(Thio)chromenone derivatives exhibit anti-metastatic effects through selective inhibition of uPAR in cancer cell lines: discovery of an uPAR-targeting fluorescent probe
A class of (thio)chromenone derivatives has been identified as suitable ligands for uPAR, a glycoprotein with a prognostic value in a large number of human cancers. The (thio)chromenone agents actively inhibited the binding of uPAR to uPA with a binding affinity of 18.6 nM, reducing cell migration in the wound healing assay by up to 40% without apparent cell motility. The discovery of an uPAR-targeting fluorescent probe was also made in this study that can selectively bind to the membrane uPAR, providing valuable molecular insights into the role of uPAR in cancer metastasis. This study should serve as a basis for the development of new uPAR-targeting agents that can control the metastatic potential of cancer cells with minimal cytotoxicity.
Authors
- Hye‐Jung Yoon (ORCID: https://orcid.org/0000-0002-3534-3295)
- So‐Young Chun
- Hun Young Kim (ORCID: https://orcid.org/0000-0002-8461-8910)
- Kyungsoo Oh (ORCID: https://orcid.org/0000-0002-4566-6573)
- Hye Ran Koh (ORCID: https://orcid.org/0000-0001-6262-7018)
- Seung Wook Ham (ORCID: https://orcid.org/0000-0001-9816-6911)
- Hyung Ho Lee (ORCID: https://orcid.org/0000-0003-4160-0216)
- Tae‐Il Kim (ORCID: https://orcid.org/0000-0003-2644-3427)
- Youngmi Kim (ORCID: https://orcid.org/0000-0003-2189-8342)
- Jiwon Oh (ORCID: https://orcid.org/0000-0003-0129-3936)
- Chanhee Park (ORCID: https://orcid.org/0000-0001-8380-4976)
Institutions
- Seoul National University (KR)
- Korea University (KR)
- Kyung Hee University (KR)
- Chung-Ang University (KR)
Publication Details
- Journal
- Chemical Communications
- Published
- 2024-12-04
- DOI
- https://doi.org/10.1039/d4cc05907g
- Citations
- 1
- Primary Topic
- Oxidative Organic Chemistry Reactions
- Type
- article
- Field-Weighted Citation Impact
- 0.25
Funders
- National Research Foundation of Korea