ArticleEuropean journal of medicinal chemistry2014
Design, synthesis, and biological evaluation of novel FAK scaffold inhibitors targeting the FAK-VEGFR3 protein-protein interaction.
Article in European journal of medicinal chemistry, 2014. The graph could read no effect estimate from its abstract, so it casts no vote on the map. Cited by 13 papers.
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Who cites it
13 citing papers in PubMed, 33 citations in OpenAlex.
- Recent progress in the exploitation of anti-cancer small molecules targeting angiogenesis.Journal of enzyme inhibition and medicinal chemistry · 2025Review
- Recent advances in focal adhesion kinase (FAK)-targeting antitumor agents.RSC advances · 2025Review
- Methods for the Discovery and Identification of Small Molecules Targeting Oxidative Stress-Related Protein-Protein Interactions: An Update.Antioxidants (Basel, Switzerland) · 2022Review
- FAK inhibitors as promising anticancer targets: present and future directions.Future medicinal chemistry · 2021Review
- Article
- Structure-Based Virtual Screening, Synthesis and Biological Evaluation of Potential FAK-FAT Domain Inhibitors for Treatment of Metastatic Cancer.Molecules (Basel, Switzerland) · 2020Article
- Review
- Diverse Coordinative Zinc Complexes Containing Amido-Pyridinate Ligands: Structural and Catalytic Studies.Frontiers in chemistry · 2018Article
- Characterizing the Hot Spots Involved in RON-MSPβ Complex Formation UsingAdvanced pharmaceutical bulletin · 2017Article
- SASH1 mediates sensitivity of breast cancer cells to chloropyramine and is associated with prognosis in breast cancer.Oncotarget · 2016Article
- FOXO3-NF-κB RelA Protein Complexes Reduce Proinflammatory Cell Signaling and Function.Journal of immunology (Baltimore, Md. : 1950) · 2015Article
- Anti-metastatic action of FAK inhibitor OXA-11 in combination with VEGFR-2 signaling blockade in pancreatic neuroendocrine tumors.Clinical & experimental metastasis · 2015Article
- Targeting the C-terminal focal adhesion kinase scaffold in pancreatic cancer.Cancer letters · 2014Article
Corrections and comments
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Authors and funding
6 authors at 2 institutions in 1 country.
Funding
Abstract
Focal adhesion kinase (FAK) and vascular endothelial growth factor receptor 3 (VEGFR3) are tyrosine kinases, which function as key modulators of survival and metastasis signals in cancer cells. Previously, we reported that small molecule chlorpyramine hydrochloride (C4) specifically targets the interaction between FAK and VEGFR3 and exhibits anti-tumor efficacy. In this study, we designed and synthesized a series of 1 (C4) analogs on the basis of structure activity relationship and molecular modeling. The resulting new compounds were evaluated for their binding to the FAT domain of FAK and anti-cancer activity. Amongst all tested analogs, compound 29 augmented anti-proliferative activity in multiple cancer cell lines with stronger binding to the FAT domain of FAK and disrupted the FAK-VEGFR3 interaction. In conclusion, we hope that this work will contribute to further studies of more potent and selective FAK-VEGFR3 protein-protein interaction inhibitors.
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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.