Cancer stem cells (CSCs) contribute to the recurrence and metastasis of cancer. The discovery of synthetic binders of CSCs could help with studying the biology of CSCs as well as in developing diagnostic and therapeutic agents targeting CSCs.

Jiyong Lee and colleagues, University of Texas at Dallas, USA, have isolated the synthetic ligand CL-1-19-1 that specifically binds to CSCs over non-CSCs of breast cancer cells. The binder was identified using a high-throughput screening with a one-bead-one-compound (OBOC) combinatorial chemistry library. OBOC libraries have been previously used to isolate ligands that bind specifically to cancer cells over normal cells but not, as in this case, to isolate ligands that bind to a sub-population of the cancer cells such as CSCs.

The ligand showed specific binding to CD24⁻/CD44⁺/ALDH⁺ CSC population of the breast cancer cell lines MCF-7 and MDA-MB-231. The CL-1-19-1-bound cell population shows greater capability of tumor initiation and growth in a mouse model of human breast cancer. According to the researchers, their synthetic binder of breast CSCs can be used to advance knowledge of CSCs and to develop novel imaging/diagnostic/therapeutic agents to detect breast CSCs in vivo.

• A Synthetic Binder of Breast Cancer Stem Cells,
  Luxi Chen, Chao Long, Kha Andy Minh Tran, Jiyong Lee,
  Chem. Eur. J. 2018.
  https://doi.org/10.1002/chem.201705663