Citation: Kun Liu, Yulin Cong, Xiongfeng Luo, Meicun Yao, Zhiyong Xie, Hao Li. Utilizing bivalent aptamers as first DNA agonist to activate RTKs heterodimer of different families[J]. Chinese Chemical Letters, ;2025, 36(1): 109839. doi: 10.1016/j.cclet.2024.109839 shu

Utilizing bivalent aptamers as first DNA agonist to activate RTKs heterodimer of different families

Kun Liu ¹ ,
Yulin Cong ¹ ,
Xiongfeng Luo ,
Meicun Yao ^*, ,
Zhiyong Xie ^*, ,
Hao Li ^*,

School of Pharmaceutical Sciences (Shenzhen), Shenzhen Campus of Sun Yat-sen University, Shenzhen 518107, China

Lssymc@mail.sysu.edu.cn

xiezhy@mail.sysu.edu.cn

lihao258@mail.sysu.edu.cn

Received Date: 4 February 2024
Revised Date: 1 March 2024
Accepted Date: 27 March 2024
Available Online: 28 March 2024

Figures(4)

Heterodimerization in RTKs is of vital importance in the RTK signaling and cell functions. Heterodimerization between RTKs can result in diversity of downstream signals, increasing the ability of cells to respond to external experiments. Traditional RTKs heterodimerization always occur in the same families and is lack of agonists to activate the heterodimeric RTKs signaling pathway. Herein, we developed the DNA agonist based on bivalent aptamers for the heterodimerized RTKs of different families, AF/AM-1, which could simultaneously activate FGFR1 and c-Met signaling. It is the first agonist that realizing the heterodimerization and activation of FGFR1 and c-Met, two different RTK families. The activation of FGFR1/c-Met heterodimer result in the down-stream signals transduction, such as the phosphorylation of Akt and Erk, inducing the cell migration and proliferation. The DNA agonist for RTK heterodimer of different families would have potential applications in the fields of biomedicine.
- DNA Agonist,
- Bivalent aptamers,
- RTKs heterodimer
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