglycoside II Inhibit the Progression of Non-small Cell Lung Cancer through the ITGB4/FAK Signaling Pathway].Zhongguo fei ai za zhi = Chinese journal of lung cancer · 2026Article
- Article
- Bioenergetic responses to β-adrenergic stimulation in beige adipocyte depend on actomyosin driven forces.bioRxiv : the preprint server for biology · 2025Article
- Focal adhesion kinase: A promising regulator of colitis-associated healing.World journal of gastroenterology · 2025Review
- The Toxoplasma secreted effector TgWIP modulates dendritic cell motility by activating host tyrosine phosphatases Shp1 and Shp2.Cellular and molecular life sciences : CMLS · 2024Article
- The Toxoplasma secreted effector TgWIP modulates dendritic cell motility by activating host tyrosine phosphatases Shp1 and Shp2.Research square · 2024Article
- Sustained intestinal epithelial monolayer wound closure after transient application of a FAK-activating small molecule.PloS one · 2024Article
- The dysadherin/FAK axis promotes individual cell migration in colon cancer.International journal of biological sciences · 2024Article
- Enhanced Bone Regeneration through Regulation of Mechanoresponsive FAK-ERK1/2 Signaling by ZINC40099027 during Distraction Osteogenesis.International journal of medical sciences · 2024Article
- Force-dependent focal adhesion assembly and disassembly: A computational study.PLoS computational biology · 2023Article
- A novel drug-like water-soluble small molecule Focal Adhesion Kinase (FAK) activator promotes intestinal mucosal healing.Current research in pharmacology and drug discovery · 2023Article
- An αvβ3 integrin checkpoint is critical for efficient TNature immunology · 2023Article
- Gut homeostasis, injury, and healing: New therapeutic targets.World journal of gastroenterology · 2022Review
- GSDMB is increased in IBD and regulates epithelial restitution/repair independent of pyroptosis.Cell · 2022Article
- Review
- Article
- ZINC40099027 activates human focal adhesion kinase by accelerating the enzymatic activity of the FAK kinase domain.Pharmacology research & perspectives · 2021Article
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Authors and funding
6 authors at 1 institution in 1 country.
Funding
Abstract
Focal adhesion kinase (FAK) regulates gastrointestinal epithelial restitution and healing. ZINC40099027 (Zn27) activates cellular FAK and promotes intestinal epithelial wound closure in vitro and in mice. However, whether Zn27 activates FAK directly or indirectly remains unknown. We evaluated Zn27 potential modulation of the key phosphatases, PTP-PEST, PTP1B, and SHP2, that inactivate FAK, and performed in vitro kinase assays with purified FAK to assess direct Zn27-FAK interaction. In human Caco-2 cells, Zn27-stimulated FAK-Tyr-397 phosphorylation despite PTP-PEST inhibition and did not affect PTP1B-FAK interaction or SHP2 activity. Conversely, in vitro kinase assays demonstrated that Zn27 directly activates both full-length 125 kDa FAK and its 35 kDa kinase domain. The ATP-competitive FAK inhibitor PF573228 reduced basal and ZN27-stimulated FAK phosphorylation in Caco-2 cells, but Zn27 increased FAK phosphorylation even in cells treated with PF573228. Increasing PF573228 concentrations completely prevented activation of 35 kDa FAK in vitro by a normally effective Zn27 concentration. Conversely, increasing Zn27 concentrations dose-dependently activated kinase activity and overcame PF573228 inhibition of FAK, suggesting the direct interactions of Zn27 with FAK may be competitive. Zn27 increased the maximal activity (V
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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.