Cancer stem cells (CSCs) are associated with drug resistance, metastasis and recurrence of cancer. A synthetic binder of CSCs can provide a valuable tool to study the biology of CSCs and a lead to develop imaging, diagnostic and therapeutic agents targeting CSCs. Herein, a synthetic ligand (1) that specifically binds to CSCs over non‐CSCs of breast cancer cells was identified for the first time via a cell‐binding screening of a chemical library. The ligand 1 showed specific binding to CD24−/CD44+/ALDH+ CSC population of MCF‐7 and MDA‐MB‐231. We have demonstrated that 1‐immobilized beads can be used as matrices for affinity isolation of 1‐binding CSC population from breast cancer cells. The 1‐binding population showed significantly increased expressions of stemness‐associated transcription factors. Importantly, the 1‐binding population demonstrated accelerated tumor growth in vivo, and the resulting tumor displayed an increased migratory activity and high expressions of CSC markers.
Chemistry - A European Journal – Wiley
Published: Jan 12, 2018
Keywords: ; ; ; ;
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